Cayman

Showing 37951–38100 of 45550 results

  • Rimantadine is a derivative of amantadine (Item No. 21364) with antiviral activity.{22179} It inhibits recombinant influenza A matrix protein 2 (M2) expressed in X. laevis oocytes (IC50 = 10.8 µM) and recombinant hepatitis C virus (HCV) p7 protein expressed in HEK293 cells (IC50s = 0.7, 24, 1.6, and 3.0 nM for HCV genotypes 1a, 2a, 3a, and 4a, respectively).{43207,43208} Rimantadine inhibits cytotoxicity induced by the influenza A strains A/PR/8/34 (H1N1) and A/HK/7/87 (H3N2), but not the influenza B strain B/HK/72, in MDCK cells (EC50s = 18, 0.62, and >500 µM, respectively).{42218} It increases the survival rate of mice infected with the influenza A strain A2/Jap/305 from 20 to 90% when administered at a dose of 24 mg/kg two hours post-infection, with the survival rate decreasing when rimantadine is administered at longer timepoints following infection.{43209} It also has trypanocidal activity against bloodstream forms of T. brucei in vitro (IC50 = 1.26 µg/ml).{43210} Formulations containing rimantadine have been used in the prophylaxis and treatment of influenza A.  

     

    Brand:
    Cayman
    SKU:23838 - 25 mg

    Available on backorder

  • Rimantadine is a derivative of amantadine (Item No. 21364) with antiviral activity.{22179} It inhibits recombinant influenza A matrix protein 2 (M2) expressed in X. laevis oocytes (IC50 = 10.8 µM) and recombinant hepatitis C virus (HCV) p7 protein expressed in HEK293 cells (IC50s = 0.7, 24, 1.6, and 3.0 nM for HCV genotypes 1a, 2a, 3a, and 4a, respectively).{43207,43208} Rimantadine inhibits cytotoxicity induced by the influenza A strains A/PR/8/34 (H1N1) and A/HK/7/87 (H3N2), but not the influenza B strain B/HK/72, in MDCK cells (EC50s = 18, 0.62, and >500 µM, respectively).{42218} It increases the survival rate of mice infected with the influenza A strain A2/Jap/305 from 20 to 90% when administered at a dose of 24 mg/kg two hours post-infection, with the survival rate decreasing when rimantadine is administered at longer timepoints following infection.{43209} It also has trypanocidal activity against bloodstream forms of T. brucei in vitro (IC50 = 1.26 µg/ml).{43210} Formulations containing rimantadine have been used in the prophylaxis and treatment of influenza A.  

     

    Brand:
    Cayman
    SKU:23838 - 250 mg

    Available on backorder

  • Rimantadine is a derivative of amantadine (Item No. 21364) with antiviral activity.{22179} It inhibits recombinant influenza A matrix protein 2 (M2) expressed in X. laevis oocytes (IC50 = 10.8 µM) and recombinant hepatitis C virus (HCV) p7 protein expressed in HEK293 cells (IC50s = 0.7, 24, 1.6, and 3.0 nM for HCV genotypes 1a, 2a, 3a, and 4a, respectively).{43207,43208} Rimantadine inhibits cytotoxicity induced by the influenza A strains A/PR/8/34 (H1N1) and A/HK/7/87 (H3N2), but not the influenza B strain B/HK/72, in MDCK cells (EC50s = 18, 0.62, and >500 µM, respectively).{42218} It increases the survival rate of mice infected with the influenza A strain A2/Jap/305 from 20 to 90% when administered at a dose of 24 mg/kg two hours post-infection, with the survival rate decreasing when rimantadine is administered at longer timepoints following infection.{43209} It also has trypanocidal activity against bloodstream forms of T. brucei in vitro (IC50 = 1.26 µg/ml).{43210} Formulations containing rimantadine have been used in the prophylaxis and treatment of influenza A.  

     

    Brand:
    Cayman
    SKU:23838 - 50 mg

    Available on backorder

  • Rimegepant is an orally bioavailable antagonist of the calcitonin gene-related peptide (CGRP) receptor (Ki = 0.027 nM).{47524} It inhibits cAMP production stimulated by α-CGRP (Item No. 24405) in SK-N-MC human neuroblastoma cells (IC50 = 0.14 nM). Rimegepant (7 mg/kg, s.c.) reduces human α-CGRP-induced increases in facial blood flow, a surrogate for changes in intracranial artery diameter, in anesthetized marmosets.  

     

    Brand:
    Cayman
    SKU:26338 - 1 mg

    Available on backorder

  • Rimegepant is an orally bioavailable antagonist of the calcitonin gene-related peptide (CGRP) receptor (Ki = 0.027 nM).{47524} It inhibits cAMP production stimulated by α-CGRP (Item No. 24405) in SK-N-MC human neuroblastoma cells (IC50 = 0.14 nM). Rimegepant (7 mg/kg, s.c.) reduces human α-CGRP-induced increases in facial blood flow, a surrogate for changes in intracranial artery diameter, in anesthetized marmosets.  

     

    Brand:
    Cayman
    SKU:26338 - 10 mg

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  • Rimegepant is an orally bioavailable antagonist of the calcitonin gene-related peptide (CGRP) receptor (Ki = 0.027 nM).{47524} It inhibits cAMP production stimulated by α-CGRP (Item No. 24405) in SK-N-MC human neuroblastoma cells (IC50 = 0.14 nM). Rimegepant (7 mg/kg, s.c.) reduces human α-CGRP-induced increases in facial blood flow, a surrogate for changes in intracranial artery diameter, in anesthetized marmosets.  

     

    Brand:
    Cayman
    SKU:26338 - 25 mg

    Available on backorder

  • Rimegepant is an orally bioavailable antagonist of the calcitonin gene-related peptide (CGRP) receptor (Ki = 0.027 nM).{47524} It inhibits cAMP production stimulated by α-CGRP (Item No. 24405) in SK-N-MC human neuroblastoma cells (IC50 = 0.14 nM). Rimegepant (7 mg/kg, s.c.) reduces human α-CGRP-induced increases in facial blood flow, a surrogate for changes in intracranial artery diameter, in anesthetized marmosets.  

     

    Brand:
    Cayman
    SKU:26338 - 5 mg

    Available on backorder

  • Rimonabant is a potent and selective cannabinoid (CB) receptor 1 antagonist (Kis = 5.6 and >1,000 nM for CB1 and CB2, respectively).{3133} In rodent models, rimonabant induces lipolysis, reduces hepatomegaly, decreases body weight, and improves dyslipidemia by reducing triglyceride, free fatty acid, and total cholesterol levels and by increasing HDL/LDL ratios.{17168} Rimonabant elicits antiproliferative and immunomodulatory effects (e.g., cell cycle arrest, increased expression of IκB and phosphorylated Akt, and decreased expression of NF-κB, phosphorylated ERK1/2, COX-2, and iNOS) in vitro.{17167}  

     

    Brand:
    Cayman
    SKU:9000484 - 10 mg

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  • Rimonabant is a potent and selective cannabinoid (CB) receptor 1 antagonist (Kis = 5.6 and >1,000 nM for CB1 and CB2, respectively).{3133} In rodent models, rimonabant induces lipolysis, reduces hepatomegaly, decreases body weight, and improves dyslipidemia by reducing triglyceride, free fatty acid, and total cholesterol levels and by increasing HDL/LDL ratios.{17168} Rimonabant elicits antiproliferative and immunomodulatory effects (e.g., cell cycle arrest, increased expression of IκB and phosphorylated Akt, and decreased expression of NF-κB, phosphorylated ERK1/2, COX-2, and iNOS) in vitro.{17167}  

     

    Brand:
    Cayman
    SKU:9000484 - 25 mg

    Available on backorder

  • Rimonabant is a potent and selective cannabinoid (CB) receptor 1 antagonist (Kis = 5.6 and >1,000 nM for CB1 and CB2, respectively).{3133} In rodent models, rimonabant induces lipolysis, reduces hepatomegaly, decreases body weight, and improves dyslipidemia by reducing triglyceride, free fatty acid, and total cholesterol levels and by increasing HDL/LDL ratios.{17168} Rimonabant elicits antiproliferative and immunomodulatory effects (e.g., cell cycle arrest, increased expression of IκB and phosphorylated Akt, and decreased expression of NF-κB, phosphorylated ERK1/2, COX-2, and iNOS) in vitro.{17167}  

     

    Brand:
    Cayman
    SKU:9000484 - 5 mg

    Available on backorder

  • Rimonabant is a potent and selective cannabinoid (CB) receptor 1 antagonist (Kis = 5.6 and >1,000 nM for CB1 and CB2, respectively).{3133} In rodent models, rimonabant induces lipolysis, reduces hepatomegaly, decreases body weight, and improves dyslipidemia by reducing triglyceride, free fatty acid, and total cholesterol levels and by increasing HDL/LDL ratios.{17168} Rimonabant elicits antiproliferative and immunomodulatory effects (e.g., cell cycle arrest, increased expression of IκB and phosphorylated Akt, and decreased expression of NF-κB, phosphorylated ERK1/2, COX-2, and iNOS) in vitro.{17167}  

     

    Brand:
    Cayman
    SKU:9000484 - 50 mg

    Available on backorder

  • Rimonabant-d10 contains 10 deuterium atoms at the 2, 2’, 3, 3’, 4, 4’, 5, 5’, 6, and 6’ positions. It is intended for use as an internal standard for the quantification of rimonabant (Item No. 9000484) by GC- or LC-MS. Rimonabant, also known as SR141716, was the first selective central cannabinoid (CB1) receptor inverse agonist (Ki = 1.8 nM) to be developed as an appetite suppressant and anti-obesity drug.{3133} It is widely used as a tool to investigate CB receptor properties and the mechanisms by which CB agonists exert their pharmacological effects.  

     

    Brand:
    Cayman
    SKU:9001821 - 1 mg

    Available on backorder

  • Rimonabant-d10 contains 10 deuterium atoms at the 2, 2’, 3, 3’, 4, 4’, 5, 5’, 6, and 6’ positions. It is intended for use as an internal standard for the quantification of rimonabant (Item No. 9000484) by GC- or LC-MS. Rimonabant, also known as SR141716, was the first selective central cannabinoid (CB1) receptor inverse agonist (Ki = 1.8 nM) to be developed as an appetite suppressant and anti-obesity drug.{3133} It is widely used as a tool to investigate CB receptor properties and the mechanisms by which CB agonists exert their pharmacological effects.  

     

    Brand:
    Cayman
    SKU:9001821 - 500 µg

    Available on backorder

  • Riociguat is a stimulator of soluble guanylate cyclase (sGC).{36864},{26751} It stimulates recombinant sGC in a concentration-dependent manner in vitro by up to 73-fold when used at a concentration of 100 μM or by up to 112-fold when used in combination with the nitric oxide (NO) donor DEA NONOate (Item No. 82100).{36864} It has no effect on phosphodiesterases PDE1-9 and PDE11 when used at concentrations up to 3 μM. Riociguat (1 and 10 mg/kg) reduces pulmonary and systemic arterial pressure in a rabbit model of acute pulmonary arterial hypertension (PAH) induced by U-46619 (Item No. 16450). It also inhibits increases in right ventricular systolic pressure, right heart hypertrophy, and pulmonary artery muscularization in hypoxia-induced mouse and monocrotaline-injected rat models of chronic PAH when administered at a dose of 10 mg/kg. Formulations containing riociguat have been used in the treatment of chronic thromboembolic pulmonary hypertension (CTEPH) and PAH.  

     

    Brand:
    Cayman
    SKU:9000554 - 10 mg

    Available on backorder

  • Riociguat is a stimulator of soluble guanylate cyclase (sGC).{36864},{26751} It stimulates recombinant sGC in a concentration-dependent manner in vitro by up to 73-fold when used at a concentration of 100 μM or by up to 112-fold when used in combination with the nitric oxide (NO) donor DEA NONOate (Item No. 82100).{36864} It has no effect on phosphodiesterases PDE1-9 and PDE11 when used at concentrations up to 3 μM. Riociguat (1 and 10 mg/kg) reduces pulmonary and systemic arterial pressure in a rabbit model of acute pulmonary arterial hypertension (PAH) induced by U-46619 (Item No. 16450). It also inhibits increases in right ventricular systolic pressure, right heart hypertrophy, and pulmonary artery muscularization in hypoxia-induced mouse and monocrotaline-injected rat models of chronic PAH when administered at a dose of 10 mg/kg. Formulations containing riociguat have been used in the treatment of chronic thromboembolic pulmonary hypertension (CTEPH) and PAH.  

     

    Brand:
    Cayman
    SKU:9000554 - 25 mg

    Available on backorder

  • Riociguat is a stimulator of soluble guanylate cyclase (sGC).{36864},{26751} It stimulates recombinant sGC in a concentration-dependent manner in vitro by up to 73-fold when used at a concentration of 100 μM or by up to 112-fold when used in combination with the nitric oxide (NO) donor DEA NONOate (Item No. 82100).{36864} It has no effect on phosphodiesterases PDE1-9 and PDE11 when used at concentrations up to 3 μM. Riociguat (1 and 10 mg/kg) reduces pulmonary and systemic arterial pressure in a rabbit model of acute pulmonary arterial hypertension (PAH) induced by U-46619 (Item No. 16450). It also inhibits increases in right ventricular systolic pressure, right heart hypertrophy, and pulmonary artery muscularization in hypoxia-induced mouse and monocrotaline-injected rat models of chronic PAH when administered at a dose of 10 mg/kg. Formulations containing riociguat have been used in the treatment of chronic thromboembolic pulmonary hypertension (CTEPH) and PAH.  

     

    Brand:
    Cayman
    SKU:9000554 - 5 mg

    Available on backorder

  • Riociguat is a stimulator of soluble guanylate cyclase (sGC).{36864},{26751} It stimulates recombinant sGC in a concentration-dependent manner in vitro by up to 73-fold when used at a concentration of 100 μM or by up to 112-fold when used in combination with the nitric oxide (NO) donor DEA NONOate (Item No. 82100).{36864} It has no effect on phosphodiesterases PDE1-9 and PDE11 when used at concentrations up to 3 μM. Riociguat (1 and 10 mg/kg) reduces pulmonary and systemic arterial pressure in a rabbit model of acute pulmonary arterial hypertension (PAH) induced by U-46619 (Item No. 16450). It also inhibits increases in right ventricular systolic pressure, right heart hypertrophy, and pulmonary artery muscularization in hypoxia-induced mouse and monocrotaline-injected rat models of chronic PAH when administered at a dose of 10 mg/kg. Formulations containing riociguat have been used in the treatment of chronic thromboembolic pulmonary hypertension (CTEPH) and PAH.  

     

    Brand:
    Cayman
    SKU:9000554 - 50 mg

    Available on backorder

  • RIPGBM is a prodrug form of the pro-apoptotic compound cRIPGBM.{35798} It is converted to cRIPGBM in GBM-1 glioblastoma multiforme (GBM) cancer stem cells (CSCs) but not primary human lung fibroblasts (HLFs). RIPGBM induces apoptosis in GBM CSCs (EC50 = ≤500 nM) and selectively reduces survival of GBM-1 cells (EC50 = 0.22 μM) over human neural stem cells, primary human astrocytes, and primary HLFs (EC50s = 1.7, 2.9, and 3.5 μM, respectively). It reduces tumor growth in a GBM mouse xenograft model using patient-derived GBM-39 cells engineered to express IR fluorescent protein 720 (IRFP720) when administered at a dose of 50 mg/kg twice per day.  

     

    Brand:
    Cayman
    SKU:27860 - 1 mg

    Available on backorder

  • RIPGBM is a prodrug form of the pro-apoptotic compound cRIPGBM.{35798} It is converted to cRIPGBM in GBM-1 glioblastoma multiforme (GBM) cancer stem cells (CSCs) but not primary human lung fibroblasts (HLFs). RIPGBM induces apoptosis in GBM CSCs (EC50 = ≤500 nM) and selectively reduces survival of GBM-1 cells (EC50 = 0.22 μM) over human neural stem cells, primary human astrocytes, and primary HLFs (EC50s = 1.7, 2.9, and 3.5 μM, respectively). It reduces tumor growth in a GBM mouse xenograft model using patient-derived GBM-39 cells engineered to express IR fluorescent protein 720 (IRFP720) when administered at a dose of 50 mg/kg twice per day.  

     

    Brand:
    Cayman
    SKU:27860 - 10 mg

    Available on backorder

  • RIPGBM is a prodrug form of the pro-apoptotic compound cRIPGBM.{35798} It is converted to cRIPGBM in GBM-1 glioblastoma multiforme (GBM) cancer stem cells (CSCs) but not primary human lung fibroblasts (HLFs). RIPGBM induces apoptosis in GBM CSCs (EC50 = ≤500 nM) and selectively reduces survival of GBM-1 cells (EC50 = 0.22 μM) over human neural stem cells, primary human astrocytes, and primary HLFs (EC50s = 1.7, 2.9, and 3.5 μM, respectively). It reduces tumor growth in a GBM mouse xenograft model using patient-derived GBM-39 cells engineered to express IR fluorescent protein 720 (IRFP720) when administered at a dose of 50 mg/kg twice per day.  

     

    Brand:
    Cayman
    SKU:27860 - 5 mg

    Available on backorder

  • Risdiplam is a survival of motor neuron-2 (SMN2) splicing modifier.{50413} It enhances SMN2 splicing (EC1.5x = 40 nM) and increases SMN protein levels (EC1.5x = 163 nM) in cellular assays. Risdiplam (3 mg/kg) increases brain and quadricep muscle SMN protein levels in the adult C/C-allele mouse model of mild spinal muscular atrophy (SMA) and the SMND7 neonate mouse model of severe SMA. It also increases the number of vesicular glutamate transporter 1 (vGLUT1) proprioceptive inputs on motor neurons, the number of L3 to L5 spinal motor neurons, the percentage of fully innervated neuromuscular junctions (NMJs), and the size of the extensor digitorum longus muscles in adult SMND7 mice. Formulations containing risdiplam have been used in the treatment of spinal muscular atrophy.  

     

    Brand:
    Cayman
    SKU:29028 - 1 mg

    Available on backorder

  • Risdiplam is a survival of motor neuron-2 (SMN2) splicing modifier.{50413} It enhances SMN2 splicing (EC1.5x = 40 nM) and increases SMN protein levels (EC1.5x = 163 nM) in cellular assays. Risdiplam (3 mg/kg) increases brain and quadricep muscle SMN protein levels in the adult C/C-allele mouse model of mild spinal muscular atrophy (SMA) and the SMND7 neonate mouse model of severe SMA. It also increases the number of vesicular glutamate transporter 1 (vGLUT1) proprioceptive inputs on motor neurons, the number of L3 to L5 spinal motor neurons, the percentage of fully innervated neuromuscular junctions (NMJs), and the size of the extensor digitorum longus muscles in adult SMND7 mice. Formulations containing risdiplam have been used in the treatment of spinal muscular atrophy.  

     

    Brand:
    Cayman
    SKU:29028 - 10 mg

    Available on backorder

  • Risdiplam is a survival of motor neuron-2 (SMN2) splicing modifier.{50413} It enhances SMN2 splicing (EC1.5x = 40 nM) and increases SMN protein levels (EC1.5x = 163 nM) in cellular assays. Risdiplam (3 mg/kg) increases brain and quadricep muscle SMN protein levels in the adult C/C-allele mouse model of mild spinal muscular atrophy (SMA) and the SMND7 neonate mouse model of severe SMA. It also increases the number of vesicular glutamate transporter 1 (vGLUT1) proprioceptive inputs on motor neurons, the number of L3 to L5 spinal motor neurons, the percentage of fully innervated neuromuscular junctions (NMJs), and the size of the extensor digitorum longus muscles in adult SMND7 mice. Formulations containing risdiplam have been used in the treatment of spinal muscular atrophy.  

     

    Brand:
    Cayman
    SKU:29028 - 25 mg

    Available on backorder

  • Risdiplam is a survival of motor neuron-2 (SMN2) splicing modifier.{50413} It enhances SMN2 splicing (EC1.5x = 40 nM) and increases SMN protein levels (EC1.5x = 163 nM) in cellular assays. Risdiplam (3 mg/kg) increases brain and quadricep muscle SMN protein levels in the adult C/C-allele mouse model of mild spinal muscular atrophy (SMA) and the SMND7 neonate mouse model of severe SMA. It also increases the number of vesicular glutamate transporter 1 (vGLUT1) proprioceptive inputs on motor neurons, the number of L3 to L5 spinal motor neurons, the percentage of fully innervated neuromuscular junctions (NMJs), and the size of the extensor digitorum longus muscles in adult SMND7 mice. Formulations containing risdiplam have been used in the treatment of spinal muscular atrophy.  

     

    Brand:
    Cayman
    SKU:29028 - 5 mg

    Available on backorder

  • Risedronate is a heterocyclic orally active aminobisphosphonate.{32680} Like other bisphosphonates, it inhibits bone resorption.{32679,32680} In addition, it has antimalarial activity and inhibits growth of P. falciparum in vitro (IC50 = 20.3 µM) and P. berghei in vivo (25 mg/kg for one week).{35110} It also inhibits protein prenylation by preventing the transfer of a farnesyl pyrophosphate group to parasite proteins. Formulations containing risedronate have been used to reduce fracture risk in both age- and steroid-related osteoporosis.{21586,32679,32680}  

     

    Brand:
    Cayman
    SKU:20740 -

    Available on backorder

  • Risedronate is a heterocyclic orally active aminobisphosphonate.{32680} Like other bisphosphonates, it inhibits bone resorption.{32679,32680} In addition, it has antimalarial activity and inhibits growth of P. falciparum in vitro (IC50 = 20.3 µM) and P. berghei in vivo (25 mg/kg for one week).{35110} It also inhibits protein prenylation by preventing the transfer of a farnesyl pyrophosphate group to parasite proteins. Formulations containing risedronate have been used to reduce fracture risk in both age- and steroid-related osteoporosis.{21586,32679,32680}  

     

    Brand:
    Cayman
    SKU:20740 -

    Available on backorder

  • Risedronate is a heterocyclic orally active aminobisphosphonate.{32680} Like other bisphosphonates, it inhibits bone resorption.{32679,32680} In addition, it has antimalarial activity and inhibits growth of P. falciparum in vitro (IC50 = 20.3 µM) and P. berghei in vivo (25 mg/kg for one week).{35110} It also inhibits protein prenylation by preventing the transfer of a farnesyl pyrophosphate group to parasite proteins. Formulations containing risedronate have been used to reduce fracture risk in both age- and steroid-related osteoporosis.{21586,32679,32680}  

     

    Brand:
    Cayman
    SKU:20740 -

    Available on backorder

  • Risedronate is a heterocyclic orally active aminobisphosphonate.{32680} Like other bisphosphonates, it inhibits bone resorption.{32679,32680} In addition, it has antimalarial activity and inhibits growth of P. falciparum in vitro (IC50 = 20.3 µM) and P. berghei in vivo (25 mg/kg for one week).{35110} It also inhibits protein prenylation by preventing the transfer of a farnesyl pyrophosphate group to parasite proteins. Formulations containing risedronate have been used to reduce fracture risk in both age- and steroid-related osteoporosis.{21586,32679,32680}  

     

    Brand:
    Cayman
    SKU:20740 -

    Available on backorder

  • Risperidone is an atypical antipsychotic that binds to dopamine D2 receptors (Ki = 3 nM) and the serotonin (5-HT) receptor subtype 5-HT2A (Ki = 0.12 nM).{39942,21347} It also binds to dopamine D4, α1- and α2-adrenergic, 5-HT1C, 5-HT1D, and histamine H1 receptors (Kis = 7, 0.81, 7.3, 47, 52, and 2.1 nM, respectively). Risperidone (0.1 mg/kg per day, i.p.) attenuates deficits in prepulse inhibition of the acoustic startle response, but not deficits in social interaction, in a rat neonatal ventral hippocampal lesion model of schizophrenia.{39941} Formulations containing risperidone have been used in the treatment of schizophrenia and bipolar disorder.  

     

    Brand:
    Cayman
    SKU:-
  • Risperidone is an atypical antipsychotic that binds to dopamine D2 receptors (Ki = 3 nM) and the serotonin (5-HT) receptor subtype 5-HT2A (Ki = 0.12 nM).{39942,21347} It also binds to dopamine D4, α1- and α2-adrenergic, 5-HT1C, 5-HT1D, and histamine H1 receptors (Kis = 7, 0.81, 7.3, 47, 52, and 2.1 nM, respectively). Risperidone (0.1 mg/kg per day, i.p.) attenuates deficits in prepulse inhibition of the acoustic startle response, but not deficits in social interaction, in a rat neonatal ventral hippocampal lesion model of schizophrenia.{39941} Formulations containing risperidone have been used in the treatment of schizophrenia and bipolar disorder.  

     

    Brand:
    Cayman
    SKU:-
  • Risperidone is an atypical antipsychotic that binds to dopamine D2 receptors (Ki = 3 nM) and the serotonin (5-HT) receptor subtype 5-HT2A (Ki = 0.12 nM).{39942,21347} It also binds to dopamine D4, α1- and α2-adrenergic, 5-HT1C, 5-HT1D, and histamine H1 receptors (Kis = 7, 0.81, 7.3, 47, 52, and 2.1 nM, respectively). Risperidone (0.1 mg/kg per day, i.p.) attenuates deficits in prepulse inhibition of the acoustic startle response, but not deficits in social interaction, in a rat neonatal ventral hippocampal lesion model of schizophrenia.{39941} Formulations containing risperidone have been used in the treatment of schizophrenia and bipolar disorder.  

     

    Brand:
    Cayman
    SKU:-
  • Risperidone E-oxime is a potential impurity found in commercial preparations of risperidone.{34751,34752} Risperidone (Item No. 13629) is a longer-acting benzisoxazole derivative used for treating schizophrenia, and also the psychotic, affective, or behavioral symptoms associated with other disorders.{17629,17608} This second-generation antipsychotic was designed to antagonize both D2 and 5-HT2A receptors.{22210,21347} It has little effect on cholinergic and β-adrenergic receptors but does affect α2-adrenergic and histamine H1 receptors.{22210,21347}  

     

    Brand:
    Cayman
    SKU:22156 -

    Out of stock

  • Risperidone E-oxime is a potential impurity found in commercial preparations of risperidone.{34751,34752} Risperidone (Item No. 13629) is a longer-acting benzisoxazole derivative used for treating schizophrenia, and also the psychotic, affective, or behavioral symptoms associated with other disorders.{17629,17608} This second-generation antipsychotic was designed to antagonize both D2 and 5-HT2A receptors.{22210,21347} It has little effect on cholinergic and β-adrenergic receptors but does affect α2-adrenergic and histamine H1 receptors.{22210,21347}  

     

    Brand:
    Cayman
    SKU:22156 -

    Out of stock

  • Risperidone E-oxime is a potential impurity found in commercial preparations of risperidone.{34751,34752} Risperidone (Item No. 13629) is a longer-acting benzisoxazole derivative used for treating schizophrenia, and also the psychotic, affective, or behavioral symptoms associated with other disorders.{17629,17608} This second-generation antipsychotic was designed to antagonize both D2 and 5-HT2A receptors.{22210,21347} It has little effect on cholinergic and β-adrenergic receptors but does affect α2-adrenergic and histamine H1 receptors.{22210,21347}  

     

    Brand:
    Cayman
    SKU:22156 -

    Out of stock

  • Risperidone E-oxime is a potential impurity found in commercial preparations of risperidone.{34751,34752} Risperidone (Item No. 13629) is a longer-acting benzisoxazole derivative used for treating schizophrenia, and also the psychotic, affective, or behavioral symptoms associated with other disorders.{17629,17608} This second-generation antipsychotic was designed to antagonize both D2 and 5-HT2A receptors.{22210,21347} It has little effect on cholinergic and β-adrenergic receptors but does affect α2-adrenergic and histamine H1 receptors.{22210,21347}  

     

    Brand:
    Cayman
    SKU:22156 -

    Out of stock

  • Risperidone-d5 is intended for use as an internal standard for the quantification of risperidone (Item No. 13629) by GC- or LC-MS. Risperidone is an atypical antipsychotic that binds to dopamine D2 receptors (Ki = 3 nM) and the serotonin (5-HT) receptor subtype 5-HT2A (Ki = 0.12 nM).{39942,21347} It also binds to dopamine D4, α1- and α2-adrenergic, 5-HT1C, 5-HT1D, and histamine H1 receptors (Kis = 7, 0.81, 7.3, 47, 52, and 2.1 nM, respectively). Risperidone (0.1 mg/kg per day, i.p.) attenuates deficits in prepulse inhibition of the acoustic startle response, but not deficits in social interaction, in a rat neonatal ventral hippocampal lesion model of schizophrenia.{39941} Formulations containing risperidone have been used in the treatment of schizophrenia and bipolar disorder.  

     

    Brand:
    Cayman
    SKU:10010570 - 1 mg

    Available on backorder

  • Risperidone-d5 is intended for use as an internal standard for the quantification of risperidone (Item No. 13629) by GC- or LC-MS. Risperidone is an atypical antipsychotic that binds to dopamine D2 receptors (Ki = 3 nM) and the serotonin (5-HT) receptor subtype 5-HT2A (Ki = 0.12 nM).{39942,21347} It also binds to dopamine D4, α1- and α2-adrenergic, 5-HT1C, 5-HT1D, and histamine H1 receptors (Kis = 7, 0.81, 7.3, 47, 52, and 2.1 nM, respectively). Risperidone (0.1 mg/kg per day, i.p.) attenuates deficits in prepulse inhibition of the acoustic startle response, but not deficits in social interaction, in a rat neonatal ventral hippocampal lesion model of schizophrenia.{39941} Formulations containing risperidone have been used in the treatment of schizophrenia and bipolar disorder.  

     

    Brand:
    Cayman
    SKU:10010570 - 500 µg

    Available on backorder

  • Ristocetin A is an antibiotic that was used to treat staphylococcal infections.{32140} However, side effects of ristocetin A included thrombocytopenia and platelet agglutination. Ristocetin A is now used in two assays related to these actions, the ristocetin cofactor assay and the ristocetin-induced platelet aggregation assay. Both assays are used in the diagnosis of von Willebrand disease and other bleeding disorders.{32139,32140}  

     

    Brand:
    Cayman
    SKU:20601 -

    Available on backorder

  • Ristocetin A is an antibiotic that was used to treat staphylococcal infections.{32140} However, side effects of ristocetin A included thrombocytopenia and platelet agglutination. Ristocetin A is now used in two assays related to these actions, the ristocetin cofactor assay and the ristocetin-induced platelet aggregation assay. Both assays are used in the diagnosis of von Willebrand disease and other bleeding disorders.{32139,32140}  

     

    Brand:
    Cayman
    SKU:20601 -

    Available on backorder

  • HDM-2 (human double minute-2; MDM-2 in mouse) is a key negative regulator of p53 that binds to and targets p53 for proteasomal degradation. Overexpression of HDM-2 in some tumors leads to inactivation of p53 thereby allowing tumor cells to escape p53-induced apoptosis.{13684} RITA (reactivation of p53 and induction of tumor cell apoptosis) is a small molecule inhibitor of p53-HDM-2 interaction that can reactivate the tumor suppressor function of wild-type p53.{12386} It binds to p53 with an apparent Kd of 1.5 nM and prevents interaction with HDM-2 resulting in p53 stabilization, accumulation and activation.{12386} RITA potently inhibits the growth of a variety of cancer cell lines in the sub-micromolar range, inducing both DNA-protein and DNA-DNA cross links in human renal cancer cells.{13683} RITA reduced tumor size by 90% at a dose of 10 mg/kg in SCID mice bearing HCT116 tumors, and caused complete regression of A-498 tumor cell xenografts in nude mice at a dose of 45 mg/kg.{12386,13682}  

     

    Brand:
    Cayman
    SKU:10006426 - 1 mg

    Available on backorder

  • HDM-2 (human double minute-2; MDM-2 in mouse) is a key negative regulator of p53 that binds to and targets p53 for proteasomal degradation. Overexpression of HDM-2 in some tumors leads to inactivation of p53 thereby allowing tumor cells to escape p53-induced apoptosis.{13684} RITA (reactivation of p53 and induction of tumor cell apoptosis) is a small molecule inhibitor of p53-HDM-2 interaction that can reactivate the tumor suppressor function of wild-type p53.{12386} It binds to p53 with an apparent Kd of 1.5 nM and prevents interaction with HDM-2 resulting in p53 stabilization, accumulation and activation.{12386} RITA potently inhibits the growth of a variety of cancer cell lines in the sub-micromolar range, inducing both DNA-protein and DNA-DNA cross links in human renal cancer cells.{13683} RITA reduced tumor size by 90% at a dose of 10 mg/kg in SCID mice bearing HCT116 tumors, and caused complete regression of A-498 tumor cell xenografts in nude mice at a dose of 45 mg/kg.{12386,13682}  

     

    Brand:
    Cayman
    SKU:10006426 - 10 mg

    Available on backorder

  • HDM-2 (human double minute-2; MDM-2 in mouse) is a key negative regulator of p53 that binds to and targets p53 for proteasomal degradation. Overexpression of HDM-2 in some tumors leads to inactivation of p53 thereby allowing tumor cells to escape p53-induced apoptosis.{13684} RITA (reactivation of p53 and induction of tumor cell apoptosis) is a small molecule inhibitor of p53-HDM-2 interaction that can reactivate the tumor suppressor function of wild-type p53.{12386} It binds to p53 with an apparent Kd of 1.5 nM and prevents interaction with HDM-2 resulting in p53 stabilization, accumulation and activation.{12386} RITA potently inhibits the growth of a variety of cancer cell lines in the sub-micromolar range, inducing both DNA-protein and DNA-DNA cross links in human renal cancer cells.{13683} RITA reduced tumor size by 90% at a dose of 10 mg/kg in SCID mice bearing HCT116 tumors, and caused complete regression of A-498 tumor cell xenografts in nude mice at a dose of 45 mg/kg.{12386,13682}  

     

    Brand:
    Cayman
    SKU:10006426 - 5 mg

    Available on backorder

  • HDM-2 (human double minute-2; MDM-2 in mouse) is a key negative regulator of p53 that binds to and targets p53 for proteasomal degradation. Overexpression of HDM-2 in some tumors leads to inactivation of p53 thereby allowing tumor cells to escape p53-induced apoptosis.{13684} RITA (reactivation of p53 and induction of tumor cell apoptosis) is a small molecule inhibitor of p53-HDM-2 interaction that can reactivate the tumor suppressor function of wild-type p53.{12386} It binds to p53 with an apparent Kd of 1.5 nM and prevents interaction with HDM-2 resulting in p53 stabilization, accumulation and activation.{12386} RITA potently inhibits the growth of a variety of cancer cell lines in the sub-micromolar range, inducing both DNA-protein and DNA-DNA cross links in human renal cancer cells.{13683} RITA reduced tumor size by 90% at a dose of 10 mg/kg in SCID mice bearing HCT116 tumors, and caused complete regression of A-498 tumor cell xenografts in nude mice at a dose of 45 mg/kg.{12386,13682}  

     

    Brand:
    Cayman
    SKU:10006426 - 50 mg

    Available on backorder

  • Ritalinic acid is an inactive, major metabolite of methylphenidate (Item No. 11639), a schedule II drug in the United States commonly used as a psychostimulant for the treatment of attention-deficit hyperactivity disorder, also known as ADHD.{22009} Ritalinic acid is reported to reach plasma concentrations of 1-2 orders of magnitude greater than that of the parent drug and has been monitored in urine to ensure compliance with treatment programs.{25908} This product is intended for forensic and biological research purposes.  

     

    Brand:
    Cayman
    SKU:-
  • Ritalinic acid is an inactive, major metabolite of methylphenidate (Item No. 11639), a schedule II drug in the United States commonly used as a psychostimulant for the treatment of attention-deficit hyperactivity disorder, also known as ADHD.{22009} Ritalinic acid is reported to reach plasma concentrations of 1-2 orders of magnitude greater than that of the parent drug and has been monitored in urine to ensure compliance with treatment programs.{25908} This product is intended for forensic and biological research purposes.  

     

    Brand:
    Cayman
    SKU:-
  • Ritalinic acid is an inactive, major metabolite of methylphenidate (Item No. 11639), a schedule II drug in the United States commonly used as a psychostimulant for the treatment of attention-deficit hyperactivity disorder, also known as ADHD.{22009} Ritalinic acid is reported to reach plasma concentrations of 1-2 orders of magnitude greater than that of the parent drug and has been monitored in urine to ensure compliance with treatment programs.{25908} This product is intended for forensic and biological research purposes.  

     

    Brand:
    Cayman
    SKU:-
  • Ritanserin is a selective antagonist of the serotonin (5-HT) receptor subtype, 5-HT2A.{39295} In a radioligand binding assay, ritanserin exhibits high selectivity for 5-HT2A over 5-HT1 receptors (IC50s = 0.9 nM and >1000 nM, respectively).{39296} It also demonstrates relatively low affinity for histamine H1, dopamine D2, α1-adrenergic, and α2-adrenergic receptors (39-, 77-, 107-, and 166-fold lower relative to 5-HT2A, respectively). Ritanserin (2.5 mg/kg) is long-acting, occupying >70% of 5-HT2A sites up to 48 hours following subcutaneous administration to rats and guinea pigs. In vivo, ritanserin (10 mg/kg) blocks 5-hydroxy tryptophan-induced head twitches in rats.{39297}  

     

    Brand:
    Cayman
    SKU:21374 -

    Out of stock

  • Ritanserin is a selective antagonist of the serotonin (5-HT) receptor subtype, 5-HT2A.{39295} In a radioligand binding assay, ritanserin exhibits high selectivity for 5-HT2A over 5-HT1 receptors (IC50s = 0.9 nM and >1000 nM, respectively).{39296} It also demonstrates relatively low affinity for histamine H1, dopamine D2, α1-adrenergic, and α2-adrenergic receptors (39-, 77-, 107-, and 166-fold lower relative to 5-HT2A, respectively). Ritanserin (2.5 mg/kg) is long-acting, occupying >70% of 5-HT2A sites up to 48 hours following subcutaneous administration to rats and guinea pigs. In vivo, ritanserin (10 mg/kg) blocks 5-hydroxy tryptophan-induced head twitches in rats.{39297}  

     

    Brand:
    Cayman
    SKU:21374 -

    Out of stock

  • Ritanserin is a selective antagonist of the serotonin (5-HT) receptor subtype, 5-HT2A.{39295} In a radioligand binding assay, ritanserin exhibits high selectivity for 5-HT2A over 5-HT1 receptors (IC50s = 0.9 nM and >1000 nM, respectively).{39296} It also demonstrates relatively low affinity for histamine H1, dopamine D2, α1-adrenergic, and α2-adrenergic receptors (39-, 77-, 107-, and 166-fold lower relative to 5-HT2A, respectively). Ritanserin (2.5 mg/kg) is long-acting, occupying >70% of 5-HT2A sites up to 48 hours following subcutaneous administration to rats and guinea pigs. In vivo, ritanserin (10 mg/kg) blocks 5-hydroxy tryptophan-induced head twitches in rats.{39297}  

     

    Brand:
    Cayman
    SKU:21374 -

    Out of stock

  • Ritodrine is an agonist of β2-adrenergic receptors (β2-ARs).{47089} It induces relaxation of isolated pig detrusor muscle when used at concentrations ranging from 0.001 to 1 μM. Ritodrine (30 μg/ml) reduces electrically-induced isometric tension in myometrial strips isolated from rabbits on day 25 of pregnancy.{47090} It also suppresses spontaneous motility of and increases concentration of cyclic AMP (cAMP) in isolated pregnant rat uterus.{47091} Formulations containing ritodrine were previously used to stop premature labor.  

     

    Brand:
    Cayman
    SKU:26084 - 1 g

    Available on backorder

  • Ritodrine is an agonist of β2-adrenergic receptors (β2-ARs).{47089} It induces relaxation of isolated pig detrusor muscle when used at concentrations ranging from 0.001 to 1 μM. Ritodrine (30 μg/ml) reduces electrically-induced isometric tension in myometrial strips isolated from rabbits on day 25 of pregnancy.{47090} It also suppresses spontaneous motility of and increases concentration of cyclic AMP (cAMP) in isolated pregnant rat uterus.{47091} Formulations containing ritodrine were previously used to stop premature labor.  

     

    Brand:
    Cayman
    SKU:26084 - 250 mg

    Available on backorder

  • Ritodrine is an agonist of β2-adrenergic receptors (β2-ARs).{47089} It induces relaxation of isolated pig detrusor muscle when used at concentrations ranging from 0.001 to 1 μM. Ritodrine (30 μg/ml) reduces electrically-induced isometric tension in myometrial strips isolated from rabbits on day 25 of pregnancy.{47090} It also suppresses spontaneous motility of and increases concentration of cyclic AMP (cAMP) in isolated pregnant rat uterus.{47091} Formulations containing ritodrine were previously used to stop premature labor.  

     

    Brand:
    Cayman
    SKU:26084 - 5 g

    Available on backorder

  • Ritodrine is an agonist of β2-adrenergic receptors (β2-ARs).{47089} It induces relaxation of isolated pig detrusor muscle when used at concentrations ranging from 0.001 to 1 μM. Ritodrine (30 μg/ml) reduces electrically-induced isometric tension in myometrial strips isolated from rabbits on day 25 of pregnancy.{47090} It also suppresses spontaneous motility of and increases concentration of cyclic AMP (cAMP) in isolated pregnant rat uterus.{47091} Formulations containing ritodrine were previously used to stop premature labor.  

     

    Brand:
    Cayman
    SKU:26084 - 500 mg

    Available on backorder

  • Ritonavir is an HIV protease inhibitor.{24746} It inhibits recombinant HIV-1 protease by 79% when used at a concentration of 0.5 nM. It inhibits HIV-13B-induced cell death in MT-4 human T cell leukemia cells (EC50 = 25 nM) as well as cell death induced by HIV-1LAI, HIV-2ROD, and HIV-2EHO in human MT-2 cells (IC50s = 0.045, 0.13, and 0.24 μM, respectively).{24746,26076} Ritonavir also inhibits the cytochrome P450 (CYP) isoform CYP3A (IC50 = 0.14 μM).{24198} It inhibits CYP-mediated oxidative metabolism of the HIV protease inhibitors saquinavir (Item No. 9001893), indinavir (Item No. 15150), nelfinavir (Item No. 15144), and amprenavir (Item No. 15369) in rat and human liver microsomes in a concentration-dependent manner.{42447} Ritonavir (10 mg/kg) also prevents decreases in plasma levels of these four compounds in rats. Formulations containing ritonavir have been used in the treatment of HIV-1 infection.  

     

    Brand:
    Cayman
    SKU:-
  • Ritonavir is an HIV protease inhibitor.{24746} It inhibits recombinant HIV-1 protease by 79% when used at a concentration of 0.5 nM. It inhibits HIV-13B-induced cell death in MT-4 human T cell leukemia cells (EC50 = 25 nM) as well as cell death induced by HIV-1LAI, HIV-2ROD, and HIV-2EHO in human MT-2 cells (IC50s = 0.045, 0.13, and 0.24 μM, respectively).{24746,26076} Ritonavir also inhibits the cytochrome P450 (CYP) isoform CYP3A (IC50 = 0.14 μM).{24198} It inhibits CYP-mediated oxidative metabolism of the HIV protease inhibitors saquinavir (Item No. 9001893), indinavir (Item No. 15150), nelfinavir (Item No. 15144), and amprenavir (Item No. 15369) in rat and human liver microsomes in a concentration-dependent manner.{42447} Ritonavir (10 mg/kg) also prevents decreases in plasma levels of these four compounds in rats. Formulations containing ritonavir have been used in the treatment of HIV-1 infection.  

     

    Brand:
    Cayman
    SKU:-
  • Ritonavir is an HIV protease inhibitor.{24746} It inhibits recombinant HIV-1 protease by 79% when used at a concentration of 0.5 nM. It inhibits HIV-13B-induced cell death in MT-4 human T cell leukemia cells (EC50 = 25 nM) as well as cell death induced by HIV-1LAI, HIV-2ROD, and HIV-2EHO in human MT-2 cells (IC50s = 0.045, 0.13, and 0.24 μM, respectively).{24746,26076} Ritonavir also inhibits the cytochrome P450 (CYP) isoform CYP3A (IC50 = 0.14 μM).{24198} It inhibits CYP-mediated oxidative metabolism of the HIV protease inhibitors saquinavir (Item No. 9001893), indinavir (Item No. 15150), nelfinavir (Item No. 15144), and amprenavir (Item No. 15369) in rat and human liver microsomes in a concentration-dependent manner.{42447} Ritonavir (10 mg/kg) also prevents decreases in plasma levels of these four compounds in rats. Formulations containing ritonavir have been used in the treatment of HIV-1 infection.  

     

    Brand:
    Cayman
    SKU:-
  • Ritonavir-d6 is intended for use as an internal standard for the quantification of ritonavir (Item No. 13872) by GC- or LC-MS. Ritonavir is an HIV protease inhibitor.{24746} It inhibits recombinant HIV-1 protease by 79% when used at a concentration of 0.5 nM. It inhibits HIV-13B-induced cell death in MT-4 human T cell leukemia cells (EC50 = 25 nM) as well as cell death induced by HIV-1LAI, HIV-2ROD, and HIV-2EHO in human MT-2 cells (IC50s = 0.045, 0.13, and 0.24 μM, respectively).{24746,26076} Ritonavir also inhibits the cytochrome P450 (CYP) isoform CYP3A (IC50 = 0.14 μM).{24198} It inhibits CYP-mediated oxidative metabolism of the HIV protease inhibitors saquinavir (Item No. 9001893), indinavir (Item No. 15150), nelfinavir (Item No. 15144), and amprenavir (Item No. 15369) in rat and human liver microsomes in a concentration-dependent manner.{42447} Ritonavir (10 mg/kg) also prevents decreases in plasma levels of these four compounds in rats. Formulations containing ritonavir have been used in the treatment of HIV-1 infection.  

     

    Brand:
    Cayman
    SKU:25462 - 1 mg

    Available on backorder

  • Ritonavir-d6 is intended for use as an internal standard for the quantification of ritonavir (Item No. 13872) by GC- or LC-MS. Ritonavir is an HIV protease inhibitor.{24746} It inhibits recombinant HIV-1 protease by 79% when used at a concentration of 0.5 nM. It inhibits HIV-13B-induced cell death in MT-4 human T cell leukemia cells (EC50 = 25 nM) as well as cell death induced by HIV-1LAI, HIV-2ROD, and HIV-2EHO in human MT-2 cells (IC50s = 0.045, 0.13, and 0.24 μM, respectively).{24746,26076} Ritonavir also inhibits the cytochrome P450 (CYP) isoform CYP3A (IC50 = 0.14 μM).{24198} It inhibits CYP-mediated oxidative metabolism of the HIV protease inhibitors saquinavir (Item No. 9001893), indinavir (Item No. 15150), nelfinavir (Item No. 15144), and amprenavir (Item No. 15369) in rat and human liver microsomes in a concentration-dependent manner.{42447} Ritonavir (10 mg/kg) also prevents decreases in plasma levels of these four compounds in rats. Formulations containing ritonavir have been used in the treatment of HIV-1 infection.  

     

    Brand:
    Cayman
    SKU:25462 - 500 µg

    Available on backorder

  • Rivaroxaban is an orally active, direct inhibitor of Factor Xa (Ki = 0.4 nM), which is a crucial component of the intrinsic and extrinsic pathways of the blood coagulation cascade.{25094} It demonstrates >10,000-fold greater selectivity for Factor Xa compared to other related serine proteases.{25094} In various animal arterial and venous thrombosis models, rivaroxaban is reported to inhibit thrombin formation without prolonging bleeding time and has been approved for clinical use as an anticoagulant in the prevention of stroke and the treatment of venous thromboembolisms.{26130,26131}  

     

    Brand:
    Cayman
    SKU:-
  • Rivaroxaban is an orally active, direct inhibitor of Factor Xa (Ki = 0.4 nM), which is a crucial component of the intrinsic and extrinsic pathways of the blood coagulation cascade.{25094} It demonstrates >10,000-fold greater selectivity for Factor Xa compared to other related serine proteases.{25094} In various animal arterial and venous thrombosis models, rivaroxaban is reported to inhibit thrombin formation without prolonging bleeding time and has been approved for clinical use as an anticoagulant in the prevention of stroke and the treatment of venous thromboembolisms.{26130,26131}  

     

    Brand:
    Cayman
    SKU:-
  • Rivaroxaban is an orally active, direct inhibitor of Factor Xa (Ki = 0.4 nM), which is a crucial component of the intrinsic and extrinsic pathways of the blood coagulation cascade.{25094} It demonstrates >10,000-fold greater selectivity for Factor Xa compared to other related serine proteases.{25094} In various animal arterial and venous thrombosis models, rivaroxaban is reported to inhibit thrombin formation without prolonging bleeding time and has been approved for clinical use as an anticoagulant in the prevention of stroke and the treatment of venous thromboembolisms.{26130,26131}  

     

    Brand:
    Cayman
    SKU:-
  • Rivaroxaban is an orally active, direct inhibitor of Factor Xa (Ki = 0.4 nM), which is a crucial component of the intrinsic and extrinsic pathways of the blood coagulation cascade.{25094} It demonstrates >10,000-fold greater selectivity for Factor Xa compared to other related serine proteases.{25094} In various animal arterial and venous thrombosis models, rivaroxaban is reported to inhibit thrombin formation without prolonging bleeding time and has been approved for clinical use as an anticoagulant in the prevention of stroke and the treatment of venous thromboembolisms.{26130,26131}  

     

    Brand:
    Cayman
    SKU:-
  • Rivaroxaban-d4 is intended for use as an internal standard for the quantification of rivaroxaban (Item No. 16043) by GC- or LC-MS. Rivaroxaban is an orally active, direct inhibitor of Factor Xa (Ki = 0.4 nM), which is a crucial component of the intrinsic and extrinsic pathways of the blood coagulation cascade.{25094} It demonstrates >10,000-fold greater selectivity for Factor Xa compared to other related serine proteases. In various animal arterial and venous thrombosis models, rivaroxaban is reported to inhibit thrombin formation without prolonging bleeding time. Formulations containing rivaroxaban have been used as an anticoagulant in the prevention of stroke and the treatment of venous thromboembolisms.{26130,26131}  

     

    Brand:
    Cayman
    SKU:22563 -

    Out of stock

  • Rivaroxaban-d4 is intended for use as an internal standard for the quantification of rivaroxaban (Item No. 16043) by GC- or LC-MS. Rivaroxaban is an orally active, direct inhibitor of Factor Xa (Ki = 0.4 nM), which is a crucial component of the intrinsic and extrinsic pathways of the blood coagulation cascade.{25094} It demonstrates >10,000-fold greater selectivity for Factor Xa compared to other related serine proteases. In various animal arterial and venous thrombosis models, rivaroxaban is reported to inhibit thrombin formation without prolonging bleeding time. Formulations containing rivaroxaban have been used as an anticoagulant in the prevention of stroke and the treatment of venous thromboembolisms.{26130,26131}  

     

    Brand:
    Cayman
    SKU:22563 -

    Out of stock

  • Rivastigmine is a cholinesterase (ChE) inhibitor that inhibits butyryl ChE (BChE) and acetyl ChE (AChE; IC50s = 0.037 and 4.15 μM, respectively).{24084} It increases levels of secreted amyloid precursor protein (sAPP) and decreases levels of soluble amyloid-β (1-40) and various N-terminal cleavage products in primary embryonic rat neurons undergoing degeneration when used at concentrations of 5 and 10 μM.{36871}. In a rat model of Alzheimer’s disease induced by aluminum chloride (AlCl3), rivastigmine (1 mg/kg per day) inhibits formation of amyloid plaques in brain sections and increases in AChE, IL-1β, and β-secretase 1 (BACE1) mRNA expression in the cerebral cortex.{36872} It inhibits AlCl3-induced increases in escape latency time in the Morris water maze in a rat model of Alzheimer’s disease when administered at a dose of 1 mg/kg. Rivastigmine (2 mg/kg) also reverses decreases in time spent in the open arms of an elevated plus maze, exploration time of a novel object in a novel object recognition test, and sucrose intake in a rat model of chronic mild stress.{36873} Formulations containing rivastigmine have been used in the treatment of dementia associated with Alzheimer’s disease and Parkinson’s disease.  

     

    Brand:
    Cayman
    SKU:-
  • Rivastigmine is a cholinesterase (ChE) inhibitor that inhibits butyryl ChE (BChE) and acetyl ChE (AChE; IC50s = 0.037 and 4.15 μM, respectively).{24084} It increases levels of secreted amyloid precursor protein (sAPP) and decreases levels of soluble amyloid-β (1-40) and various N-terminal cleavage products in primary embryonic rat neurons undergoing degeneration when used at concentrations of 5 and 10 μM.{36871}. In a rat model of Alzheimer’s disease induced by aluminum chloride (AlCl3), rivastigmine (1 mg/kg per day) inhibits formation of amyloid plaques in brain sections and increases in AChE, IL-1β, and β-secretase 1 (BACE1) mRNA expression in the cerebral cortex.{36872} It inhibits AlCl3-induced increases in escape latency time in the Morris water maze in a rat model of Alzheimer’s disease when administered at a dose of 1 mg/kg. Rivastigmine (2 mg/kg) also reverses decreases in time spent in the open arms of an elevated plus maze, exploration time of a novel object in a novel object recognition test, and sucrose intake in a rat model of chronic mild stress.{36873} Formulations containing rivastigmine have been used in the treatment of dementia associated with Alzheimer’s disease and Parkinson’s disease.  

     

    Brand:
    Cayman
    SKU:-
  • Rivastigmine is a cholinesterase (ChE) inhibitor that inhibits butyryl ChE (BChE) and acetyl ChE (AChE; IC50s = 0.037 and 4.15 μM, respectively).{24084} It increases levels of secreted amyloid precursor protein (sAPP) and decreases levels of soluble amyloid-β (1-40) and various N-terminal cleavage products in primary embryonic rat neurons undergoing degeneration when used at concentrations of 5 and 10 μM.{36871}. In a rat model of Alzheimer’s disease induced by aluminum chloride (AlCl3), rivastigmine (1 mg/kg per day) inhibits formation of amyloid plaques in brain sections and increases in AChE, IL-1β, and β-secretase 1 (BACE1) mRNA expression in the cerebral cortex.{36872} It inhibits AlCl3-induced increases in escape latency time in the Morris water maze in a rat model of Alzheimer’s disease when administered at a dose of 1 mg/kg. Rivastigmine (2 mg/kg) also reverses decreases in time spent in the open arms of an elevated plus maze, exploration time of a novel object in a novel object recognition test, and sucrose intake in a rat model of chronic mild stress.{36873} Formulations containing rivastigmine have been used in the treatment of dementia associated with Alzheimer’s disease and Parkinson’s disease.  

     

    Brand:
    Cayman
    SKU:-
  • Rivastigmine is a cholinesterase (ChE) inhibitor that inhibits butyryl ChE (BChE) and acetyl ChE (AChE; IC50s = 0.037 and 4.15 μM, respectively).{24084} It increases levels of secreted amyloid precursor protein (sAPP) and decreases levels of soluble amyloid-β (1-40) and various N-terminal cleavage products in primary embryonic rat neurons undergoing degeneration when used at concentrations of 5 and 10 μM.{36871}. In a rat model of Alzheimer’s disease induced by aluminum chloride (AlCl3), rivastigmine (1 mg/kg per day) inhibits formation of amyloid plaques in brain sections and increases in AChE, IL-1β, and β-secretase 1 (BACE1) mRNA expression in the cerebral cortex.{36872} It inhibits AlCl3-induced increases in escape latency time in the Morris water maze in a rat model of Alzheimer’s disease when administered at a dose of 1 mg/kg. Rivastigmine (2 mg/kg) also reverses decreases in time spent in the open arms of an elevated plus maze, exploration time of a novel object in a novel object recognition test, and sucrose intake in a rat model of chronic mild stress.{36873} Formulations containing rivastigmine have been used in the treatment of dementia associated with Alzheimer’s disease and Parkinson’s disease.  

     

    Brand:
    Cayman
    SKU:-
  • Rivastigmine-d6 is intended for use as an internal standard for the quantification of rivastigmine (Item No. 14270) by GC- or LC-MS. Rivastigmine is a cholinesterase (ChE) inhibitor that inhibits butyrl ChE (BChE) and acetyl ChE (AChE; IC50s = 0.037 and 4.15 μM, respectively).{24084} It increases levels of secreted amyloid precursor protein (sAPP) and decreases levels of soluble amyloid-β (1-40) and various N-terminal cleavage products in primary embryonic rat neurons undergoing degeneration when used at concentrations of 5 and 10 μM.{36871} In a rat model of Alzheimer’s disease induced by aluminum chloride (AlCl3), rivastigmine (1 mg/kg per day) inhibits formation of amyloid plaques in brain sections and increases in AChE, IL-1β, and β-secretase 1 (BACE1) mRNA expression in the cerebral cortex.{36872} It inhibits AlCl3-induced increases in escape latency time in the Morris water maze in a rat model of Alzheimer’s disease when administered at a dose of 1 mg/kg. Rivastigmine (2 mg/kg) also reverses decreases in time spent in the open arms of an elevated plus maze, exploration time of a novel object in a novel object recognition test, and sucrose intake in a rat model of chronic mild stress.{36873} Formulations containing rivastigmine have been used in the treatment of dementia associated with Alzheimer’s disease and Parkinson’s disease.  

     

    Brand:
    Cayman
    SKU:25633 - 1 mg

    Available on backorder

  • Rivastigmine-d6 is intended for use as an internal standard for the quantification of rivastigmine (Item No. 14270) by GC- or LC-MS. Rivastigmine is a cholinesterase (ChE) inhibitor that inhibits butyrl ChE (BChE) and acetyl ChE (AChE; IC50s = 0.037 and 4.15 μM, respectively).{24084} It increases levels of secreted amyloid precursor protein (sAPP) and decreases levels of soluble amyloid-β (1-40) and various N-terminal cleavage products in primary embryonic rat neurons undergoing degeneration when used at concentrations of 5 and 10 μM.{36871} In a rat model of Alzheimer’s disease induced by aluminum chloride (AlCl3), rivastigmine (1 mg/kg per day) inhibits formation of amyloid plaques in brain sections and increases in AChE, IL-1β, and β-secretase 1 (BACE1) mRNA expression in the cerebral cortex.{36872} It inhibits AlCl3-induced increases in escape latency time in the Morris water maze in a rat model of Alzheimer’s disease when administered at a dose of 1 mg/kg. Rivastigmine (2 mg/kg) also reverses decreases in time spent in the open arms of an elevated plus maze, exploration time of a novel object in a novel object recognition test, and sucrose intake in a rat model of chronic mild stress.{36873} Formulations containing rivastigmine have been used in the treatment of dementia associated with Alzheimer’s disease and Parkinson’s disease.  

     

    Brand:
    Cayman
    SKU:25633 - 500 µg

    Available on backorder

  • Prostaglandin E2 activates four distinct G protein-coupled receptors, EP1-4. Rivenprost is a potent and selective agonist for the EP4 receptor (Ki = 0.7, 56, 620, and >10,000 nM for EP4, EP3, EP2, and EP1, respectively).{10581} It has been used to promote EP4-mediated bone formation, prevent bone loss related to osteoporosis, drive osteoblast differentiation, and stabilize bone implants.{10581,18823,18825,18824,18827} Rivenprost has also been used to support wound healing.{18826}  

     

    Brand:
    Cayman
    SKU:-
  • Prostaglandin E2 activates four distinct G protein-coupled receptors, EP1-4. Rivenprost is a potent and selective agonist for the EP4 receptor (Ki = 0.7, 56, 620, and >10,000 nM for EP4, EP3, EP2, and EP1, respectively).{10581} It has been used to promote EP4-mediated bone formation, prevent bone loss related to osteoporosis, drive osteoblast differentiation, and stabilize bone implants.{10581,18823,18825,18824,18827} Rivenprost has also been used to support wound healing.{18826}  

     

    Brand:
    Cayman
    SKU:-
  • Prostaglandin E2 activates four distinct G protein-coupled receptors, EP1-4. Rivenprost is a potent and selective agonist for the EP4 receptor (Ki = 0.7, 56, 620, and >10,000 nM for EP4, EP3, EP2, and EP1, respectively).{10581} It has been used to promote EP4-mediated bone formation, prevent bone loss related to osteoporosis, drive osteoblast differentiation, and stabilize bone implants.{10581,18823,18825,18824,18827} Rivenprost has also been used to support wound healing.{18826}  

     

    Brand:
    Cayman
    SKU:-
  • Rizatriptan is an orally bioavailable agonist at the serotonin (5-HT) receptor subtypes, 5-HT1B and 5-HT1D, with Ki values of 10.1 and 4.3 nM, respectively.{34530} It is less selective for the 5-HT1A receptor subtype (Ki = 140 nM). Rizatriptan has vasoconstrictive properties, which are more potent in isolated cranial arteries than coronary arteries.{34529} Formulations containing rizatriptan are used to treat patients with migraine headaches.  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Rizatriptan is an orally bioavailable agonist at the serotonin (5-HT) receptor subtypes, 5-HT1B and 5-HT1D, with Ki values of 10.1 and 4.3 nM, respectively.{34530} It is less selective for the 5-HT1A receptor subtype (Ki = 140 nM). Rizatriptan has vasoconstrictive properties, which are more potent in isolated cranial arteries than coronary arteries.{34529} Formulations containing rizatriptan are used to treat patients with migraine headaches.  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Rizatriptan is an orally bioavailable agonist at the serotonin (5-HT) receptor subtypes, 5-HT1B and 5-HT1D, with Ki values of 10.1 and 4.3 nM, respectively.{34530} It is less selective for the 5-HT1A receptor subtype (Ki = 140 nM). Rizatriptan has vasoconstrictive properties, which are more potent in isolated cranial arteries than coronary arteries.{34529} Formulations containing rizatriptan are used to treat patients with migraine headaches.  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Rizatriptan is an orally bioavailable agonist at the serotonin (5-HT) receptor subtypes, 5-HT1B and 5-HT1D, with Ki values of 10.1 and 4.3 nM, respectively.{34530} It is less selective for the 5-HT1A receptor subtype (Ki = 140 nM). Rizatriptan has vasoconstrictive properties, which are more potent in isolated cranial arteries than coronary arteries.{34529} Formulations containing rizatriptan are used to treat patients with migraine headaches.  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • RJR 2429 is a nicotinic acetylcholine receptor (AChR) agonist.{49443} It is selective for α4β2 or α7 subunit-containing nicotinic AChRs (Kis = 0.7 and 10.9 nM in isolated rat cortex and isolated rat hippocampus, respectively) over α1βɣδ subunit-containing nicotinic AChRs (EC50 = 1,000 nM in PC12 cells). RJR 2429 induces dopamine release from isolated rat striatal synaptosomes (EC50 = 2.4 nM) and increases nicotine-induced elevations in epinephrine and norepinephrine levels in isolated rat adrenal gland when used at a concentration of 100 µM.{49444},{49446} It inhibits nicotine-induced ion flux in isolated rat thalamic synaptosomes (IC50 = 154 nM).{49444}  

     

    Brand:
    Cayman
    SKU:29745 - 10 mg

    Available on backorder

  • RJR 2429 is a nicotinic acetylcholine receptor (AChR) agonist.{49443} It is selective for α4β2 or α7 subunit-containing nicotinic AChRs (Kis = 0.7 and 10.9 nM in isolated rat cortex and isolated rat hippocampus, respectively) over α1βɣδ subunit-containing nicotinic AChRs (EC50 = 1,000 nM in PC12 cells). RJR 2429 induces dopamine release from isolated rat striatal synaptosomes (EC50 = 2.4 nM) and increases nicotine-induced elevations in epinephrine and norepinephrine levels in isolated rat adrenal gland when used at a concentration of 100 µM.{49444},{49446} It inhibits nicotine-induced ion flux in isolated rat thalamic synaptosomes (IC50 = 154 nM).{49444}  

     

    Brand:
    Cayman
    SKU:29745 - 25 mg

    Available on backorder

  • RJR 2429 is a nicotinic acetylcholine receptor (AChR) agonist.{49443} It is selective for α4β2 or α7 subunit-containing nicotinic AChRs (Kis = 0.7 and 10.9 nM in isolated rat cortex and isolated rat hippocampus, respectively) over α1βɣδ subunit-containing nicotinic AChRs (EC50 = 1,000 nM in PC12 cells). RJR 2429 induces dopamine release from isolated rat striatal synaptosomes (EC50 = 2.4 nM) and increases nicotine-induced elevations in epinephrine and norepinephrine levels in isolated rat adrenal gland when used at a concentration of 100 µM.{49444},{49446} It inhibits nicotine-induced ion flux in isolated rat thalamic synaptosomes (IC50 = 154 nM).{49444}  

     

    Brand:
    Cayman
    SKU:29745 - 5 mg

    Available on backorder

  • RK-20448 is an ATP-competitive inhibitor of Lck, Src, KDR/VEGF2R, and Tie-2 (IC50s = 0.24, 1.19, 10.74, and 5.85 µM, respectively).{24190} It also inhibits BLK, Csk, Fyn, and Lyn (IC50s = 0.37, 4.27, 2.03, and 0.43 µM, respectively). RK-20448 is the cis isomer of A-419259 (Item No. 18168).  

     

    Brand:
    Cayman
    SKU:25606 - 1 mg

    Available on backorder

  • RK-20448 is an ATP-competitive inhibitor of Lck, Src, KDR/VEGF2R, and Tie-2 (IC50s = 0.24, 1.19, 10.74, and 5.85 µM, respectively).{24190} It also inhibits BLK, Csk, Fyn, and Lyn (IC50s = 0.37, 4.27, 2.03, and 0.43 µM, respectively). RK-20448 is the cis isomer of A-419259 (Item No. 18168).  

     

    Brand:
    Cayman
    SKU:25606 - 10 mg

    Available on backorder

  • RK-20448 is an ATP-competitive inhibitor of Lck, Src, KDR/VEGF2R, and Tie-2 (IC50s = 0.24, 1.19, 10.74, and 5.85 µM, respectively).{24190} It also inhibits BLK, Csk, Fyn, and Lyn (IC50s = 0.37, 4.27, 2.03, and 0.43 µM, respectively). RK-20448 is the cis isomer of A-419259 (Item No. 18168).  

     

    Brand:
    Cayman
    SKU:25606 - 5 mg

    Available on backorder

  • RK-20448 is an ATP-competitive inhibitor of Lck, Src, KDR/VEGF2R, and Tie-2 (IC50s = 0.24, 1.19, 10.74, and 5.85 µM, respectively).{24190} It also inhibits BLK, Csk, Fyn, and Lyn (IC50s = 0.37, 4.27, 2.03, and 0.43 µM, respectively). RK-20448 is the cis isomer of A-419259 (Item No. 18168).  

     

    Brand:
    Cayman
    SKU:25606 - 500 µg

    Available on backorder

  • RK-287107 is an inhibitor of the tankyrases TNKS1 and TNKS2 (IC50s = 0.014 and 0.010 µM, respectively).{60079} It is selective for TNKS1 and TNKS2 over poly(ADP-ribose) polymerase 1 (PARP1), PARP2, and PARP10 (IC50s = >20, 2.7, and 19.8 µM, respectively). RK-287107 inhibits Wnt-dependent signaling with an IC50 value of 0.077 µM in a reporter assay. It increases accumulation of Axin2, indicating inhibition of TNKS-mediated auto-PARsylation, in COLO 320DM colorectal cancer cells when used at a concentration of 0.1 µM. RK-287107 also inhibits cell growth in the same model (GI50 = 0.45 µM). It reduces tumor growth in a COLO 320DM mouse xenograft model when administered at a dose of 150 mg/kg twice per day.  

     

    Brand:
    Cayman
    SKU:30998 - 1 mg

    Available on backorder

  • RK-287107 is an inhibitor of the tankyrases TNKS1 and TNKS2 (IC50s = 0.014 and 0.010 µM, respectively).{60079} It is selective for TNKS1 and TNKS2 over poly(ADP-ribose) polymerase 1 (PARP1), PARP2, and PARP10 (IC50s = >20, 2.7, and 19.8 µM, respectively). RK-287107 inhibits Wnt-dependent signaling with an IC50 value of 0.077 µM in a reporter assay. It increases accumulation of Axin2, indicating inhibition of TNKS-mediated auto-PARsylation, in COLO 320DM colorectal cancer cells when used at a concentration of 0.1 µM. RK-287107 also inhibits cell growth in the same model (GI50 = 0.45 µM). It reduces tumor growth in a COLO 320DM mouse xenograft model when administered at a dose of 150 mg/kg twice per day.  

     

    Brand:
    Cayman
    SKU:30998 - 10 mg

    Available on backorder

  • RK-287107 is an inhibitor of the tankyrases TNKS1 and TNKS2 (IC50s = 0.014 and 0.010 µM, respectively).{60079} It is selective for TNKS1 and TNKS2 over poly(ADP-ribose) polymerase 1 (PARP1), PARP2, and PARP10 (IC50s = >20, 2.7, and 19.8 µM, respectively). RK-287107 inhibits Wnt-dependent signaling with an IC50 value of 0.077 µM in a reporter assay. It increases accumulation of Axin2, indicating inhibition of TNKS-mediated auto-PARsylation, in COLO 320DM colorectal cancer cells when used at a concentration of 0.1 µM. RK-287107 also inhibits cell growth in the same model (GI50 = 0.45 µM). It reduces tumor growth in a COLO 320DM mouse xenograft model when administered at a dose of 150 mg/kg twice per day.  

     

    Brand:
    Cayman
    SKU:30998 - 5 mg

    Available on backorder

  • Protein tyrosine phosphatases (PTPs) remove phosphate from tyrosine residues of cellular proteins. Reversible phosphorylation catalyzed by the coordinated actions of protein tyrosine kinases and phosphatases is key to the regulation of the signaling events that control cell growth and proliferation, differentiation, and survival or apoptosis, as well as adhesion and motility. RK-682, a bioactive compound originally isolated from the fermentation of Streptomyces sp. 88-682, is an inhibitor of the PTPs.{31099} It inhibits the phosphorylation of CD45 and VHR with IC50 values of 54 and 2 µM, respectively, and arrests cell cycle progress at the G1/S transition.{31099} It is also reported to inhibit heparanase (IC50 = 17 µM), an endo-β-D-glucuronidase involved in tumor cell invasion and angiogenesis.{31100} RK-682 (calcium salt) is a less soluble version of the free acid.{31101}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Protein tyrosine phosphatases (PTPs) remove phosphate from tyrosine residues of cellular proteins. Reversible phosphorylation catalyzed by the coordinated actions of protein tyrosine kinases and phosphatases is key to the regulation of the signaling events that control cell growth and proliferation, differentiation, and survival or apoptosis, as well as adhesion and motility. RK-682, a bioactive compound originally isolated from the fermentation of Streptomyces sp. 88-682, is an inhibitor of the PTPs.{31099} It inhibits the phosphorylation of CD45 and VHR with IC50 values of 54 and 2 µM, respectively, and arrests cell cycle progress at the G1/S transition.{31099} It is also reported to inhibit heparanase (IC50 = 17 µM), an endo-β-D-glucuronidase involved in tumor cell invasion and angiogenesis.{31100} RK-682 (calcium salt) is a less soluble version of the free acid.{31101}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • RKI-1313 is an inhibitor of Rho-associated kinase I (ROCK-I) and II (IC50s = 34 and 8 µM, respectively).{27949} It has been used as a negative control for the ROCK inhibitor RKI-1447 (Item No. 16278).  

     

    Brand:
    Cayman
    SKU:22933 - 1 mg

    Available on backorder

  • RKI-1313 is an inhibitor of Rho-associated kinase I (ROCK-I) and II (IC50s = 34 and 8 µM, respectively).{27949} It has been used as a negative control for the ROCK inhibitor RKI-1447 (Item No. 16278).  

     

    Brand:
    Cayman
    SKU:22933 - 10 mg

    Available on backorder

  • RKI-1313 is an inhibitor of Rho-associated kinase I (ROCK-I) and II (IC50s = 34 and 8 µM, respectively).{27949} It has been used as a negative control for the ROCK inhibitor RKI-1447 (Item No. 16278).  

     

    Brand:
    Cayman
    SKU:22933 - 5 mg

    Available on backorder

  • RKI-1447 is an inhibitor of the Rho-associated kinases ROCK-I and II (IC50s = 14.5 and 6.2 nM, respectively) that functions by binding to the ATP binding site of the kinase.{27949} In cancer cells, RKI-1447 at a concentration of 100 nM has been found to suppress the activation of ROCK substrates myosin light chain (MLC)-2 and the MLC phosphatase PP1 regulatory subunit MYPT1 without effect on the phosphorylation of Akt, MEK, or S6 kinase.{27949} Furthermore, it can prevent ROCK-mediated migration, invasion, and anchorage-independent growth of MDA-MB-231 breast cancer cells (IC50 = 709 nM).{27949}  

     

    Brand:
    Cayman
    SKU:-
  • RKI-1447 is an inhibitor of the Rho-associated kinases ROCK-I and II (IC50s = 14.5 and 6.2 nM, respectively) that functions by binding to the ATP binding site of the kinase.{27949} In cancer cells, RKI-1447 at a concentration of 100 nM has been found to suppress the activation of ROCK substrates myosin light chain (MLC)-2 and the MLC phosphatase PP1 regulatory subunit MYPT1 without effect on the phosphorylation of Akt, MEK, or S6 kinase.{27949} Furthermore, it can prevent ROCK-mediated migration, invasion, and anchorage-independent growth of MDA-MB-231 breast cancer cells (IC50 = 709 nM).{27949}  

     

    Brand:
    Cayman
    SKU:-
  • RKI-1447 is an inhibitor of the Rho-associated kinases ROCK-I and II (IC50s = 14.5 and 6.2 nM, respectively) that functions by binding to the ATP binding site of the kinase.{27949} In cancer cells, RKI-1447 at a concentration of 100 nM has been found to suppress the activation of ROCK substrates myosin light chain (MLC)-2 and the MLC phosphatase PP1 regulatory subunit MYPT1 without effect on the phosphorylation of Akt, MEK, or S6 kinase.{27949} Furthermore, it can prevent ROCK-mediated migration, invasion, and anchorage-independent growth of MDA-MB-231 breast cancer cells (IC50 = 709 nM).{27949}  

     

    Brand:
    Cayman
    SKU:-
  • RMC-4550 is an inhibitor of Src homology region 2 domain-containing phosphatase 2 (SHP-2; IC50 = 1.55 nM).{58010} It is selective for SHP-2 over a panel of 14 additional protein phosphatases and a panel of 468 protein kinases at 10 µM. It inhibits tumor ERK phosphorylation in a KYSE-520 human esophageal cancer xenograft model in a dose-dependent manner.  

     

    Brand:
    Cayman
    SKU:31011 - 1 mg

    Available on backorder

  • RMC-4550 is an inhibitor of Src homology region 2 domain-containing phosphatase 2 (SHP-2; IC50 = 1.55 nM).{58010} It is selective for SHP-2 over a panel of 14 additional protein phosphatases and a panel of 468 protein kinases at 10 µM. It inhibits tumor ERK phosphorylation in a KYSE-520 human esophageal cancer xenograft model in a dose-dependent manner.  

     

    Brand:
    Cayman
    SKU:31011 - 10 mg

    Available on backorder

  • RMC-4550 is an inhibitor of Src homology region 2 domain-containing phosphatase 2 (SHP-2; IC50 = 1.55 nM).{58010} It is selective for SHP-2 over a panel of 14 additional protein phosphatases and a panel of 468 protein kinases at 10 µM. It inhibits tumor ERK phosphorylation in a KYSE-520 human esophageal cancer xenograft model in a dose-dependent manner.  

     

    Brand:
    Cayman
    SKU:31011 - 25 mg

    Available on backorder

  • RMC-4550 is an inhibitor of Src homology region 2 domain-containing phosphatase 2 (SHP-2; IC50 = 1.55 nM).{58010} It is selective for SHP-2 over a panel of 14 additional protein phosphatases and a panel of 468 protein kinases at 10 µM. It inhibits tumor ERK phosphorylation in a KYSE-520 human esophageal cancer xenograft model in a dose-dependent manner.  

     

    Brand:
    Cayman
    SKU:31011 - 5 mg

    Available on backorder

  • Lysine-specific demethylase 1 (LSD1) belongs to the family of flavin adenine dinucleotide (FAD)-dependent amine oxidases that include monoamine oxidases (MAOs).{12422} RN-1 is a potent, irreversible inhibitor of LSD1 (IC50 = 70 nM).{29862} It is much less effective against MAO-A and MAO-B (IC50s = 0.51 and 2.8 µM, respectively).{29862} Following intraperitoneal administration, RN-1 penetrates the blood-brain barrier and distributes in mice to a brain/plasma exposure ratio of 88.9.{29862} It blocks long-term but not short-term memory in mice.{29862} RN-1 also induces cytotoxicity in ovarian cancer cell lines and induces fetal hemoglobin synthesis while reducing disease pathology in sickle cell mice.{29861,29860}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Lysine-specific demethylase 1 (LSD1) belongs to the family of flavin adenine dinucleotide (FAD)-dependent amine oxidases that include monoamine oxidases (MAOs).{12422} RN-1 is a potent, irreversible inhibitor of LSD1 (IC50 = 70 nM).{29862} It is much less effective against MAO-A and MAO-B (IC50s = 0.51 and 2.8 µM, respectively).{29862} Following intraperitoneal administration, RN-1 penetrates the blood-brain barrier and distributes in mice to a brain/plasma exposure ratio of 88.9.{29862} It blocks long-term but not short-term memory in mice.{29862} RN-1 also induces cytotoxicity in ovarian cancer cell lines and induces fetal hemoglobin synthesis while reducing disease pathology in sickle cell mice.{29861,29860}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Lysine-specific demethylase 1 (LSD1) belongs to the family of flavin adenine dinucleotide (FAD)-dependent amine oxidases that include monoamine oxidases (MAOs).{12422} RN-1 is a potent, irreversible inhibitor of LSD1 (IC50 = 70 nM).{29862} It is much less effective against MAO-A and MAO-B (IC50s = 0.51 and 2.8 µM, respectively).{29862} Following intraperitoneal administration, RN-1 penetrates the blood-brain barrier and distributes in mice to a brain/plasma exposure ratio of 88.9.{29862} It blocks long-term but not short-term memory in mice.{29862} RN-1 also induces cytotoxicity in ovarian cancer cell lines and induces fetal hemoglobin synthesis while reducing disease pathology in sickle cell mice.{29861,29860}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • RN-1734 is a transient receptor potential vanilloid 4 (TRPV4) antagonist, blocking calcium influx induced by the TRPV4 agonist 4α-phorbol 12,13-didecanoate (Item No. 20446) with IC50 values of 2.3, 5.9, and 3.2 µM for human, mouse, and rat TRPV4, respectively.{41579} It is selective for TRPV4 over TRPV1, TRPV3, and TRPM8 (IC50s = >100, >30, and >30 µM, respectively). RN-1734 (10 µM) reduces GSK1016790A-induced increases in glycine-activated current (IGly) from 34.5 to 0.97% in mouse hippocampal neurons in vitro.{41580} It blocks arteriolar dilation induced by GSK1016790A (Item No. 17289) and increases myogenic tone in rat cremaster arterioles ex vivo when used at a concentration of 30 µM.{41581} RN-1734 (1 mg/kg, i.p.) reduces edema and MAPK signaling induced by traumatic brain injury in rats.{41582} It also inhibits breakdown of the blood-retinal barrier in streptozotocin-induced diabetic rats when administered at a dose of 100 µM.{41583}  

     

    Brand:
    Cayman
    SKU:24205 - 10 mg

    Available on backorder

  • RN-1734 is a transient receptor potential vanilloid 4 (TRPV4) antagonist, blocking calcium influx induced by the TRPV4 agonist 4α-phorbol 12,13-didecanoate (Item No. 20446) with IC50 values of 2.3, 5.9, and 3.2 µM for human, mouse, and rat TRPV4, respectively.{41579} It is selective for TRPV4 over TRPV1, TRPV3, and TRPM8 (IC50s = >100, >30, and >30 µM, respectively). RN-1734 (10 µM) reduces GSK1016790A-induced increases in glycine-activated current (IGly) from 34.5 to 0.97% in mouse hippocampal neurons in vitro.{41580} It blocks arteriolar dilation induced by GSK1016790A (Item No. 17289) and increases myogenic tone in rat cremaster arterioles ex vivo when used at a concentration of 30 µM.{41581} RN-1734 (1 mg/kg, i.p.) reduces edema and MAPK signaling induced by traumatic brain injury in rats.{41582} It also inhibits breakdown of the blood-retinal barrier in streptozotocin-induced diabetic rats when administered at a dose of 100 µM.{41583}  

     

    Brand:
    Cayman
    SKU:24205 - 25 mg

    Available on backorder

  • RN-1734 is a transient receptor potential vanilloid 4 (TRPV4) antagonist, blocking calcium influx induced by the TRPV4 agonist 4α-phorbol 12,13-didecanoate (Item No. 20446) with IC50 values of 2.3, 5.9, and 3.2 µM for human, mouse, and rat TRPV4, respectively.{41579} It is selective for TRPV4 over TRPV1, TRPV3, and TRPM8 (IC50s = >100, >30, and >30 µM, respectively). RN-1734 (10 µM) reduces GSK1016790A-induced increases in glycine-activated current (IGly) from 34.5 to 0.97% in mouse hippocampal neurons in vitro.{41580} It blocks arteriolar dilation induced by GSK1016790A (Item No. 17289) and increases myogenic tone in rat cremaster arterioles ex vivo when used at a concentration of 30 µM.{41581} RN-1734 (1 mg/kg, i.p.) reduces edema and MAPK signaling induced by traumatic brain injury in rats.{41582} It also inhibits breakdown of the blood-retinal barrier in streptozotocin-induced diabetic rats when administered at a dose of 100 µM.{41583}  

     

    Brand:
    Cayman
    SKU:24205 - 5 mg

    Available on backorder

  • RN-18 is an inhibitor of HIV-1 viral infectivity factor (Vif), an HIV-1 regulatory protein that does not have cellular homologs.{40237} RN-18 inhibits Vif-mediated degradation of the DNA editing enzyme APOBEC3G with IC50 values of 10-30 µM in a high-throughput fluorescence screen. It inhibits viral replication of HIV-1 with IC50 values of 4.5 and 10 µM for nonpermissive CEM and H9 cells, respectively, and >100 µM for permissive cells.  

     

    Brand:
    Cayman
    SKU:23331 - 1 mg

    Available on backorder

  • RN-18 is an inhibitor of HIV-1 viral infectivity factor (Vif), an HIV-1 regulatory protein that does not have cellular homologs.{40237} RN-18 inhibits Vif-mediated degradation of the DNA editing enzyme APOBEC3G with IC50 values of 10-30 µM in a high-throughput fluorescence screen. It inhibits viral replication of HIV-1 with IC50 values of 4.5 and 10 µM for nonpermissive CEM and H9 cells, respectively, and >100 µM for permissive cells.  

     

    Brand:
    Cayman
    SKU:23331 - 10 mg

    Available on backorder

  • RN-18 is an inhibitor of HIV-1 viral infectivity factor (Vif), an HIV-1 regulatory protein that does not have cellular homologs.{40237} RN-18 inhibits Vif-mediated degradation of the DNA editing enzyme APOBEC3G with IC50 values of 10-30 µM in a high-throughput fluorescence screen. It inhibits viral replication of HIV-1 with IC50 values of 4.5 and 10 µM for nonpermissive CEM and H9 cells, respectively, and >100 µM for permissive cells.  

     

    Brand:
    Cayman
    SKU:23331 - 25 mg

    Available on backorder

  • RN-18 is an inhibitor of HIV-1 viral infectivity factor (Vif), an HIV-1 regulatory protein that does not have cellular homologs.{40237} RN-18 inhibits Vif-mediated degradation of the DNA editing enzyme APOBEC3G with IC50 values of 10-30 µM in a high-throughput fluorescence screen. It inhibits viral replication of HIV-1 with IC50 values of 4.5 and 10 µM for nonpermissive CEM and H9 cells, respectively, and >100 µM for permissive cells.  

     

    Brand:
    Cayman
    SKU:23331 - 5 mg

    Available on backorder

  • RN-486 is a Bruton’s tyrosine kinase inhibitor (Kd = 0.31 nM; IC50 = 4 nM) that displays a high degree of selectivity when tested against a panel of 369 kinases.{32326} It has been shown to block Fcε receptor cross-linking-induced degranulation in mast cells (IC50 = 2.9 nM), Fcγ receptor engagement-mediated TNF-α production in monocytes (IC50 = 7 nM), and B cell antigen receptor-induced expression of CD69 in B cells whole blood (IC50 = 21 nM).{32326} RN-486 is reported to produce anti-inflammatory and bone-protective effects in mouse collagen-induced arthritis and rat adjuvant-induced arthritis models.{32326}  

     

    Brand:
    Cayman
    SKU:20536 -

    Available on backorder

  • RN-486 is a Bruton’s tyrosine kinase inhibitor (Kd = 0.31 nM; IC50 = 4 nM) that displays a high degree of selectivity when tested against a panel of 369 kinases.{32326} It has been shown to block Fcε receptor cross-linking-induced degranulation in mast cells (IC50 = 2.9 nM), Fcγ receptor engagement-mediated TNF-α production in monocytes (IC50 = 7 nM), and B cell antigen receptor-induced expression of CD69 in B cells whole blood (IC50 = 21 nM).{32326} RN-486 is reported to produce anti-inflammatory and bone-protective effects in mouse collagen-induced arthritis and rat adjuvant-induced arthritis models.{32326}  

     

    Brand:
    Cayman
    SKU:20536 -

    Available on backorder

  • RN-486 is a Bruton’s tyrosine kinase inhibitor (Kd = 0.31 nM; IC50 = 4 nM) that displays a high degree of selectivity when tested against a panel of 369 kinases.{32326} It has been shown to block Fcε receptor cross-linking-induced degranulation in mast cells (IC50 = 2.9 nM), Fcγ receptor engagement-mediated TNF-α production in monocytes (IC50 = 7 nM), and B cell antigen receptor-induced expression of CD69 in B cells whole blood (IC50 = 21 nM).{32326} RN-486 is reported to produce anti-inflammatory and bone-protective effects in mouse collagen-induced arthritis and rat adjuvant-induced arthritis models.{32326}  

     

    Brand:
    Cayman
    SKU:20536 -

    Available on backorder

  • RN-9893 is an antagonist of transient receptor potential vanilloid 4 (TRPV4; IC50s = 0.42 and 0.66 μM, respectively, for the human and rat receptors).{52086} It is selective for TRPV4 over TRPV1, TRPV3, and TRPM8 (IC50s = 10, >30, and 30 μM, respectively). RN-9893 reduces rat TRPV4 activity induced by 4α-phorbol 12,13-didecanoate (4α-PDD; Item No. 20446) or hypotonicity (IC50s = 0.57 and 2.1 μM, respectively, in cell free assays).  

     

    Brand:
    Cayman
    SKU:29172 - 1 mg

    Available on backorder

  • RN-9893 is an antagonist of transient receptor potential vanilloid 4 (TRPV4; IC50s = 0.42 and 0.66 μM, respectively, for the human and rat receptors).{52086} It is selective for TRPV4 over TRPV1, TRPV3, and TRPM8 (IC50s = 10, >30, and 30 μM, respectively). RN-9893 reduces rat TRPV4 activity induced by 4α-phorbol 12,13-didecanoate (4α-PDD; Item No. 20446) or hypotonicity (IC50s = 0.57 and 2.1 μM, respectively, in cell free assays).  

     

    Brand:
    Cayman
    SKU:29172 - 5 mg

    Available on backorder

  • [Bertin Catalog No. G01033]  

     

    Brand:
    Cayman
    SKU:32823 - 100 µl

    Available on backorder

  • Host: Mouse • Applications: ELISA, IF, WB  

     

    Brand:
    Cayman
    SKU:32823- 100 µl

    Available on backorder

  • Host: Mouse • Applications: ELISA, IF, WB  

     

    Brand:
    Cayman
    SKU:32823- 100 µl
  • Glutamate, the major excitatory neurotransmitter in the CNS, activates eight known subtypes of metabotropic glutamate receptors (mGluRs). Highly selective modulators designed to act at allosteric sites on certain mGluR subtypes are being developed to preferentially regulate subtype-specific, glutamate-induced receptor activation.{22053} Ro 01-6128 is a positive allosteric modulator of mGluR1 that can potentiate glutamate-induced calcium release at rat mGluR1a with an EC50 value of 104 nM.{22051,22050} Ro 01-6128 activates ERK1/2 phosphorylation in the absence of exogenously added glutamate with an EC50 value of 248 nM and potentiates glutamate-induced cAMP production with an EC50 value of 21.5 μM.{22053}  

     

    Brand:
    Cayman
    SKU:11991 - 1 mg

    Available on backorder

  • Glutamate, the major excitatory neurotransmitter in the CNS, activates eight known subtypes of metabotropic glutamate receptors (mGluRs). Highly selective modulators designed to act at allosteric sites on certain mGluR subtypes are being developed to preferentially regulate subtype-specific, glutamate-induced receptor activation.{22053} Ro 01-6128 is a positive allosteric modulator of mGluR1 that can potentiate glutamate-induced calcium release at rat mGluR1a with an EC50 value of 104 nM.{22051,22050} Ro 01-6128 activates ERK1/2 phosphorylation in the absence of exogenously added glutamate with an EC50 value of 248 nM and potentiates glutamate-induced cAMP production with an EC50 value of 21.5 μM.{22053}  

     

    Brand:
    Cayman
    SKU:11991 - 10 mg

    Available on backorder

  • Glutamate, the major excitatory neurotransmitter in the CNS, activates eight known subtypes of metabotropic glutamate receptors (mGluRs). Highly selective modulators designed to act at allosteric sites on certain mGluR subtypes are being developed to preferentially regulate subtype-specific, glutamate-induced receptor activation.{22053} Ro 01-6128 is a positive allosteric modulator of mGluR1 that can potentiate glutamate-induced calcium release at rat mGluR1a with an EC50 value of 104 nM.{22051,22050} Ro 01-6128 activates ERK1/2 phosphorylation in the absence of exogenously added glutamate with an EC50 value of 248 nM and potentiates glutamate-induced cAMP production with an EC50 value of 21.5 μM.{22053}  

     

    Brand:
    Cayman
    SKU:11991 - 5 mg

    Available on backorder

  • Ro 08-2750 is a p75 neurotrophin receptor (p75NTR) ligand that completely inhibits nerve growth factor (NGF) binding to p75NTR in PC12 cells when used at a concentration of 100 μM.{47722} It also binds to NGF dimers (Kd = ~1 μM) to induce a conformational change that prevents NGF binding to p75NTR or tropomyosin-related kinase A (TrkA). Ro 08-2750 inhibits NGF-induced death of SK-N-MC cells and inhibits autophosphorylation of TrkA in PC12 cells. It reverses NGF-induced decreases in β-catenin mRNA expression in, and migration of, SKOV3 and OVCAR-3 ovarian cancer cells.{47723}  

     

    Brand:
    Cayman
    SKU:28772 - 1 mg

    Available on backorder

  • Ro 08-2750 is a p75 neurotrophin receptor (p75NTR) ligand that completely inhibits nerve growth factor (NGF) binding to p75NTR in PC12 cells when used at a concentration of 100 μM.{47722} It also binds to NGF dimers (Kd = ~1 μM) to induce a conformational change that prevents NGF binding to p75NTR or tropomyosin-related kinase A (TrkA). Ro 08-2750 inhibits NGF-induced death of SK-N-MC cells and inhibits autophosphorylation of TrkA in PC12 cells. It reverses NGF-induced decreases in β-catenin mRNA expression in, and migration of, SKOV3 and OVCAR-3 ovarian cancer cells.{47723}  

     

    Brand:
    Cayman
    SKU:28772 - 10 mg

    Available on backorder

  • Ro 08-2750 is a p75 neurotrophin receptor (p75NTR) ligand that completely inhibits nerve growth factor (NGF) binding to p75NTR in PC12 cells when used at a concentration of 100 μM.{47722} It also binds to NGF dimers (Kd = ~1 μM) to induce a conformational change that prevents NGF binding to p75NTR or tropomyosin-related kinase A (TrkA). Ro 08-2750 inhibits NGF-induced death of SK-N-MC cells and inhibits autophosphorylation of TrkA in PC12 cells. It reverses NGF-induced decreases in β-catenin mRNA expression in, and migration of, SKOV3 and OVCAR-3 ovarian cancer cells.{47723}  

     

    Brand:
    Cayman
    SKU:28772 - 5 mg

    Available on backorder

  • Transcriptional activation by NF-κB is limited by IκBα binding, which masks the NF-κB nuclear localization signal that initiates nuclear translocation. Cytokines trigger a signaling cascade of kinases that target IκBα for degradation, enabling NF-κB to promote gene expression. Because NF-κB regulates the transcription of inflammatory mediators, blocking its signaling activity is regarded as an effective means to treat inflammatory diseases. Ro 106-9920 is a small molecule inhibitor of NF-κB-dependent expression of TNF-α, interleukin-1β, and interleukin-6 (IC50 50 value of 2.3 µM demonstrating little activity against the ubiquitin-activating enzyme E1 (IC50s >100 µM), the ubiquinating-conjugating enzyme E2UBCH7, nonspecific ubiquitination of cellular proteins, and 97 other molecular targets.{25615} In two different models of acute inflammation, Ro 106-9920 at 10-100 mg/kg has been shown to dose-dependently inhibit cytokine production in rat.{25615}  

     

    Brand:
    Cayman
    SKU:-
  • Transcriptional activation by NF-κB is limited by IκBα binding, which masks the NF-κB nuclear localization signal that initiates nuclear translocation. Cytokines trigger a signaling cascade of kinases that target IκBα for degradation, enabling NF-κB to promote gene expression. Because NF-κB regulates the transcription of inflammatory mediators, blocking its signaling activity is regarded as an effective means to treat inflammatory diseases. Ro 106-9920 is a small molecule inhibitor of NF-κB-dependent expression of TNF-α, interleukin-1β, and interleukin-6 (IC50 50 value of 2.3 µM demonstrating little activity against the ubiquitin-activating enzyme E1 (IC50s >100 µM), the ubiquinating-conjugating enzyme E2UBCH7, nonspecific ubiquitination of cellular proteins, and 97 other molecular targets.{25615} In two different models of acute inflammation, Ro 106-9920 at 10-100 mg/kg has been shown to dose-dependently inhibit cytokine production in rat.{25615}  

     

    Brand:
    Cayman
    SKU:-
  • Transcriptional activation by NF-κB is limited by IκBα binding, which masks the NF-κB nuclear localization signal that initiates nuclear translocation. Cytokines trigger a signaling cascade of kinases that target IκBα for degradation, enabling NF-κB to promote gene expression. Because NF-κB regulates the transcription of inflammatory mediators, blocking its signaling activity is regarded as an effective means to treat inflammatory diseases. Ro 106-9920 is a small molecule inhibitor of NF-κB-dependent expression of TNF-α, interleukin-1β, and interleukin-6 (IC50 50 value of 2.3 µM demonstrating little activity against the ubiquitin-activating enzyme E1 (IC50s >100 µM), the ubiquinating-conjugating enzyme E2UBCH7, nonspecific ubiquitination of cellular proteins, and 97 other molecular targets.{25615} In two different models of acute inflammation, Ro 106-9920 at 10-100 mg/kg has been shown to dose-dependently inhibit cytokine production in rat.{25615}  

     

    Brand:
    Cayman
    SKU:-
  • Ro 20-1724 is a cell-permeable, cAMP-specific phosphodiesterase type IV (PDE4) inhibitor (IC50 = 2 µM).{29744,29745} It weakly inhibits PDE3 with a Ki value greater than 25 µM.{29744} Ro 20-1724 inhibits the release of cytokines and other inflammatory signals as well as prevents the development of reactive oxygen species.{29746} It is often used to study cAMP-related functions in vascular cells.{27634}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Ro 20-1724 is a cell-permeable, cAMP-specific phosphodiesterase type IV (PDE4) inhibitor (IC50 = 2 µM).{29744,29745} It weakly inhibits PDE3 with a Ki value greater than 25 µM.{29744} Ro 20-1724 inhibits the release of cytokines and other inflammatory signals as well as prevents the development of reactive oxygen species.{29746} It is often used to study cAMP-related functions in vascular cells.{27634}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Ro 20-1724 is a cell-permeable, cAMP-specific phosphodiesterase type IV (PDE4) inhibitor (IC50 = 2 µM).{29744,29745} It weakly inhibits PDE3 with a Ki value greater than 25 µM.{29744} Ro 20-1724 inhibits the release of cytokines and other inflammatory signals as well as prevents the development of reactive oxygen species.{29746} It is often used to study cAMP-related functions in vascular cells.{27634}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Ro 25-6981 (maleate) is a potent, selective activity-dependent blocker of NMDA receptors containing the NR2B subunit (IC50s = 9 nM and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A, respectively).{22852} Ro 25-6981 (maleate) displays neuroprotectant effects in vitro, protecting cortical neurons against glutamate toxicity and combined oxygen and glucose deprivation with IC50 values of 0.4 and 0.04 μM, respectively.{22852}  

     

    Brand:
    Cayman
    SKU:-
  • Ro 25-6981 (maleate) is a potent, selective activity-dependent blocker of NMDA receptors containing the NR2B subunit (IC50s = 9 nM and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A, respectively).{22852} Ro 25-6981 (maleate) displays neuroprotectant effects in vitro, protecting cortical neurons against glutamate toxicity and combined oxygen and glucose deprivation with IC50 values of 0.4 and 0.04 μM, respectively.{22852}  

     

    Brand:
    Cayman
    SKU:-
  • Ro 25-6981 (maleate) is a potent, selective activity-dependent blocker of NMDA receptors containing the NR2B subunit (IC50s = 9 nM and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A, respectively).{22852} Ro 25-6981 (maleate) displays neuroprotectant effects in vitro, protecting cortical neurons against glutamate toxicity and combined oxygen and glucose deprivation with IC50 values of 0.4 and 0.04 μM, respectively.{22852}  

     

    Brand:
    Cayman
    SKU:-
  • Ro 3280 is a selective inhibitor of polo-like kinase 1 (Plk1), a proto-oncogene, with IC50 values of 3 and 6 nM in an enzymatic assay and H82 lung cancer cells, respectively.{34562} Ro 3280 is over 500-fold selective for PlK1 over a panel of 318 kinases. It inhibits tumor growth in a mouse xenograft model using the HT-29 colorectal cancer cell line, increases autophagy and mTOR phosphorylation in NB4 acute myeloid leukemia cells, and induces apoptosis in human bladder cancer and leukemia cells.{34562,34563,34565,34564}  

     

    Brand:
    Cayman
    SKU:21669 -

    Out of stock

  • Ro 3280 is a selective inhibitor of polo-like kinase 1 (Plk1), a proto-oncogene, with IC50 values of 3 and 6 nM in an enzymatic assay and H82 lung cancer cells, respectively.{34562} Ro 3280 is over 500-fold selective for PlK1 over a panel of 318 kinases. It inhibits tumor growth in a mouse xenograft model using the HT-29 colorectal cancer cell line, increases autophagy and mTOR phosphorylation in NB4 acute myeloid leukemia cells, and induces apoptosis in human bladder cancer and leukemia cells.{34562,34563,34565,34564}  

     

    Brand:
    Cayman
    SKU:21669 -

    Out of stock

  • Ro 3280 is a selective inhibitor of polo-like kinase 1 (Plk1), a proto-oncogene, with IC50 values of 3 and 6 nM in an enzymatic assay and H82 lung cancer cells, respectively.{34562} Ro 3280 is over 500-fold selective for PlK1 over a panel of 318 kinases. It inhibits tumor growth in a mouse xenograft model using the HT-29 colorectal cancer cell line, increases autophagy and mTOR phosphorylation in NB4 acute myeloid leukemia cells, and induces apoptosis in human bladder cancer and leukemia cells.{34562,34563,34565,34564}  

     

    Brand:
    Cayman
    SKU:21669 -

    Out of stock

  • Ro 3280 is a selective inhibitor of polo-like kinase 1 (Plk1), a proto-oncogene, with IC50 values of 3 and 6 nM in an enzymatic assay and H82 lung cancer cells, respectively.{34562} Ro 3280 is over 500-fold selective for PlK1 over a panel of 318 kinases. It inhibits tumor growth in a mouse xenograft model using the HT-29 colorectal cancer cell line, increases autophagy and mTOR phosphorylation in NB4 acute myeloid leukemia cells, and induces apoptosis in human bladder cancer and leukemia cells.{34562,34563,34565,34564}  

     

    Brand:
    Cayman
    SKU:21669 -

    Out of stock

  • Cyclin-dependent kinase 1 (Cdk1) complexes with different cyclins, with the cyclin determining substrate specificity. Ro 3306 is a cell-permeable, reversible inhibitor of Cdk1, showing preference for Cdk1/cyclin B1 (Ki = 35 nM) over Cdk1/cyclin A (Ki = 110 nM), two CDK complexes which regulate cell cycling.{24139} It also inhibits Cdk2 (Ki = 340 nM), PKCδ (Ki = 318 nM), and serum- and glucocorticoid-induce kinase (Ki = 497 nM) but not Cdk4.{24139} Through its effects on Cdk1, Ro 3306 reversibly arrests proliferating cells at the G2/M phase border, allowing cell synchronization without the use of microtubule poisons.{24140} Prolonged treatment of cells with Ro 3306 induces apoptosis and this can be augmented in acute myeloid leukemia cells by stimulating p53 activity with nutlin-3.{24141}  

     

    Brand:
    Cayman
    SKU:-
  • Cyclin-dependent kinase 1 (Cdk1) complexes with different cyclins, with the cyclin determining substrate specificity. Ro 3306 is a cell-permeable, reversible inhibitor of Cdk1, showing preference for Cdk1/cyclin B1 (Ki = 35 nM) over Cdk1/cyclin A (Ki = 110 nM), two CDK complexes which regulate cell cycling.{24139} It also inhibits Cdk2 (Ki = 340 nM), PKCδ (Ki = 318 nM), and serum- and glucocorticoid-induce kinase (Ki = 497 nM) but not Cdk4.{24139} Through its effects on Cdk1, Ro 3306 reversibly arrests proliferating cells at the G2/M phase border, allowing cell synchronization without the use of microtubule poisons.{24140} Prolonged treatment of cells with Ro 3306 induces apoptosis and this can be augmented in acute myeloid leukemia cells by stimulating p53 activity with nutlin-3.{24141}  

     

    Brand:
    Cayman
    SKU:-
  • Cyclin-dependent kinase 1 (Cdk1) complexes with different cyclins, with the cyclin determining substrate specificity. Ro 3306 is a cell-permeable, reversible inhibitor of Cdk1, showing preference for Cdk1/cyclin B1 (Ki = 35 nM) over Cdk1/cyclin A (Ki = 110 nM), two CDK complexes which regulate cell cycling.{24139} It also inhibits Cdk2 (Ki = 340 nM), PKCδ (Ki = 318 nM), and serum- and glucocorticoid-induce kinase (Ki = 497 nM) but not Cdk4.{24139} Through its effects on Cdk1, Ro 3306 reversibly arrests proliferating cells at the G2/M phase border, allowing cell synchronization without the use of microtubule poisons.{24140} Prolonged treatment of cells with Ro 3306 induces apoptosis and this can be augmented in acute myeloid leukemia cells by stimulating p53 activity with nutlin-3.{24141}  

     

    Brand:
    Cayman
    SKU:-
  • Cyclin-dependent kinase 1 (Cdk1) complexes with different cyclins, with the cyclin determining substrate specificity. Ro 3306 is a cell-permeable, reversible inhibitor of Cdk1, showing preference for Cdk1/cyclin B1 (Ki = 35 nM) over Cdk1/cyclin A (Ki = 110 nM), two CDK complexes which regulate cell cycling.{24139} It also inhibits Cdk2 (Ki = 340 nM), PKCδ (Ki = 318 nM), and serum- and glucocorticoid-induce kinase (Ki = 497 nM) but not Cdk4.{24139} Through its effects on Cdk1, Ro 3306 reversibly arrests proliferating cells at the G2/M phase border, allowing cell synchronization without the use of microtubule poisons.{24140} Prolonged treatment of cells with Ro 3306 induces apoptosis and this can be augmented in acute myeloid leukemia cells by stimulating p53 activity with nutlin-3.{24141}  

     

    Brand:
    Cayman
    SKU:-
  • Ro 41-0960 is a catechol-O-methyltransferase (COMT) inhibitor.{48777} It prevents dopaminergic neuron loss induced by L-DOPA (Item No. 13248) in primary rat rostral mesencephalic tegmentum cultures (EC50 = 0.1 µM). Ro 41-0960 (30 mg/kg) potentiates L-DOPA and carbidopa-induced reversal of reserpine-induced akinesias in rats and reserpine-induced catalepsy and hypothermia in mice.{48778} It reduces striatal 3-methyl-DOPA levels and increases striatal dopamine (Item No. 21992) and 3,4-dihydroxyphenylacetic acid (DOPAC; Item No. 24912) levels in rats. Ro 41-0960 (150 mg/kg) also reduces fibroid volume in the Eker rat model of uterine fibroids.{48779}  

     

    Brand:
    Cayman
    SKU:29621 - 10 mg

    Available on backorder

  • Ro 41-0960 is a catechol-O-methyltransferase (COMT) inhibitor.{48777} It prevents dopaminergic neuron loss induced by L-DOPA (Item No. 13248) in primary rat rostral mesencephalic tegmentum cultures (EC50 = 0.1 µM). Ro 41-0960 (30 mg/kg) potentiates L-DOPA and carbidopa-induced reversal of reserpine-induced akinesias in rats and reserpine-induced catalepsy and hypothermia in mice.{48778} It reduces striatal 3-methyl-DOPA levels and increases striatal dopamine (Item No. 21992) and 3,4-dihydroxyphenylacetic acid (DOPAC; Item No. 24912) levels in rats. Ro 41-0960 (150 mg/kg) also reduces fibroid volume in the Eker rat model of uterine fibroids.{48779}  

     

    Brand:
    Cayman
    SKU:29621 - 25 mg

    Available on backorder

  • Ro 41-0960 is a catechol-O-methyltransferase (COMT) inhibitor.{48777} It prevents dopaminergic neuron loss induced by L-DOPA (Item No. 13248) in primary rat rostral mesencephalic tegmentum cultures (EC50 = 0.1 µM). Ro 41-0960 (30 mg/kg) potentiates L-DOPA and carbidopa-induced reversal of reserpine-induced akinesias in rats and reserpine-induced catalepsy and hypothermia in mice.{48778} It reduces striatal 3-methyl-DOPA levels and increases striatal dopamine (Item No. 21992) and 3,4-dihydroxyphenylacetic acid (DOPAC; Item No. 24912) levels in rats. Ro 41-0960 (150 mg/kg) also reduces fibroid volume in the Eker rat model of uterine fibroids.{48779}  

     

    Brand:
    Cayman
    SKU:29621 - 5 mg

    Available on backorder

  • Oxidosqualene cyclase (OSC) is a microsomal enzyme that catalyzes the cyclization of monooxidosqualene to lanosterol in the cholesterol synthetic pathway.{8343,12383} Ro 48-8071 is an inhibitor of oxidosqualene cyclase (OSC) that has low-density lipoprotein (LDL) cholesterol lowering activity similar to the 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitor simvastatin.{13141} It inhibits OSC from human liver microsomes and HepG2 cells with IC50 values of approximately 6.5 nM and 1.5 nM, respectively.{13141} Ro 48-8071 lowered LDL cholesterol ~40% in hamsters at a dose of 150 µg/kg without affecting high-density lipoprotein levels and with no sign of liver toxicity.{13141} Ro 48-8071 increases cytochrome P3A mRNA and protein levels in primary rat and murine hepatocyte cultures with a maximal effect at 30 µM.{13142}  

     

    Brand:
    Cayman
    SKU:10006415 - 10 mg

    Available on backorder

  • Oxidosqualene cyclase (OSC) is a microsomal enzyme that catalyzes the cyclization of monooxidosqualene to lanosterol in the cholesterol synthetic pathway.{8343,12383} Ro 48-8071 is an inhibitor of oxidosqualene cyclase (OSC) that has low-density lipoprotein (LDL) cholesterol lowering activity similar to the 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitor simvastatin.{13141} It inhibits OSC from human liver microsomes and HepG2 cells with IC50 values of approximately 6.5 nM and 1.5 nM, respectively.{13141} Ro 48-8071 lowered LDL cholesterol ~40% in hamsters at a dose of 150 µg/kg without affecting high-density lipoprotein levels and with no sign of liver toxicity.{13141} Ro 48-8071 increases cytochrome P3A mRNA and protein levels in primary rat and murine hepatocyte cultures with a maximal effect at 30 µM.{13142}  

     

    Brand:
    Cayman
    SKU:10006415 - 100 mg

    Available on backorder

  • Oxidosqualene cyclase (OSC) is a microsomal enzyme that catalyzes the cyclization of monooxidosqualene to lanosterol in the cholesterol synthetic pathway.{8343,12383} Ro 48-8071 is an inhibitor of oxidosqualene cyclase (OSC) that has low-density lipoprotein (LDL) cholesterol lowering activity similar to the 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitor simvastatin.{13141} It inhibits OSC from human liver microsomes and HepG2 cells with IC50 values of approximately 6.5 nM and 1.5 nM, respectively.{13141} Ro 48-8071 lowered LDL cholesterol ~40% in hamsters at a dose of 150 µg/kg without affecting high-density lipoprotein levels and with no sign of liver toxicity.{13141} Ro 48-8071 increases cytochrome P3A mRNA and protein levels in primary rat and murine hepatocyte cultures with a maximal effect at 30 µM.{13142}  

     

    Brand:
    Cayman
    SKU:10006415 - 5 mg

    Available on backorder

  • Oxidosqualene cyclase (OSC) is a microsomal enzyme that catalyzes the cyclization of monooxidosqualene to lanosterol in the cholesterol synthetic pathway.{8343,12383} Ro 48-8071 is an inhibitor of oxidosqualene cyclase (OSC) that has low-density lipoprotein (LDL) cholesterol lowering activity similar to the 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitor simvastatin.{13141} It inhibits OSC from human liver microsomes and HepG2 cells with IC50 values of approximately 6.5 nM and 1.5 nM, respectively.{13141} Ro 48-8071 lowered LDL cholesterol ~40% in hamsters at a dose of 150 µg/kg without affecting high-density lipoprotein levels and with no sign of liver toxicity.{13141} Ro 48-8071 increases cytochrome P3A mRNA and protein levels in primary rat and murine hepatocyte cultures with a maximal effect at 30 µM.{13142}  

     

    Brand:
    Cayman
    SKU:10006415 - 50 mg

    Available on backorder

  • Ro 4929097 is a potent inhibitor of γ-secretase (IC50 = 4 nM) that blocks both Aβ40 and Notch processing (IC50s = 14 and 5 nM, respectively).{32226} It displays greater than 100-fold selectivity for γ-secretase over a panel of 75 other enzymes, receptors, and ion channels. Ro 4929097 does not block tumor cell growth or induce apoptosis but instead produces a less transformed, flattened, slower-growing phenotype.{32226} It is orally active against cancer xenograft models, altering gene expression related to angiogenesis and cell differentiation.{32226} Ro 4929097 also reduces tumor initiating potential of melanoma cells in vivo by blocking Notch-dependent gene expression.{32225}  

     

    Brand:
    Cayman
    SKU:19996 -

    Available on backorder

  • Ro 4929097 is a potent inhibitor of γ-secretase (IC50 = 4 nM) that blocks both Aβ40 and Notch processing (IC50s = 14 and 5 nM, respectively).{32226} It displays greater than 100-fold selectivity for γ-secretase over a panel of 75 other enzymes, receptors, and ion channels. Ro 4929097 does not block tumor cell growth or induce apoptosis but instead produces a less transformed, flattened, slower-growing phenotype.{32226} It is orally active against cancer xenograft models, altering gene expression related to angiogenesis and cell differentiation.{32226} Ro 4929097 also reduces tumor initiating potential of melanoma cells in vivo by blocking Notch-dependent gene expression.{32225}  

     

    Brand:
    Cayman
    SKU:19996 -

    Available on backorder

  • Ro 4929097 is a potent inhibitor of γ-secretase (IC50 = 4 nM) that blocks both Aβ40 and Notch processing (IC50s = 14 and 5 nM, respectively).{32226} It displays greater than 100-fold selectivity for γ-secretase over a panel of 75 other enzymes, receptors, and ion channels. Ro 4929097 does not block tumor cell growth or induce apoptosis but instead produces a less transformed, flattened, slower-growing phenotype.{32226} It is orally active against cancer xenograft models, altering gene expression related to angiogenesis and cell differentiation.{32226} Ro 4929097 also reduces tumor initiating potential of melanoma cells in vivo by blocking Notch-dependent gene expression.{32225}  

     

    Brand:
    Cayman
    SKU:19996 -

    Available on backorder