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Showing 39451–39600 of 45550 results

  • SHS4121705 is an orally bioavailable mitochondrial uncoupler.{54188} It increases oxygen consumption rate in L6 rat myoblast cells with an EC50 value of 4.3 μM. SHS4121705 (25 mg/kg per day in the diet) reduces hepatic steatosis, liver triglyceride levels, and plasma alanine aminotransferase (ALT) levels in Stelic animal model (STAM) mice, a model of non-alcoholic steatohepatitis (NASH).  

     

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    SKU:31053 - 10 mg

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  • SHS4121705 is an orally bioavailable mitochondrial uncoupler.{54188} It increases oxygen consumption rate in L6 rat myoblast cells with an EC50 value of 4.3 μM. SHS4121705 (25 mg/kg per day in the diet) reduces hepatic steatosis, liver triglyceride levels, and plasma alanine aminotransferase (ALT) levels in Stelic animal model (STAM) mice, a model of non-alcoholic steatohepatitis (NASH).  

     

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    SKU:31053 - 5 mg

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  • SHU9119 is an agonist of melanocortin receptor 1 (MC1R) and antagonist of MC4R (IC50s = 1.2 and 2.9 nM, respectively, for displacement of melanocortin).{41427} It induces cAMP formation in HEK293 cells expressing human MC1R (EC50 = 1.11 nM), but inhibits cAMP formation in cells expressing human MC4R.{41427} In rats, SHU9119 (24 nmol, i.c.v. per day for seven days) increases food intake, body weight, fat mass, and lean mass, with concomitant increases in blood glucose, insulin, and leptin levels via disrupted melanocortin signaling.{41426} Similarly, mice treated with SHU9119 (5 nmol/day, i.c.v.) exhibit food intake-independent increases in body weight and fat mass consequent to MC4R inhibition and subsequent brown adipose tissue dysfunction.{41425}  

     

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    SKU:24152 - 1 mg

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  • SHU9119 is an agonist of melanocortin receptor 1 (MC1R) and antagonist of MC4R (IC50s = 1.2 and 2.9 nM, respectively, for displacement of melanocortin).{41427} It induces cAMP formation in HEK293 cells expressing human MC1R (EC50 = 1.11 nM), but inhibits cAMP formation in cells expressing human MC4R.{41427} In rats, SHU9119 (24 nmol, i.c.v. per day for seven days) increases food intake, body weight, fat mass, and lean mass, with concomitant increases in blood glucose, insulin, and leptin levels via disrupted melanocortin signaling.{41426} Similarly, mice treated with SHU9119 (5 nmol/day, i.c.v.) exhibit food intake-independent increases in body weight and fat mass consequent to MC4R inhibition and subsequent brown adipose tissue dysfunction.{41425}  

     

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    SKU:24152 - 500 µg

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  • Shz-1 is a Shz that activates cardiac differentiation, inducing the expression of early cardiac genes in mouse pluripotent and embryonic stem cells in vitro at low micromolar concentrations.{24724} In addition, Shz-1 drives differentiation of human peripheral blood mononuclear cells, mobilized by granule colony-stimulating factor, toward a cardiac phenotype.{24724} These Shz-1 treated cells enhance myocardial regenerative repair in cryo-injured rat heart.{24724}  

     

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  • Shz-1 is a Shz that activates cardiac differentiation, inducing the expression of early cardiac genes in mouse pluripotent and embryonic stem cells in vitro at low micromolar concentrations.{24724} In addition, Shz-1 drives differentiation of human peripheral blood mononuclear cells, mobilized by granule colony-stimulating factor, toward a cardiac phenotype.{24724} These Shz-1 treated cells enhance myocardial regenerative repair in cryo-injured rat heart.{24724}  

     

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  • Shz-1 is a Shz that activates cardiac differentiation, inducing the expression of early cardiac genes in mouse pluripotent and embryonic stem cells in vitro at low micromolar concentrations.{24724} In addition, Shz-1 drives differentiation of human peripheral blood mononuclear cells, mobilized by granule colony-stimulating factor, toward a cardiac phenotype.{24724} These Shz-1 treated cells enhance myocardial regenerative repair in cryo-injured rat heart.{24724}  

     

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  • Shz-1 is a Shz that activates cardiac differentiation, inducing the expression of early cardiac genes in mouse pluripotent and embryonic stem cells in vitro at low micromolar concentrations.{24724} In addition, Shz-1 drives differentiation of human peripheral blood mononuclear cells, mobilized by granule colony-stimulating factor, toward a cardiac phenotype.{24724} These Shz-1 treated cells enhance myocardial regenerative repair in cryo-injured rat heart.{24724}  

     

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  • SI-2 is an inhibitor of steroid receptor coactivator 3 (SRC-3). It has been shown to selectively reduce the transcriptional activities and the protein concentrations of SRC-3 in cells through direct physical interactions with SRC-3.{31177} SI-2 induces death in various breast cancer cells with IC50 values of 3-20 nM without affecting normal cell viability.{31177} At 2 mg/kg, SI-2 can also inhibit primary tumor growth and reduce SRC-3 protein levels in an MDA-MB-468 breast cancer mouse model.{31177}  

     

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  • SI-2 is an inhibitor of steroid receptor coactivator 3 (SRC-3). It has been shown to selectively reduce the transcriptional activities and the protein concentrations of SRC-3 in cells through direct physical interactions with SRC-3.{31177} SI-2 induces death in various breast cancer cells with IC50 values of 3-20 nM without affecting normal cell viability.{31177} At 2 mg/kg, SI-2 can also inhibit primary tumor growth and reduce SRC-3 protein levels in an MDA-MB-468 breast cancer mouse model.{31177}  

     

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  • SI-2 is an inhibitor of steroid receptor coactivator 3 (SRC-3). It has been shown to selectively reduce the transcriptional activities and the protein concentrations of SRC-3 in cells through direct physical interactions with SRC-3.{31177} SI-2 induces death in various breast cancer cells with IC50 values of 3-20 nM without affecting normal cell viability.{31177} At 2 mg/kg, SI-2 can also inhibit primary tumor growth and reduce SRC-3 protein levels in an MDA-MB-468 breast cancer mouse model.{31177}  

     

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  • SI-2 is an inhibitor of steroid receptor coactivator 3 (SRC-3). It has been shown to selectively reduce the transcriptional activities and the protein concentrations of SRC-3 in cells through direct physical interactions with SRC-3.{31177} SI-2 induces death in various breast cancer cells with IC50 values of 3-20 nM without affecting normal cell viability.{31177} At 2 mg/kg, SI-2 can also inhibit primary tumor growth and reduce SRC-3 protein levels in an MDA-MB-468 breast cancer mouse model.{31177}  

     

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  • Siamycin I is a tricyclic peptide originally isolated from Streptomyces and has antiviral and antibacterial activities.{47469,47470} It is active against laboratory strains and clinical isolates of HIV-1 (ED50s = 0.05-0.45 and 0.89-5.7 μM, respectively), as well as the CBL-20 strain of HIV-2 (ED50 = 0.45 μM), in vitro.{47469} Siamycin I inhibits HIV-induced fusion of C8166 T cells with HIV-1-infected CEM-SS cells with an ED50 value of 0.08 μM. It is also active against B. subtilis, M. luteus, and S. aureus (MICs = 1.6-6.3 μg/ml).{47470} Siamycin I inhibits autophosphorylation of the E. faecalis quorum sensing kinase FsrC induced by gelatinase biosynthesis-activating pheromone (GBAP).{47471}  

     

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    SKU:27783 - 1 mg

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  • Siamycin I is a tricyclic peptide originally isolated from Streptomyces and has antiviral and antibacterial activities.{47469,47470} It is active against laboratory strains and clinical isolates of HIV-1 (ED50s = 0.05-0.45 and 0.89-5.7 μM, respectively), as well as the CBL-20 strain of HIV-2 (ED50 = 0.45 μM), in vitro.{47469} Siamycin I inhibits HIV-induced fusion of C8166 T cells with HIV-1-infected CEM-SS cells with an ED50 value of 0.08 μM. It is also active against B. subtilis, M. luteus, and S. aureus (MICs = 1.6-6.3 μg/ml).{47470} Siamycin I inhibits autophosphorylation of the E. faecalis quorum sensing kinase FsrC induced by gelatinase biosynthesis-activating pheromone (GBAP).{47471}  

     

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    SKU:27783 - 500 µg

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  • SIB 1553A is an agonist of nicotinic acetylcholine receptors (nAChRs) that displays selectivity for β4 subunit-containing receptors.{33653} Formulations containing SIB 1553A improve attentional function and performance in spatial and non-spatial working memory tasks in animals.{33653,33654,33655}  

     

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  • SIB 1553A is an agonist of nicotinic acetylcholine receptors (nAChRs) that displays selectivity for β4 subunit-containing receptors.{33653} Formulations containing SIB 1553A improve attentional function and performance in spatial and non-spatial working memory tasks in animals.{33653,33654,33655}  

     

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  • SIB 1553A is an agonist of nicotinic acetylcholine receptors (nAChRs) that displays selectivity for β4 subunit-containing receptors.{33653} Formulations containing SIB 1553A improve attentional function and performance in spatial and non-spatial working memory tasks in animals.{33653,33654,33655}  

     

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  • SIB 1553A is an agonist of nicotinic acetylcholine receptors (nAChRs) that displays selectivity for β4 subunit-containing receptors.{33653} Formulations containing SIB 1553A improve attentional function and performance in spatial and non-spatial working memory tasks in animals.{33653,33654,33655}  

     

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  • Siccanin is an inhibitor of mitochondrial complex II (succinate dehydrogenase; IC50s = 0.87 and 9.3 μM for P. aeruginosa and rat mitochondria, respectively).{41290} It inhibits the growth of T. mentagrophytes (IC50 = 0.3 μg/ml) via inhibition of succinate oxidation in the mitochondria.{41291} It also inhibits the growth of C. albicans strains with IC50 values ranging from 5-40 and 80-90 μg/ml for aerobic and anaerobic conditions, respectively.{41292}  

     

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    SKU:23654 - 1 mg

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  • Siccanin is an inhibitor of mitochondrial complex II (succinate dehydrogenase; IC50s = 0.87 and 9.3 μM for P. aeruginosa and rat mitochondria, respectively).{41290} It inhibits the growth of T. mentagrophytes (IC50 = 0.3 μg/ml) via inhibition of succinate oxidation in the mitochondria.{41291} It also inhibits the growth of C. albicans strains with IC50 values ranging from 5-40 and 80-90 μg/ml for aerobic and anaerobic conditions, respectively.{41292}  

     

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    SKU:23654 - 500 µg

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  • SID 3712249 inhibits the biogenesis of microRNA-544 (miR-544), a silencer of mammalian target of rapamycin (mTOR).{54014} Under hypoxic conditions, SID 3712249 (20 nM) increases MTOR mRNA expression and decreases the mRNA expression of the genes encoding miR-544, hypoxia-inducible factor-1α (HIF-1α), and ataxia-telangiectasia mutated kinase (ATM) in MDA-MB-231, MCF-7, and MCF-10A cells. It induces apoptosis in MDA-MB-231 cells in a hypoxia- and mTOR-dependent manner when used at a concentration of 20 nM. SID 3712249 (20 nM) enhances the sensitivity of MCF-7 and MDA-MB-231 cells cultured under hypoxic conditions to decreases in cell viability induced by 5-fluorouracil (5-FU; Item No. 14416). It reduces tumor growth in an MDA-MB-231 mouse xenograft model.  

     

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    SKU:29723 - 10 mg

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  • SID 3712249 inhibits the biogenesis of microRNA-544 (miR-544), a silencer of mammalian target of rapamycin (mTOR).{54014} Under hypoxic conditions, SID 3712249 (20 nM) increases MTOR mRNA expression and decreases the mRNA expression of the genes encoding miR-544, hypoxia-inducible factor-1α (HIF-1α), and ataxia-telangiectasia mutated kinase (ATM) in MDA-MB-231, MCF-7, and MCF-10A cells. It induces apoptosis in MDA-MB-231 cells in a hypoxia- and mTOR-dependent manner when used at a concentration of 20 nM. SID 3712249 (20 nM) enhances the sensitivity of MCF-7 and MDA-MB-231 cells cultured under hypoxic conditions to decreases in cell viability induced by 5-fluorouracil (5-FU; Item No. 14416). It reduces tumor growth in an MDA-MB-231 mouse xenograft model.  

     

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    SKU:29723 - 25 mg

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  • SID 3712249 inhibits the biogenesis of microRNA-544 (miR-544), a silencer of mammalian target of rapamycin (mTOR).{54014} Under hypoxic conditions, SID 3712249 (20 nM) increases MTOR mRNA expression and decreases the mRNA expression of the genes encoding miR-544, hypoxia-inducible factor-1α (HIF-1α), and ataxia-telangiectasia mutated kinase (ATM) in MDA-MB-231, MCF-7, and MCF-10A cells. It induces apoptosis in MDA-MB-231 cells in a hypoxia- and mTOR-dependent manner when used at a concentration of 20 nM. SID 3712249 (20 nM) enhances the sensitivity of MCF-7 and MDA-MB-231 cells cultured under hypoxic conditions to decreases in cell viability induced by 5-fluorouracil (5-FU; Item No. 14416). It reduces tumor growth in an MDA-MB-231 mouse xenograft model.  

     

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    SKU:29723 - 5 mg

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  • SID 3712249 inhibits the biogenesis of microRNA-544 (miR-544), a silencer of mammalian target of rapamycin (mTOR).{54014} Under hypoxic conditions, SID 3712249 (20 nM) increases MTOR mRNA expression and decreases the mRNA expression of the genes encoding miR-544, hypoxia-inducible factor-1α (HIF-1α), and ataxia-telangiectasia mutated kinase (ATM) in MDA-MB-231, MCF-7, and MCF-10A cells. It induces apoptosis in MDA-MB-231 cells in a hypoxia- and mTOR-dependent manner when used at a concentration of 20 nM. SID 3712249 (20 nM) enhances the sensitivity of MCF-7 and MDA-MB-231 cells cultured under hypoxic conditions to decreases in cell viability induced by 5-fluorouracil (5-FU; Item No. 14416). It reduces tumor growth in an MDA-MB-231 mouse xenograft model.  

     

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    SKU:29723 - 50 mg

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  • Sildenafil is a potent inhibitor of phosphodiesterase 5 (PDE5) with IC50 values of 3.6 and 3 nM for PDE5 activity in isolated rabbit platelets and human corpus cavernosum, respectively.{21636} It is selective for PDE5 over PDE1 and PDE3 (IC50s = 0.26 and 65 μM, respectively). Sildenafil reverses glucose-induced decreases in angiopoietin 1 (ANG1) expression and reduction of capillary-like tube formation by mouse dermal endothelial cells in vitro and increases the number of functional blood vessels and regional blood flow in the sciatic nerve in a db/db mouse model of diabetic peripheral neuropathy.{42390} It increases the ratio of maximum intracavernosal pressure to mean arterial blood pressure (ICP/MAP), a measure of erectile function, in castrated rats when administered at a dose of 20 mg/kg per day.{42389} Sildenafil (0.5 mg/kg) also reduces cardiac arrest and resuscitation-induced increases in angiotensin II (Item No. 17150), angiotensin converting enzyme (ACE), ACE2, and various angiotensin receptors and increases survival in a porcine model of ischemia/reperfusion injury.{42391} Formulations containing sildenafil have been used in the treatment of erectile dysfunction, pulmonary arterial hypertension, and high-altitude pulmonary edema associated with altitude sickness.  

     

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    SKU:10008671 - 10 mg

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  • Sildenafil is a potent inhibitor of phosphodiesterase 5 (PDE5) with IC50 values of 3.6 and 3 nM for PDE5 activity in isolated rabbit platelets and human corpus cavernosum, respectively.{21636} It is selective for PDE5 over PDE1 and PDE3 (IC50s = 0.26 and 65 μM, respectively). Sildenafil reverses glucose-induced decreases in angiopoietin 1 (ANG1) expression and reduction of capillary-like tube formation by mouse dermal endothelial cells in vitro and increases the number of functional blood vessels and regional blood flow in the sciatic nerve in a db/db mouse model of diabetic peripheral neuropathy.{42390} It increases the ratio of maximum intracavernosal pressure to mean arterial blood pressure (ICP/MAP), a measure of erectile function, in castrated rats when administered at a dose of 20 mg/kg per day.{42389} Sildenafil (0.5 mg/kg) also reduces cardiac arrest and resuscitation-induced increases in angiotensin II (Item No. 17150), angiotensin converting enzyme (ACE), ACE2, and various angiotensin receptors and increases survival in a porcine model of ischemia/reperfusion injury.{42391} Formulations containing sildenafil have been used in the treatment of erectile dysfunction, pulmonary arterial hypertension, and high-altitude pulmonary edema associated with altitude sickness.  

     

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    SKU:10008671 - 25 mg

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  • Sildenafil is a potent inhibitor of phosphodiesterase 5 (PDE5) with IC50 values of 3.6 and 3 nM for PDE5 activity in isolated rabbit platelets and human corpus cavernosum, respectively.{21636} It is selective for PDE5 over PDE1 and PDE3 (IC50s = 0.26 and 65 μM, respectively). Sildenafil reverses glucose-induced decreases in angiopoietin 1 (ANG1) expression and reduction of capillary-like tube formation by mouse dermal endothelial cells in vitro and increases the number of functional blood vessels and regional blood flow in the sciatic nerve in a db/db mouse model of diabetic peripheral neuropathy.{42390} It increases the ratio of maximum intracavernosal pressure to mean arterial blood pressure (ICP/MAP), a measure of erectile function, in castrated rats when administered at a dose of 20 mg/kg per day.{42389} Sildenafil (0.5 mg/kg) also reduces cardiac arrest and resuscitation-induced increases in angiotensin II (Item No. 17150), angiotensin converting enzyme (ACE), ACE2, and various angiotensin receptors and increases survival in a porcine model of ischemia/reperfusion injury.{42391} Formulations containing sildenafil have been used in the treatment of erectile dysfunction, pulmonary arterial hypertension, and high-altitude pulmonary edema associated with altitude sickness.  

     

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    SKU:10008671 - 50 mg

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  • Sildenafil is a potent inhibitor of phosphodiesterase 5 (PDE5) with IC50 values of 3.6 and 3 nM for PDE5 activity in isolated rabbit platelets and human corpus cavernosum, respectively.{21636} It is selective for PDE5 over PDE1 and PDE3 (IC50s = 0.26 and 65 μM, respectively). Sildenafil reverses glucose-induced decreases in angiopoietin 1 (ANG1) expression and reduction of capillary-like tube formation by mouse dermal endothelial cells in vitro and increases the number of functional blood vessels and regional blood flow in the sciatic nerve in a db/db mouse model of diabetic peripheral neuropathy.{42390} It increases the ratio of maximum intracavernosal pressure to mean arterial blood pressure (ICP/MAP), a measure of erectile function, in castrated rats when administered at a dose of 20 mg/kg per day.{42389} Sildenafil (0.5 mg/kg) also reduces cardiac arrest and resuscitation-induced increases in angiotensin II (Item No. 17150), angiotensin converting enzyme (ACE), ACE2, and various angiotensin receptors and increases survival in a porcine model of ischemia/reperfusion injury.{42391} Formulations containing sildenafil have been used in the treatment of erectile dysfunction, pulmonary arterial hypertension, and high-altitude pulmonary edema associated with altitude sickness.  

     

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  • Sildenafil is a potent inhibitor of phosphodiesterase 5 (PDE5) with IC50 values of 3.6 and 3 nM for PDE5 activity in isolated rabbit platelets and human corpus cavernosum, respectively.{21636} It is selective for PDE5 over PDE1 and PDE3 (IC50s = 0.26 and 65 μM, respectively). Sildenafil reverses glucose-induced decreases in angiopoietin 1 (ANG1) expression and reduction of capillary-like tube formation by mouse dermal endothelial cells in vitro and increases the number of functional blood vessels and regional blood flow in the sciatic nerve in a db/db mouse model of diabetic peripheral neuropathy.{42390} It increases the ratio of maximum intracavernosal pressure to mean arterial blood pressure (ICP/MAP), a measure of erectile function, in castrated rats when administered at a dose of 20 mg/kg per day.{42389} Sildenafil (0.5 mg/kg) also reduces cardiac arrest and resuscitation-induced increases in angiotensin II (Item No. 17150), angiotensin converting enzyme (ACE), ACE2, and various angiotensin receptors and increases survival in a porcine model of ischemia/reperfusion injury.{42391} Formulations containing sildenafil have been used in the treatment of erectile dysfunction, pulmonary arterial hypertension, and high-altitude pulmonary edema associated with altitude sickness.  

     

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  • Sildenafil is a potent inhibitor of phosphodiesterase 5 (PDE5) with IC50 values of 3.6 and 3 nM for PDE5 activity in isolated rabbit platelets and human corpus cavernosum, respectively.{21636} It is selective for PDE5 over PDE1 and PDE3 (IC50s = 0.26 and 65 μM, respectively). Sildenafil reverses glucose-induced decreases in angiopoietin 1 (ANG1) expression and reduction of capillary-like tube formation by mouse dermal endothelial cells in vitro and increases the number of functional blood vessels and regional blood flow in the sciatic nerve in a db/db mouse model of diabetic peripheral neuropathy.{42390} It increases the ratio of maximum intracavernosal pressure to mean arterial blood pressure (ICP/MAP), a measure of erectile function, in castrated rats when administered at a dose of 20 mg/kg per day.{42389} Sildenafil (0.5 mg/kg) also reduces cardiac arrest and resuscitation-induced increases in angiotensin II (Item No. 17150), angiotensin converting enzyme (ACE), ACE2, and various angiotensin receptors and increases survival in a porcine model of ischemia/reperfusion injury.{42391} Formulations containing sildenafil have been used in the treatment of erectile dysfunction, pulmonary arterial hypertension, and high-altitude pulmonary edema associated with altitude sickness.  

     

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  • Sildenafil-d3 is intended for use as an internal standard for the quantification of sildenafil (Item Nos. 10008671 | 14008) by GC- or LC-MS. Sildenafil is a potent inhibitor of phosphodiesterase 5 (PDE5) with IC50 values of 3.6 and 3 nM for PDE5 activity in isolated rabbit platelets and human corpus cavernosum, respectively.{21636} It is selective for PDE5 over PDE1 and PDE3 (IC50s = 0.26 and 65 μM, respectively). Sildenafil reverses glucose-induced decreases in angiopoietin 1 (Ang1) expression and reduction of capillary-like tube formation by mouse dermal endothelial cells in vitro and increases the number of functional blood vessels and regional blood flow in the sciatic nerve in a db/db mouse model of diabetic peripheral neuropathy.{42390} It increases the ratio of maximum intracavernosal pressure to mean arterial blood pressure (ICP/MAP), a measure of erectile function, in castrated rats when administered at a dose of 20 mg/kg per day.{42389} Sildenafil (0.5 mg/kg) also reduces cardiac arrest and resuscitation-induced increases in angiotensin II (Item No. 17150), angiotensin converting enzyme (ACE), ACE2, and various angiotensin receptors and increases survival in a porcine model of ischemia/reperfusion injury.{42391} Formulations containing sildenafil have been used in the treatment of erectile dysfunction, pulmonary arterial hypertension, and high-altitude pulmonary edema associated with altitude sickness.  

     

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  • Sildenafil-d3 is intended for use as an internal standard for the quantification of sildenafil (Item Nos. 10008671 | 14008) by GC- or LC-MS. Sildenafil is a potent inhibitor of phosphodiesterase 5 (PDE5) with IC50 values of 3.6 and 3 nM for PDE5 activity in isolated rabbit platelets and human corpus cavernosum, respectively.{21636} It is selective for PDE5 over PDE1 and PDE3 (IC50s = 0.26 and 65 μM, respectively). Sildenafil reverses glucose-induced decreases in angiopoietin 1 (Ang1) expression and reduction of capillary-like tube formation by mouse dermal endothelial cells in vitro and increases the number of functional blood vessels and regional blood flow in the sciatic nerve in a db/db mouse model of diabetic peripheral neuropathy.{42390} It increases the ratio of maximum intracavernosal pressure to mean arterial blood pressure (ICP/MAP), a measure of erectile function, in castrated rats when administered at a dose of 20 mg/kg per day.{42389} Sildenafil (0.5 mg/kg) also reduces cardiac arrest and resuscitation-induced increases in angiotensin II (Item No. 17150), angiotensin converting enzyme (ACE), ACE2, and various angiotensin receptors and increases survival in a porcine model of ischemia/reperfusion injury.{42391} Formulations containing sildenafil have been used in the treatment of erectile dysfunction, pulmonary arterial hypertension, and high-altitude pulmonary edema associated with altitude sickness.  

     

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  • Silodosin is a potent α1A-adrenoceptor antagonist (Ki = 0.036 nM).{25007,25008} It shows selectivity for the prostatic adrenoceptor.{25007,25005} As a result, it is effective against lower urinary tract symptoms associated with benign prostatic hyperplasia.{25009,25006}  

     

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  • Silodosin is a potent α1A-adrenoceptor antagonist (Ki = 0.036 nM).{25007,25008} It shows selectivity for the prostatic adrenoceptor.{25007,25005} As a result, it is effective against lower urinary tract symptoms associated with benign prostatic hyperplasia.{25009,25006}  

     

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  • Silodosin is a potent α1A-adrenoceptor antagonist (Ki = 0.036 nM).{25007,25008} It shows selectivity for the prostatic adrenoceptor.{25007,25005} As a result, it is effective against lower urinary tract symptoms associated with benign prostatic hyperplasia.{25009,25006}  

     

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  • Silodosin is a potent α1A-adrenoceptor antagonist (Ki = 0.036 nM).{25007,25008} It shows selectivity for the prostatic adrenoceptor.{25007,25005} As a result, it is effective against lower urinary tract symptoms associated with benign prostatic hyperplasia.{25009,25006}  

     

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  • Silodosin glucuronide is an active metabolite of the α1A-adrenergic receptor antagonist silodosin (Item No. 14866).{43909,43910} It is formed from silodosin by the UDP-glucuronosyltransferase (UGT) isoform UGT2B7.{43909} Silodosin glucuronide is toxic to rats with an LD50 value of 0.347 mg/kg.{43910}  

     

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    SKU:28045 - 500 µg

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  • Silodosin-d4 is intended for use as an internal standard for the quantification of silodosin (Item No. 14866) by GC- or LC-MS. Silodosin is an α1A-adrenergic receptor (α1A-AR) antagonist (Ki = 0.036 nM).{25007} It is 583- and 56-fold selective for α1A- over α1B- and α1D-ARs, respectively. Silodosin inhibits phenylephrine-induced contraction of isolated rabbit prostate (pA2 = 10.05) more potently than rabbit or rat aorta (pA2s = 9.36 and 8.13, respectively).{55032} It inhibits norepinephrine-induced contraction of isolated human prostate tissue when used at concentrations ranging from 0.3 to 10 nM.{25007} Silodosin (0.01-1,000 µg/kg) inhibits phenylephrine-induced increases in intraurethral pressure in rats.{25005} Formulations containing silodosin have been used in the treatment of benign prostatic hyperplasia.  

     

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    SKU:30236 - 1 mg

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  • Silybin is the major flavonolignan found in milk thistle (S. marianum).{12584} It inhibits wild mushroom tyrosinase (IC50 = 1.7 μM).{46261} Silybin scavenges superoxide radicals (IC50 = 55.2 μM) and inhibits lipid peroxidation in vitro (IC50 = 73.92 μM).{46262}  

     

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    SKU:10006211 - 1 g

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  • Silybin is the major flavonolignan found in milk thistle (S. marianum).{12584} It inhibits wild mushroom tyrosinase (IC50 = 1.7 μM).{46261} Silybin scavenges superoxide radicals (IC50 = 55.2 μM) and inhibits lipid peroxidation in vitro (IC50 = 73.92 μM).{46262}  

     

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    SKU:10006211 - 10 g

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  • Silybin is the major flavonolignan found in milk thistle (S. marianum).{12584} It inhibits wild mushroom tyrosinase (IC50 = 1.7 μM).{46261} Silybin scavenges superoxide radicals (IC50 = 55.2 μM) and inhibits lipid peroxidation in vitro (IC50 = 73.92 μM).{46262}  

     

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    Cayman
    SKU:10006211 - 5 g

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  • Silybin is the major flavonolignan found in milk thistle (S. marianum).{12584} It inhibits wild mushroom tyrosinase (IC50 = 1.7 μM).{46261} Silybin scavenges superoxide radicals (IC50 = 55.2 μM) and inhibits lipid peroxidation in vitro (IC50 = 73.92 μM).{46262}  

     

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    Cayman
    SKU:10006211 - 50 g

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  • Simeprevir is an orally bioavailable and potent inhibitor of the hepatitis C virus (HCV) nonstructural protein 3/4A (NS3/4A) protease (Ki = 0.36 nM), a serine protease essential for HCV replication.{38234} It inhibits HCV viral replication with an EC50 value of 7.8 nM in Huh7 replicon cells using a luciferase-based assay. Simeprevir is effective against the HCV genotypes 1a and 1b in biochemical assays.{38233} In Huh7 replicon cells, it is synergistically effective when used in combination with IFN-α or NM-107 and has an additive effect when used with ribavirin (Item No. 16757). Formulations containing simeprevir have been used, alone or in combination with pegylated IFN-α and ribavirin, for the treatment of HCV.  

     

    Brand:
    Cayman
    SKU:22144 -

    Out of stock

  • Simeprevir is an orally bioavailable and potent inhibitor of the hepatitis C virus (HCV) nonstructural protein 3/4A (NS3/4A) protease (Ki = 0.36 nM), a serine protease essential for HCV replication.{38234} It inhibits HCV viral replication with an EC50 value of 7.8 nM in Huh7 replicon cells using a luciferase-based assay. Simeprevir is effective against the HCV genotypes 1a and 1b in biochemical assays.{38233} In Huh7 replicon cells, it is synergistically effective when used in combination with IFN-α or NM-107 and has an additive effect when used with ribavirin (Item No. 16757). Formulations containing simeprevir have been used, alone or in combination with pegylated IFN-α and ribavirin, for the treatment of HCV.  

     

    Brand:
    Cayman
    SKU:22144 -

    Out of stock

  • Simeprevir is an orally bioavailable and potent inhibitor of the hepatitis C virus (HCV) nonstructural protein 3/4A (NS3/4A) protease (Ki = 0.36 nM), a serine protease essential for HCV replication.{38234} It inhibits HCV viral replication with an EC50 value of 7.8 nM in Huh7 replicon cells using a luciferase-based assay. Simeprevir is effective against the HCV genotypes 1a and 1b in biochemical assays.{38233} In Huh7 replicon cells, it is synergistically effective when used in combination with IFN-α or NM-107 and has an additive effect when used with ribavirin (Item No. 16757). Formulations containing simeprevir have been used, alone or in combination with pegylated IFN-α and ribavirin, for the treatment of HCV.  

     

    Brand:
    Cayman
    SKU:22144 -

    Out of stock

  • Simeprevir is an orally bioavailable and potent inhibitor of the hepatitis C virus (HCV) nonstructural protein 3/4A (NS3/4A) protease (Ki = 0.36 nM), a serine protease essential for HCV replication.{38234} It inhibits HCV viral replication with an EC50 value of 7.8 nM in Huh7 replicon cells using a luciferase-based assay. Simeprevir is effective against the HCV genotypes 1a and 1b in biochemical assays.{38233} In Huh7 replicon cells, it is synergistically effective when used in combination with IFN-α or NM-107 and has an additive effect when used with ribavirin (Item No. 16757). Formulations containing simeprevir have been used, alone or in combination with pegylated IFN-α and ribavirin, for the treatment of HCV.  

     

    Brand:
    Cayman
    SKU:22144 -

    Out of stock

  • Simetryn is a triazine herbicide that is primarily used to control broad-leaved weeds and grass in paddy rice and other crops.{34066} It is absorbed through roots and foliage and inhibits photosynthesis.{34063} Like other triazine herbicides, simetryn is characterized by high persistence and toxicity.{34066,34067}  

     

    Brand:
    Cayman
    SKU:20392 -

    Available on backorder

  • Simvastatin is a competitive inhibitor of HMG-CoA reductase with a Ki value of 0.12 nM for the hydrolyzed, open ring form of the molecule.{15312} After 18 days of treatment with simvastatin in dogs at a dose of 8 mg/kg/day, plasma cholesterol levels were reduced by 33%.{15310} Simvastatin also suppresses TNF-induced NF-κB activation (IC50 ~ 13 µM), which potentiates apoptosis in human myeloid leukemia cells and thus may be useful in treating cancer.{15363} Clinical formulations containing simvastatin are used in combination with ezetimibe to treat dyslipidemia.  

     

    Brand:
    Cayman
    SKU:10010344 - 100 mg

    Available on backorder

  • Simvastatin is a competitive inhibitor of HMG-CoA reductase with a Ki value of 0.12 nM for the hydrolyzed, open ring form of the molecule.{15312} After 18 days of treatment with simvastatin in dogs at a dose of 8 mg/kg/day, plasma cholesterol levels were reduced by 33%.{15310} Simvastatin also suppresses TNF-induced NF-κB activation (IC50 ~ 13 µM), which potentiates apoptosis in human myeloid leukemia cells and thus may be useful in treating cancer.{15363} Clinical formulations containing simvastatin are used in combination with ezetimibe to treat dyslipidemia.  

     

    Brand:
    Cayman
    SKU:10010344 - 25 mg

    Available on backorder

  • Simvastatin is a competitive inhibitor of HMG-CoA reductase with a Ki value of 0.12 nM for the hydrolyzed, open ring form of the molecule.{15312} After 18 days of treatment with simvastatin in dogs at a dose of 8 mg/kg/day, plasma cholesterol levels were reduced by 33%.{15310} Simvastatin also suppresses TNF-induced NF-κB activation (IC50 ~ 13 µM), which potentiates apoptosis in human myeloid leukemia cells and thus may be useful in treating cancer.{15363} Clinical formulations containing simvastatin are used in combination with ezetimibe to treat dyslipidemia.  

     

    Brand:
    Cayman
    SKU:10010344 - 5 mg

    Available on backorder

  • Simvastatin is a competitive inhibitor of HMG-CoA reductase with a Ki value of 0.12 nM for the hydrolyzed, open ring form of the molecule.{15312} After 18 days of treatment with simvastatin in dogs at a dose of 8 mg/kg/day, plasma cholesterol levels were reduced by 33%.{15310} Simvastatin also suppresses TNF-induced NF-κB activation (IC50 ~ 13 µM), which potentiates apoptosis in human myeloid leukemia cells and thus may be useful in treating cancer.{15363} Clinical formulations containing simvastatin are used in combination with ezetimibe to treat dyslipidemia.  

     

    Brand:
    Cayman
    SKU:10010344 - 50 mg

    Available on backorder

  • Simvastatin is a competitive inhibitor of HMG-CoA reductase with a Ki value of 0.12 nM for the hydrolyzed, open ring form of the molecule.{15312} After 18 days of treatment with simvastatin in dogs at a dose of 8 mg/kg/day, plasma cholesterol levels were reduced by 33%.{15310} Simvastatin also suppresses TNF-induced NF-κB activation (IC50 ~ 13 µM), which potentiates apoptosis in human myeloid leukemia cells and thus may be useful in treating cancer.{15363} Clinical formulations containing simvastatin are used in combination with ezetimibe to treat dyslipidemia.  

     

    Brand:
    Cayman
    SKU:10010345 - 1 mg

    Available on backorder

  • Simvastatin is a competitive inhibitor of HMG-CoA reductase with a Ki value of 0.12 nM for the hydrolyzed, open ring form of the molecule.{15312} After 18 days of treatment with simvastatin in dogs at a dose of 8 mg/kg/day, plasma cholesterol levels were reduced by 33%.{15310} Simvastatin also suppresses TNF-induced NF-κB activation (IC50 ~ 13 µM), which potentiates apoptosis in human myeloid leukemia cells and thus may be useful in treating cancer.{15363} Clinical formulations containing simvastatin are used in combination with ezetimibe to treat dyslipidemia.  

     

    Brand:
    Cayman
    SKU:10010345 - 10 mg

    Available on backorder

  • Simvastatin is a competitive inhibitor of HMG-CoA reductase with a Ki value of 0.12 nM for the hydrolyzed, open ring form of the molecule.{15312} After 18 days of treatment with simvastatin in dogs at a dose of 8 mg/kg/day, plasma cholesterol levels were reduced by 33%.{15310} Simvastatin also suppresses TNF-induced NF-κB activation (IC50 ~ 13 µM), which potentiates apoptosis in human myeloid leukemia cells and thus may be useful in treating cancer.{15363} Clinical formulations containing simvastatin are used in combination with ezetimibe to treat dyslipidemia.  

     

    Brand:
    Cayman
    SKU:10010345 - 25 mg

    Available on backorder

  • Simvastatin is a competitive inhibitor of HMG-CoA reductase with a Ki value of 0.12 nM for the hydrolyzed, open ring form of the molecule.{15312} After 18 days of treatment with simvastatin in dogs at a dose of 8 mg/kg/day, plasma cholesterol levels were reduced by 33%.{15310} Simvastatin also suppresses TNF-induced NF-κB activation (IC50 ~ 13 µM), which potentiates apoptosis in human myeloid leukemia cells and thus may be useful in treating cancer.{15363} Clinical formulations containing simvastatin are used in combination with ezetimibe to treat dyslipidemia.  

     

    Brand:
    Cayman
    SKU:10010345 - 5 mg

    Available on backorder

  • Simvastatin-d6 contains six deuterium atoms located on the methyl groups. It is intended for use as an internal standard for the quantification of simvastatin (Item No. 10010344) by GC- or LC-MS. Simvastatin is a competitive inhibitor of HMG-CoA reductase with a Ki value of 0.12 nM for the hydrolyzed, open ring form of the molecule.{15312} After 18 days of treatment with simvastatin in dogs at a dose of 8 mg/kg per day, plasma cholesterol levels were reduced by 33%.{15310} Simvastatin also suppresses TNF-induced NF-κB activation (IC50 ~ 13 µM), which potentiates apoptosis in human myeloid leukemia cells and thus may be useful in treating cancer.{15363}  

     

    Brand:
    Cayman
    SKU:22181 -

    Out of stock

  • Simvastatin-d6 contains six deuterium atoms located on the methyl groups. It is intended for use as an internal standard for the quantification of simvastatin (Item No. 10010344) by GC- or LC-MS. Simvastatin is a competitive inhibitor of HMG-CoA reductase with a Ki value of 0.12 nM for the hydrolyzed, open ring form of the molecule.{15312} After 18 days of treatment with simvastatin in dogs at a dose of 8 mg/kg per day, plasma cholesterol levels were reduced by 33%.{15310} Simvastatin also suppresses TNF-induced NF-κB activation (IC50 ~ 13 µM), which potentiates apoptosis in human myeloid leukemia cells and thus may be useful in treating cancer.{15363}  

     

    Brand:
    Cayman
    SKU:22181 -

    Out of stock

  • Simvastatin-d6 contains six deuterium atoms located on the methyl groups. It is intended for use as an internal standard for the quantification of simvastatin (Item No. 10010344) by GC- or LC-MS. Simvastatin is a competitive inhibitor of HMG-CoA reductase with a Ki value of 0.12 nM for the hydrolyzed, open ring form of the molecule.{15312} After 18 days of treatment with simvastatin in dogs at a dose of 8 mg/kg per day, plasma cholesterol levels were reduced by 33%.{15310} Simvastatin also suppresses TNF-induced NF-κB activation (IC50 ~ 13 µM), which potentiates apoptosis in human myeloid leukemia cells and thus may be useful in treating cancer.{15363}  

     

    Brand:
    Cayman
    SKU:22181 -

    Out of stock

  • Simvastatin-d6 contains six deuterium atoms located on the methyl groups. It is intended for use as an internal standard for the quantification of simvastatin (Item No. 10010344) by GC- or LC-MS. Simvastatin is a competitive inhibitor of HMG-CoA reductase with a Ki value of 0.12 nM for the hydrolyzed, open ring form of the molecule.{15312} After 18 days of treatment with simvastatin in dogs at a dose of 8 mg/kg per day, plasma cholesterol levels were reduced by 33%.{15310} Simvastatin also suppresses TNF-induced NF-κB activation (IC50 ~ 13 µM), which potentiates apoptosis in human myeloid leukemia cells and thus may be useful in treating cancer.{15363}  

     

    Brand:
    Cayman
    SKU:22181 -

    Out of stock

  • As the active metabolite of molsidomine, SIN-1 (chloride) is a potent vasorelaxant and inhibitor of platelet aggregation. It produces both NO and superoxide and can therefore be used to generate peroxynitrite under physiological conditions.{3222,6435,4159}  

     

    Brand:
    Cayman
    SKU:82220 - 10 mg

    Available on backorder

  • As the active metabolite of molsidomine, SIN-1 (chloride) is a potent vasorelaxant and inhibitor of platelet aggregation. It produces both NO and superoxide and can therefore be used to generate peroxynitrite under physiological conditions.{3222,6435,4159}  

     

    Brand:
    Cayman
    SKU:82220 - 100 mg

    Available on backorder

  • As the active metabolite of molsidomine, SIN-1 (chloride) is a potent vasorelaxant and inhibitor of platelet aggregation. It produces both NO and superoxide and can therefore be used to generate peroxynitrite under physiological conditions.{3222,6435,4159}  

     

    Brand:
    Cayman
    SKU:82220 - 50 mg

    Available on backorder

  • As the active metabolite of molsidomine, SIN-1 (chloride) is a potent vasorelaxant and inhibitor of platelet aggregation. It produces both NO and superoxide and can therefore be used to generate peroxynitrite under physiological conditions.{3222,6435,4159}  

     

    Brand:
    Cayman
    SKU:82220 - 500 mg

    Available on backorder

  • Sinapic acid is a phenylpropanoid hydroxycinnamic acid with diverse biological activities.{39903} Sinapic acid inhibits collagen-induced human platelet aggregation by up to 70% in vitro (IC50 = 1.03 mM).{39905} It scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) and 2,2′-azino-bis-(3-ethylbenzothiazoline-6-sulfonate) (ABTS) free radicals with IC50 values of 8.3 and 5.4 μg/ml, respectively.{30137} Sinapic acid (200 μM) reduces colony formation of SW480 human colon carcinoma cells by 4-fold.{39906} It also inhibits colony formation of E. coli, S. enteritidis, and S. aureus on agar (MICs = 2.2, 2, and 1.8 mM, respectively).{39907} In vivo, sinapic acid (4 mg/kg, p.o.) increases the time spent in the open arms of the elevated plus maze by approximately 15% in mice, an effect that can be blocked by the GABAA receptor antagonists flumazenil (Item No. 14252) and bicuculline (Item No. 11727).{39903} Sinapic acid is also commonly used as a matrix in protein mass spectrometry.{39904}  

     

    Brand:
    Cayman
    SKU:25457 - 1 g

    Available on backorder

  • Sinapic acid is a phenylpropanoid hydroxycinnamic acid with diverse biological activities.{39903} Sinapic acid inhibits collagen-induced human platelet aggregation by up to 70% in vitro (IC50 = 1.03 mM).{39905} It scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) and 2,2′-azino-bis-(3-ethylbenzothiazoline-6-sulfonate) (ABTS) free radicals with IC50 values of 8.3 and 5.4 μg/ml, respectively.{30137} Sinapic acid (200 μM) reduces colony formation of SW480 human colon carcinoma cells by 4-fold.{39906} It also inhibits colony formation of E. coli, S. enteritidis, and S. aureus on agar (MICs = 2.2, 2, and 1.8 mM, respectively).{39907} In vivo, sinapic acid (4 mg/kg, p.o.) increases the time spent in the open arms of the elevated plus maze by approximately 15% in mice, an effect that can be blocked by the GABAA receptor antagonists flumazenil (Item No. 14252) and bicuculline (Item No. 11727).{39903} Sinapic acid is also commonly used as a matrix in protein mass spectrometry.{39904}  

     

    Brand:
    Cayman
    SKU:25457 - 10 g

    Available on backorder

  • Sinapic acid is a phenylpropanoid hydroxycinnamic acid with diverse biological activities.{39903} Sinapic acid inhibits collagen-induced human platelet aggregation by up to 70% in vitro (IC50 = 1.03 mM).{39905} It scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) and 2,2′-azino-bis-(3-ethylbenzothiazoline-6-sulfonate) (ABTS) free radicals with IC50 values of 8.3 and 5.4 μg/ml, respectively.{30137} Sinapic acid (200 μM) reduces colony formation of SW480 human colon carcinoma cells by 4-fold.{39906} It also inhibits colony formation of E. coli, S. enteritidis, and S. aureus on agar (MICs = 2.2, 2, and 1.8 mM, respectively).{39907} In vivo, sinapic acid (4 mg/kg, p.o.) increases the time spent in the open arms of the elevated plus maze by approximately 15% in mice, an effect that can be blocked by the GABAA receptor antagonists flumazenil (Item No. 14252) and bicuculline (Item No. 11727).{39903} Sinapic acid is also commonly used as a matrix in protein mass spectrometry.{39904}  

     

    Brand:
    Cayman
    SKU:25457 - 25 g

    Available on backorder

  • Sinapic acid is a phenylpropanoid hydroxycinnamic acid with diverse biological activities.{39903} Sinapic acid inhibits collagen-induced human platelet aggregation by up to 70% in vitro (IC50 = 1.03 mM).{39905} It scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) and 2,2′-azino-bis-(3-ethylbenzothiazoline-6-sulfonate) (ABTS) free radicals with IC50 values of 8.3 and 5.4 μg/ml, respectively.{30137} Sinapic acid (200 μM) reduces colony formation of SW480 human colon carcinoma cells by 4-fold.{39906} It also inhibits colony formation of E. coli, S. enteritidis, and S. aureus on agar (MICs = 2.2, 2, and 1.8 mM, respectively).{39907} In vivo, sinapic acid (4 mg/kg, p.o.) increases the time spent in the open arms of the elevated plus maze by approximately 15% in mice, an effect that can be blocked by the GABAA receptor antagonists flumazenil (Item No. 14252) and bicuculline (Item No. 11727).{39903} Sinapic acid is also commonly used as a matrix in protein mass spectrometry.{39904}  

     

    Brand:
    Cayman
    SKU:25457 - 5 g

    Available on backorder

  • Sinefungin is a nucleoside structurally related to S-adenosylhomocysteine (Item No. 13603) and S-adenosylmethionine (Item No. 13956) that was originally isolated from Streptomyces.{18391,18646} While it has limited use as an antibiotic due to its high in vivo toxicity, sinefungin has proved useful as a non-selective inhibitor of SET domain-containing methyltransferases in the study of epigenetic regulation (IC50 values range from 0.1-20 μM).{16624,18398,24147,18480,19368}  

     

    Brand:
    Cayman
    SKU:-
  • Sinefungin is a nucleoside structurally related to S-adenosylhomocysteine (Item No. 13603) and S-adenosylmethionine (Item No. 13956) that was originally isolated from Streptomyces.{18391,18646} While it has limited use as an antibiotic due to its high in vivo toxicity, sinefungin has proved useful as a non-selective inhibitor of SET domain-containing methyltransferases in the study of epigenetic regulation (IC50 values range from 0.1-20 μM).{16624,18398,24147,18480,19368}  

     

    Brand:
    Cayman
    SKU:-
  • Sinefungin is a nucleoside structurally related to S-adenosylhomocysteine (Item No. 13603) and S-adenosylmethionine (Item No. 13956) that was originally isolated from Streptomyces.{18391,18646} While it has limited use as an antibiotic due to its high in vivo toxicity, sinefungin has proved useful as a non-selective inhibitor of SET domain-containing methyltransferases in the study of epigenetic regulation (IC50 values range from 0.1-20 μM).{16624,18398,24147,18480,19368}  

     

    Brand:
    Cayman
    SKU:-
  • Sinensetin is a polymethoxylated flavone that is present in the Southeast Asian medical plant O. stamineus, as well as in orange oil. It has been shown to enhance adipogenesis and lipolysis by increasing cAMP levels in 3T3-L1 cells.{31727} Sinensetin is also reported to inhibit α-glucosidase and α-amylase activity in vitro, indicating its potential usefulness in the control of glucose absorption.{31728} Additionally, sinensetin has been shown to suppress the expression of genes associated with inflammation by regulating IκBα protein levels in LPS-activated macrophages.{31729}  

     

    Brand:
    Cayman
    SKU:19751 -

    Available on backorder

  • Sinensetin is a polymethoxylated flavone that is present in the Southeast Asian medical plant O. stamineus, as well as in orange oil. It has been shown to enhance adipogenesis and lipolysis by increasing cAMP levels in 3T3-L1 cells.{31727} Sinensetin is also reported to inhibit α-glucosidase and α-amylase activity in vitro, indicating its potential usefulness in the control of glucose absorption.{31728} Additionally, sinensetin has been shown to suppress the expression of genes associated with inflammation by regulating IκBα protein levels in LPS-activated macrophages.{31729}  

     

    Brand:
    Cayman
    SKU:19751 -

    Available on backorder

  • Sinensetin is a polymethoxylated flavone that is present in the Southeast Asian medical plant O. stamineus, as well as in orange oil. It has been shown to enhance adipogenesis and lipolysis by increasing cAMP levels in 3T3-L1 cells.{31727} Sinensetin is also reported to inhibit α-glucosidase and α-amylase activity in vitro, indicating its potential usefulness in the control of glucose absorption.{31728} Additionally, sinensetin has been shown to suppress the expression of genes associated with inflammation by regulating IκBα protein levels in LPS-activated macrophages.{31729}  

     

    Brand:
    Cayman
    SKU:19751 -

    Available on backorder

  • Key Features Specially formulated Single-Use Arachidonic Acid (peroxide free) for use in cell culture or other in vitro experiments Peroxide free and sealed under argon to maintain product integrity Each pack contains 10 single-use ampules (>1 ml fatty acid at 500 µg/ml in ethanol) Single-use arachidonic acid (peroxide free) consists of 10 sealed ampules, each containing >1 ml of ethanolic solution of fatty acid at a concentration of 500 µg/ml. Peroxides were removed by silicic acid chromatography. The headspace in each ampule is purged with argon. Single-use polyunsaturated fatty acids (PUFAs) are intended for analytical and research applications where absence of oxidized adducts is desired. Ampules have been optimized for one-time use. For best results, use promptly after opening. Arachidonic acid (Item No. 90010) is a substrate for the biosynthesis of eicosanoid second messengers. PUFAs, including arachidonic acid, oxidize spontaneously on exposure to room air, yielding a complex mixture of fatty acid peroxides. Oxidation of PUFAs can be particularly problematic in samples stored in capped vials for prolonged periods, even at low temperatures. These single-use ampules are designed to circumvent this issue.  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Key Features Specially formulated Single-Use Docosahexaenoic Acid (peroxide free) for use in cell culture or other in vitro experiments Peroxide free and sealed under argon to maintain product integrity Each pack contains 10 single-use ampules (>1 ml fatty acid at 500 µg/ml in ethanol) Single-use docosahexaenoic acid (peroxide free) consists of 10 sealed ampules, each containing >1 ml of ethanolic solution of fatty acid at a concentration of 500 µg/ml. Peroxides were removed by silicic acid chromatography. The headspace in each ampule is purged with argon. Single-use polyunsaturated fatty acids (PUFAs) are intended for analytical and research applications where absence of oxidized adducts is desired. Ampules have been optimized for one-time use. For best results, use promptly after opening. Docosahexaenoic acid (Item No. 90310) is an essential fatty acid and the most abundant ω-3 fatty acid in neural tissues, especially in the retina and brain. PUFAs, including docosahexaenoic acid, oxidize spontaneously on exposure to room air, yielding a complex mixture of fatty acid peroxides. Oxidation of PUFAs can be particularly problematic in samples stored in capped vials for prolonged periods, even at low temperatures. These single-use ampules are designed to circumvent this issue.  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Key Features Specially formulated Single-Use Eicosapentaenoic Acid (peroxide free) for use in cell culture or other in vitro experiments Peroxide free and sealed under argon to maintain product integrity Each pack contains 10 single-use ampules (>1 ml fatty acid at 500 µg/ml in ethanol) Single-use eicosapentaenoic (peroxide free) consists of 10 sealed ampules, each containing >1 ml of ethanolic solution of fatty acid at a concentration of 500 µg/ml. Peroxides were removed by silicic acid chromatography. The headspace in each ampule is purged with argon. Single-use polyunsaturated fatty acids (PUFAs) are intended for analytical and research applications where absence of oxidized adducts is desired. Ampules have been optimized for one-time use. For best results, use promptly after opening. Eicosapentaenoic acid (Item No. 90110) is an ω-3 fatty acid abundantly available in marine organisms. PUFAs, including eicosapentaenoic acid, oxidize spontaneously on exposure to room air, yielding a complex mixture of fatty acid peroxides. Oxidation of PUFAs can be particularly problematic in samples stored in capped vials for prolonged periods, even at low temperatures. These single-use ampules are designed to circumvent this issue.  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Key Features Specially formulated Single-Use Linoleic Acid (peroxide free) for use in cell culture or other in vitro experiments Peroxide free and sealed under argon to maintain product integrity Each pack contains 10 single-use ampules (>1 ml fatty acid at 500 µg/ml in ethanol) Single-use linoleic acid (peroxide free) consists of 10 sealed ampules, each containing >1 ml of ethanolic solution of fatty acid at a concentration of 500 µg/ml. Peroxides were removed by silicic acid chromatography. The headspace in each ampule is purged with argon. Single-use polyunsaturated fatty acids (PUFAs) are intended for analytical and research applications where absence of oxidized adducts is desired. Ampules have been optimized for one-time use. For best results, use promptly after opening. Linoleic acid (Item No. 90150) is a PUFA that is prevalent in the western diet. PUFAs, including linoleic acid, oxidize spontaneously on exposure to room air, yielding a complex mixture of fatty acid peroxides. Oxidation of PUFAs can be particularly problematic in samples stored in capped vials for prolonged periods, even at low temperatures. These single-use ampules are designed to circumvent this issue.  

     

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    Cayman
    SKU:-

    Available on backorder

  • Sinomenine is a natural plant alkaloid commonly used to alleviate inflammation associated with rheumatoid arthritis.{26557} It activates histamine release, reduces joint stiffness and pain, and alters cytokine generation without producing gastrointestinal adverse events.{26557,26555,26556,26558} Sinomenine also impairs signaling through NF-κB, resulting in immunosuppression as well as reduced inflammation and pain.{26556,26557} It enhances the bioavailability of some compounds, at least in part through an inhibition of drug export by transporters like P-glycoprotein.{26559,26554}  

     

    Brand:
    Cayman
    SKU:-
  • Sinomenine is a natural plant alkaloid commonly used to alleviate inflammation associated with rheumatoid arthritis.{26557} It activates histamine release, reduces joint stiffness and pain, and alters cytokine generation without producing gastrointestinal adverse events.{26557,26555,26556,26558} Sinomenine also impairs signaling through NF-κB, resulting in immunosuppression as well as reduced inflammation and pain.{26556,26557} It enhances the bioavailability of some compounds, at least in part through an inhibition of drug export by transporters like P-glycoprotein.{26559,26554}  

     

    Brand:
    Cayman
    SKU:-
  • Sinomenine is a natural plant alkaloid commonly used to alleviate inflammation associated with rheumatoid arthritis.{26557} It activates histamine release, reduces joint stiffness and pain, and alters cytokine generation without producing gastrointestinal adverse events.{26557,26555,26556,26558} Sinomenine also impairs signaling through NF-κB, resulting in immunosuppression as well as reduced inflammation and pain.{26556,26557} It enhances the bioavailability of some compounds, at least in part through an inhibition of drug export by transporters like P-glycoprotein.{26559,26554}  

     

    Brand:
    Cayman
    SKU:-
  • The mammalian transcription factor forkhead box M1 (FoxM1) is induced during G1 phase, with expression continuing through S phase and mitosis. Siomycin A is a peptide thiazole antibiotic, first isolated from S. sioyaensis, that interacts with the 23S rRNA of bacteria.{24927} It inhibits FoxM1 (IC50 = ~5 μM), preventing the expression of FoxM1-regulated genes, which includes FoxM1 itself.{24928,24931} Through this mechanism, siomycin A prevents proliferation and induces apoptosis in certain types of stem cells as well as cancer cells.{24930,24926,24929}  

     

    Brand:
    Cayman
    SKU:-
  • Siponimod is an orally bioavailable agonist of the sphingosine-1-phosphate (S1P) receptor that is selective for S1P1 and S1P5 over S1P2, S1P3, and S1P4 (EC50s = 0.39, 0.98, >10,000, >1,000, and 750 nM, respectively, in a radioligand binding assay).{41000,41002} Siponimod activation of the S1P1 receptor leads to receptor internalization, similar to the related compound fingolimod (Item No. 11975), and attenuates psychosine-induced demyelination in organotypic cerebellar slice cultures.{41000,41001} Siponimod (0.3 mg/kg/day) reduces experimental autoimmune encephalomyelitis (EAE) symptoms in rats.{41000} Formulations containing siponimod are in clinical trials for secondary progressive multiple sclerosis.  

     

    Brand:
    Cayman
    SKU:22057 -

    Out of stock

  • Siponimod is an orally bioavailable agonist of the sphingosine-1-phosphate (S1P) receptor that is selective for S1P1 and S1P5 over S1P2, S1P3, and S1P4 (EC50s = 0.39, 0.98, >10,000, >1,000, and 750 nM, respectively, in a radioligand binding assay).{41000,41002} Siponimod activation of the S1P1 receptor leads to receptor internalization, similar to the related compound fingolimod (Item No. 11975), and attenuates psychosine-induced demyelination in organotypic cerebellar slice cultures.{41000,41001} Siponimod (0.3 mg/kg/day) reduces experimental autoimmune encephalomyelitis (EAE) symptoms in rats.{41000} Formulations containing siponimod are in clinical trials for secondary progressive multiple sclerosis.  

     

    Brand:
    Cayman
    SKU:22057 -

    Out of stock

  • Siponimod is an orally bioavailable agonist of the sphingosine-1-phosphate (S1P) receptor that is selective for S1P1 and S1P5 over S1P2, S1P3, and S1P4 (EC50s = 0.39, 0.98, >10,000, >1,000, and 750 nM, respectively, in a radioligand binding assay).{41000,41002} Siponimod activation of the S1P1 receptor leads to receptor internalization, similar to the related compound fingolimod (Item No. 11975), and attenuates psychosine-induced demyelination in organotypic cerebellar slice cultures.{41000,41001} Siponimod (0.3 mg/kg/day) reduces experimental autoimmune encephalomyelitis (EAE) symptoms in rats.{41000} Formulations containing siponimod are in clinical trials for secondary progressive multiple sclerosis.  

     

    Brand:
    Cayman
    SKU:22057 -

    Out of stock

  • Siponimod is an orally bioavailable agonist of the sphingosine-1-phosphate (S1P) receptor that is selective for S1P1 and S1P5 over S1P2, S1P3, and S1P4 (EC50s = 0.39, 0.98, >10,000, >1,000, and 750 nM, respectively, in a radioligand binding assay).{41000,41002} Siponimod activation of the S1P1 receptor leads to receptor internalization, similar to the related compound fingolimod (Item No. 11975), and attenuates psychosine-induced demyelination in organotypic cerebellar slice cultures.{41000,41001} Siponimod (0.3 mg/kg/day) reduces experimental autoimmune encephalomyelitis (EAE) symptoms in rats.{41000} Formulations containing siponimod are in clinical trials for secondary progressive multiple sclerosis.  

     

    Brand:
    Cayman
    SKU:22057 -

    Out of stock

  • Siramesine is an agonist of the sigma-2 (σ2) receptor (IC50 = 0.19 nM).{34005} It is selective for σ2 over σ1 (IC50 = 17 nM) and related receptors and transporters.{34005} Siramesine is anxiolytic without inducing sedation or impairing motor coordination in animal studies.{34005} It is known to induce the death of cancer cells in vitro by destabilizing lysosomes, although it has also been shown to destabilize mitochondria and, with lapatinib (Item No. 11493), induce ferroptosis.{34002,34003,34004}  

     

    Brand:
    Cayman
    SKU:21817 -

    Out of stock

  • Siramesine is an agonist of the sigma-2 (σ2) receptor (IC50 = 0.19 nM).{34005} It is selective for σ2 over σ1 (IC50 = 17 nM) and related receptors and transporters.{34005} Siramesine is anxiolytic without inducing sedation or impairing motor coordination in animal studies.{34005} It is known to induce the death of cancer cells in vitro by destabilizing lysosomes, although it has also been shown to destabilize mitochondria and, with lapatinib (Item No. 11493), induce ferroptosis.{34002,34003,34004}  

     

    Brand:
    Cayman
    SKU:21817 -

    Out of stock

  • Siramesine is an agonist of the sigma-2 (σ2) receptor (IC50 = 0.19 nM).{34005} It is selective for σ2 over σ1 (IC50 = 17 nM) and related receptors and transporters.{34005} Siramesine is anxiolytic without inducing sedation or impairing motor coordination in animal studies.{34005} It is known to induce the death of cancer cells in vitro by destabilizing lysosomes, although it has also been shown to destabilize mitochondria and, with lapatinib (Item No. 11493), induce ferroptosis.{34002,34003,34004}  

     

    Brand:
    Cayman
    SKU:21817 -

    Out of stock

  • Siramesine is an agonist of the sigma-2 (σ2) receptor (IC50 = 0.19 nM).{34005} It is selective for σ2 over σ1 (IC50 = 17 nM) and related receptors and transporters.{34005} Siramesine is anxiolytic without inducing sedation or impairing motor coordination in animal studies.{34005} It is known to induce the death of cancer cells in vitro by destabilizing lysosomes, although it has also been shown to destabilize mitochondria and, with lapatinib (Item No. 11493), induce ferroptosis.{34002,34003,34004}  

     

    Brand:
    Cayman
    SKU:21817 -

    Out of stock

  • Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). SIRT2 deacetylates histone H4 and α-tubulin and functions as a regulator of cell cycle progression, a determinant of myelination, a modulator of autophagy, and a suppressor of brain inflammation.{17251,17517,17518,21799} SirReal2 is an aminothiazole that acts as a SIRT-rearranging ligand to selectively inhibit SIRT2 (IC50 = 140 nM).{29169} SirReal2 is >1,000-fold more potent at inhibiting the activity of SIRT2 than that of SIRT1 or SIRT3-6.{29169} This compound has been shown to be active in HeLa cells by significantly increasing α-tubulin acetylation.{29169}  

     

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    Cayman
    SKU:-

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  • Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). SIRT2 deacetylates histone H4 and α-tubulin and functions as a regulator of cell cycle progression, a determinant of myelination, a modulator of autophagy, and a suppressor of brain inflammation.{17251,17517,17518,21799} SirReal2 is an aminothiazole that acts as a SIRT-rearranging ligand to selectively inhibit SIRT2 (IC50 = 140 nM).{29169} SirReal2 is >1,000-fold more potent at inhibiting the activity of SIRT2 than that of SIRT1 or SIRT3-6.{29169} This compound has been shown to be active in HeLa cells by significantly increasing α-tubulin acetylation.{29169}  

     

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    Cayman
    SKU:-

    Available on backorder

  • Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). SIRT2 deacetylates histone H4 and α-tubulin and functions as a regulator of cell cycle progression, a determinant of myelination, a modulator of autophagy, and a suppressor of brain inflammation.{17251,17517,17518,21799} SirReal2 is an aminothiazole that acts as a SIRT-rearranging ligand to selectively inhibit SIRT2 (IC50 = 140 nM).{29169} SirReal2 is >1,000-fold more potent at inhibiting the activity of SIRT2 than that of SIRT1 or SIRT3-6.{29169} This compound has been shown to be active in HeLa cells by significantly increasing α-tubulin acetylation.{29169}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). SIRT2 deacetylates histone H4 and α-tubulin and functions as a regulator of cell cycle progression, a determinant of myelination, a modulator of autophagy, and a suppressor of brain inflammation.{17251,17517,17518,21799} SirReal2 is an aminothiazole that acts as a SIRT-rearranging ligand to selectively inhibit SIRT2 (IC50 = 140 nM).{29169} SirReal2 is >1,000-fold more potent at inhibiting the activity of SIRT2 than that of SIRT1 or SIRT3-6.{29169} This compound has been shown to be active in HeLa cells by significantly increasing α-tubulin acetylation.{29169}  

     

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    Cayman
    SKU:-

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  • Brand:
    Cayman
    SKU:10010994 - 1 ea

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  • Brand:
    Cayman
    SKU:10011081 - 1 ea

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  • Brand:
    Cayman
    SKU:10010993 - 1 ea

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  • Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). Human SIRT1 is the homolog of yeast Silent information regulator 2 (Sir2) and has been shown to regulate the activity of the p53 tumor suppressor and inhibit apoptosis. Small molecule activators of SIRT1, such as resveratrol, extend lifespan in yeast and C. elegans in a manner that resembles caloric restriction. However, this activation of SIRT1 is under much debate. It was determined that the in vitro activation of SIRT1 and Sir2 by resveratrol was a substrate-specific event (i.e., the binding of resveratrol to SIRT1 promoted a conformational change that better accommodated the attached coumarin group in the peptide substrate). Additional research needs to be done to further elucidate the mechanism behind SIRT1 activation, as well as, to establish its role in aging, cancer, and neurodegenerative disease. Cayman’s SIRT1 Direct Fluorescent Screening Assay Kit provides a convenient fluorescence-based method for screening SIRT1 inhibitors or activators. The procedure requires only two easy steps, both performed in the same microplate. In the first step, the substrate, which comprises the p53 sequence Arg-His-Lys-Lys(e-acetyl)-AMC, is incubated with human recombinant SIRT1 along with its cosubstrate NAD+. Deacetylation sensitizes the substrate such that treatment with the developer in the second step releases a fluorescent product. The fluorophore can be easily analyzed using an excitation wavelength of 350-360 nm and an emission wavelength of 450-465 nm.  

     

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    Cayman
    SKU:10010401 - 96 wells

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  • Brand:
    Cayman
    SKU:10011080 - 1 ea

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  • Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). Human SIRT1 is the homolog of yeast Sir2 (Silent information regulator 2) and has been shown to regulate the activity of the p53 tumor suppressor and inhibit apoptosis. Small molecule activators of SIRT1, such as resveratrol, extend lifespan in yeast and C. elegans in a manner that resembles caloric restriction. Cayman’s SIRT1 FRET-based Screening Assay Kit provides a convenient fluorescence-based method for screening SIRT1 inhibitors or activators. The procedure requires only two easy steps, both performed in the same microplate. In the first step, the substrate, which is coupled to the fluorophore and quencher, is incubated with human recombinant SIRT1 along with its cosubstrate NAD+. Deacetylation sensitizes the substrate such that treatment with the developer in the second step results in the separation of the quencher and fluorophore. The resulting fluorescence can be easily analyzed using an excitation wavelength of 335-345 nm and emission wavelength of 440-465 nm.  

     

    Brand:
    Cayman
    SKU:10010991 - 96 wells

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  • SIRT1/2 inhibitor IV is a cell-permeable inhibitor of SIRT1 (IC50 = 56 µM) and SIRT2 (IC50 = 59 µM), blocking NAD+-dependent deacetylase activity in a substrate competitive manner.{22839} It less effectively inhibits SIRT5 (IC50 >300 µM) and has no effect on class I and II histone deacetylases.{22839} By inhibiting SIRT1, SIRT1/2 inhibitor IV sensitizes H460 lung cancer cells to etoposide and paclitaxel and enhances etoposide-induced G2 arrest.{22839} It also blocks a SIRT1-dependent hypoxic response in vivo, suppressing HIF-1α protein accumulation as well as EPO and VEGF expression in HepG2 tumors in mice.{22840}  

     

    Brand:
    Cayman
    SKU:-
  • SIRT1/2 inhibitor IV is a cell-permeable inhibitor of SIRT1 (IC50 = 56 µM) and SIRT2 (IC50 = 59 µM), blocking NAD+-dependent deacetylase activity in a substrate competitive manner.{22839} It less effectively inhibits SIRT5 (IC50 >300 µM) and has no effect on class I and II histone deacetylases.{22839} By inhibiting SIRT1, SIRT1/2 inhibitor IV sensitizes H460 lung cancer cells to etoposide and paclitaxel and enhances etoposide-induced G2 arrest.{22839} It also blocks a SIRT1-dependent hypoxic response in vivo, suppressing HIF-1α protein accumulation as well as EPO and VEGF expression in HepG2 tumors in mice.{22840}  

     

    Brand:
    Cayman
    SKU:-
  • SIRT1/2 inhibitor IV is a cell-permeable inhibitor of SIRT1 (IC50 = 56 µM) and SIRT2 (IC50 = 59 µM), blocking NAD+-dependent deacetylase activity in a substrate competitive manner.{22839} It less effectively inhibits SIRT5 (IC50 >300 µM) and has no effect on class I and II histone deacetylases.{22839} By inhibiting SIRT1, SIRT1/2 inhibitor IV sensitizes H460 lung cancer cells to etoposide and paclitaxel and enhances etoposide-induced G2 arrest.{22839} It also blocks a SIRT1-dependent hypoxic response in vivo, suppressing HIF-1α protein accumulation as well as EPO and VEGF expression in HepG2 tumors in mice.{22840}  

     

    Brand:
    Cayman
    SKU:-
  • SIRT1/2 inhibitor IV is a cell-permeable inhibitor of SIRT1 (IC50 = 56 µM) and SIRT2 (IC50 = 59 µM), blocking NAD+-dependent deacetylase activity in a substrate competitive manner.{22839} It less effectively inhibits SIRT5 (IC50 >300 µM) and has no effect on class I and II histone deacetylases.{22839} By inhibiting SIRT1, SIRT1/2 inhibitor IV sensitizes H460 lung cancer cells to etoposide and paclitaxel and enhances etoposide-induced G2 arrest.{22839} It also blocks a SIRT1-dependent hypoxic response in vivo, suppressing HIF-1α protein accumulation as well as EPO and VEGF expression in HepG2 tumors in mice.{22840}  

     

    Brand:
    Cayman
    SKU:-
  • Brand:
    Cayman
    SKU:700282 - 1 ea

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  • Brand:
    Cayman
    SKU:700281 - 1 ea

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  • The sirtuins represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs) that catalyze a reaction coupling lysine deacetylation to the formation of nicotinamide and O-acetyl-ADP-ribose. Cayman’s SIRT2 Direct Fluorescent Screening Assay provides a fluorescence-based method for screening SIRT2 inhibitors or activators. The procedure requires only two easy steps, both performed in the same microplate. In the first step, the substrate, which comprises the p53 sequence Gln-Pro-Lys-Lys(ε-acetyl)-AMC, is incubated with human recombinant SIRT2 along with its cosubstrate NAD+. Deacetylation sensitizes the substrate such that treatment with the Developer in the second step releases a fluorescent product.  

     

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    Cayman
    SKU:700280 - 96 wells

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  • Brand:
    Cayman
    SKU:10012541 - 1 ea

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  • Brand:
    Cayman
    SKU:10012540 - 1 ea

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  • The sirtuins represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs) that catalyze a reaction coupling lysine deacetylation to the formation of nicotinamide and O-acetyl-ADP-ribose. SIRT3 is a mitochondrial protein that plays a role in metabolic regulation and other cellular processes. It is the only human sirtuin with a direct genetic link with longevity. Additional research needs to be done to further elucidate the mechanism behind the involvement of SIRT3 in metabolic dysfunction, aging, cancer, and neurodegenerative disease. Cayman’s SIRT3 Direct Fluorescent Screening Assay Kit provides a convenient fluorescence-based method for screening SIRT3 inhibitors or activators. The procedure requires only two easy steps, both performed in the same microplate. In the first step, the substrate, which comprises the p53 sequence Gln-Pro-Lys-Lys(e-acetyl)-AMC, is incubated with human recombinant SIRT3 along with its cosubstrate NAD+. Deacetylation sensitizes the substrate such that treatment with the developer in the second step releases a fluorescent product. The fluorophore can be analyzed with an excitation wavelength of 350-360 nm and an emission wavelength of 450-465 nm.  

     

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    Cayman
    SKU:10011566 - 96 wells

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  • Antigen: human SIRT7 amino acids 35-51 and 361-377 • Host: rabbit • Cross Reactivity: (+) human SIRT7 • Application(s): WB • SIRT7 is a member of the sirtuin family of proteins, which are able to metabolize NAD+. Reports of histone-activated SIR2-mediated NAD+ metabolism and NAD+-activated SIR2-mediated histone deacetylation suggest a coupled reciprocal activation mechanism involving interactions of SIR2 with NAD+ and the N-ε-acetyl-lysine groups of acetylated histone.  

     

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    SKU:13477- 1 ea

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  • Antigen: human SIRT7 amino acids 35-51 and 361-377 • Host: rabbit • Cross Reactivity: (+) human SIRT7 • Application(s): WB • SIRT7 is a member of the sirtuin family of proteins, which are able to metabolize NAD+. Reports of histone-activated SIR2-mediated NAD+ metabolism and NAD+-activated SIR2-mediated histone deacetylation suggest a coupled reciprocal activation mechanism involving interactions of SIR2 with NAD+ and the N-ε-acetyl-lysine groups of acetylated histone.  

     

    Brand:
    Cayman
    SKU:13477- 1 ea
  • SIRT7 is a member of a famiy of proteins called sirtuins (SIR2-like proteins) and are present in prokaryotes and eukaryotes. All SIR2-like proteins have a sirtuin core domain, which contains a series of sequence motifs conserved in organisms ranging from bacteria to humans. Bacterial, yeast, and mammalian sirtuins are able to metabolize NAD+ and several act as mono-ADP-ribosyltransferases. The enzymatic function of sirtuins is not yet completely understood but recent reports of histone-activated SIR2-mediated NAD+ metabolism and NAD+-activated SIR2-mediated histone deacetylation suggest a possible coupled reciprocal activation mechanism involving interactions of SIR2 with NAD+ and the N-ε-acetyl-lysine groups of acetylated histone.  

     

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    SKU:13477 - 1 ea

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  • Sirtinol is a cell-permeable inhibitor of sirtuin NAD+-dependent deacetylases, inhibiting the yeast sirtuin Sir2p with an IC50 value of 68 μM and the human sirtuins SIRT1 and SIRT2 with IC50 values of 131 and 38 μM, respectively.{15174} It does not alter HDAC1 activity.{15174} Sirtinol inhibits the growth of cancer cells and suppresses inflammatory signaling in human dermal microvascular endothelial cells.{20764,20761,20763} In plants, sirtinol can be metabolized to 2-hydroxy-1-naphthoic acid, which activates auxin signaling and alters plant growth and development.{20765,20762}  

     

    Brand:
    Cayman
    SKU:10523 - 10 mg

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  • Sirtinol is a cell-permeable inhibitor of sirtuin NAD+-dependent deacetylases, inhibiting the yeast sirtuin Sir2p with an IC50 value of 68 μM and the human sirtuins SIRT1 and SIRT2 with IC50 values of 131 and 38 μM, respectively.{15174} It does not alter HDAC1 activity.{15174} Sirtinol inhibits the growth of cancer cells and suppresses inflammatory signaling in human dermal microvascular endothelial cells.{20764,20761,20763} In plants, sirtinol can be metabolized to 2-hydroxy-1-naphthoic acid, which activates auxin signaling and alters plant growth and development.{20765,20762}  

     

    Brand:
    Cayman
    SKU:10523 - 25 mg

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  • Sirtinol is a cell-permeable inhibitor of sirtuin NAD+-dependent deacetylases, inhibiting the yeast sirtuin Sir2p with an IC50 value of 68 μM and the human sirtuins SIRT1 and SIRT2 with IC50 values of 131 and 38 μM, respectively.{15174} It does not alter HDAC1 activity.{15174} Sirtinol inhibits the growth of cancer cells and suppresses inflammatory signaling in human dermal microvascular endothelial cells.{20764,20761,20763} In plants, sirtinol can be metabolized to 2-hydroxy-1-naphthoic acid, which activates auxin signaling and alters plant growth and development.{20765,20762}  

     

    Brand:
    Cayman
    SKU:10523 - 5 mg

    Available on backorder

  • Sirtinol is a cell-permeable inhibitor of sirtuin NAD+-dependent deacetylases, inhibiting the yeast sirtuin Sir2p with an IC50 value of 68 μM and the human sirtuins SIRT1 and SIRT2 with IC50 values of 131 and 38 μM, respectively.{15174} It does not alter HDAC1 activity.{15174} Sirtinol inhibits the growth of cancer cells and suppresses inflammatory signaling in human dermal microvascular endothelial cells.{20764,20761,20763} In plants, sirtinol can be metabolized to 2-hydroxy-1-naphthoic acid, which activates auxin signaling and alters plant growth and development.{20765,20762}  

     

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    Cayman
    SKU:10523 - 50 mg

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  • Sisomicin is a broad-spectrum aminoglycoside antibiotic originally isolated from M. inyoensis.{42272} It is active against Gram-positive and Gram-negative bacteria including B. subtilis, S. aureus, E. coli, and P. aeruginosa among others (MICs = 0.01-0.75 µg/ml) but is less active against P. multocida and V. coli (MICs = 7.5 and 2.4 µg/ml, respectively). Sisomicin is protective against Gram-positive and Gram-negative bacterial infections in mice with 50% protective dose (PD50s) values ranging from 0.5 to 6 mg/kg.  

     

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    Cayman
    SKU:21046 -

    Out of stock

  • Sisomicin is a broad-spectrum aminoglycoside antibiotic originally isolated from M. inyoensis.{42272} It is active against Gram-positive and Gram-negative bacteria including B. subtilis, S. aureus, E. coli, and P. aeruginosa among others (MICs = 0.01-0.75 µg/ml) but is less active against P. multocida and V. coli (MICs = 7.5 and 2.4 µg/ml, respectively). Sisomicin is protective against Gram-positive and Gram-negative bacterial infections in mice with 50% protective dose (PD50s) values ranging from 0.5 to 6 mg/kg.  

     

    Brand:
    Cayman
    SKU:21046 -

    Out of stock

  • Sisomicin is a broad-spectrum aminoglycoside antibiotic originally isolated from M. inyoensis.{42272} It is active against Gram-positive and Gram-negative bacteria including B. subtilis, S. aureus, E. coli, and P. aeruginosa among others (MICs = 0.01-0.75 µg/ml) but is less active against P. multocida and V. coli (MICs = 7.5 and 2.4 µg/ml, respectively). Sisomicin is protective against Gram-positive and Gram-negative bacterial infections in mice with 50% protective dose (PD50s) values ranging from 0.5 to 6 mg/kg.  

     

    Brand:
    Cayman
    SKU:21046 -

    Out of stock

  • Sisomicin is a broad-spectrum aminoglycoside antibiotic originally isolated from M. inyoensis.{42272} It is active against Gram-positive and Gram-negative bacteria including B. subtilis, S. aureus, E. coli, and P. aeruginosa among others (MICs = 0.01-0.75 µg/ml) but is less active against P. multocida and V. coli (MICs = 7.5 and 2.4 µg/ml, respectively). Sisomicin is protective against Gram-positive and Gram-negative bacterial infections in mice with 50% protective dose (PD50s) values ranging from 0.5 to 6 mg/kg.  

     

    Brand:
    Cayman
    SKU:21046 -

    Out of stock

  • Sitaxentan is a potent nonpeptide endothelin A (ETA) receptor antagonist (IC50 = 1.4 nM).{52222} It is selective for ETA over ETB receptors (IC50 = 9,800 nM). Sitaxentan inhibits phosphoinositol hydrolysis induced by endothelin-1 (Item No. 24127) in COS-7 cells (pA2 = 8). In vivo, sitaxentan reduces blood pressure in a rat model of acute hypoxia-induced pulmonary hypertension (ED50 = 0.5 mg/kg). It reduces femoral artery neointimal lesion size in a mouse model of intraluminal injury.{52223} Sitaxentan (15 mg/kg) decreases bronchoalveolar lavage fluid (BALF) pleocytosis, as well as pulmonary collagen deposition and fibrosis, and improves lung mechanics in a mouse model of bleomycin-induced lung injury.{52224} Formulations containing sitaxentan have been used in the treatment of hypertension.  

     

    Brand:
    Cayman
    SKU:29244 - 10 mg

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  • Sitaxentan is a potent nonpeptide endothelin A (ETA) receptor antagonist (IC50 = 1.4 nM).{52222} It is selective for ETA over ETB receptors (IC50 = 9,800 nM). Sitaxentan inhibits phosphoinositol hydrolysis induced by endothelin-1 (Item No. 24127) in COS-7 cells (pA2 = 8). In vivo, sitaxentan reduces blood pressure in a rat model of acute hypoxia-induced pulmonary hypertension (ED50 = 0.5 mg/kg). It reduces femoral artery neointimal lesion size in a mouse model of intraluminal injury.{52223} Sitaxentan (15 mg/kg) decreases bronchoalveolar lavage fluid (BALF) pleocytosis, as well as pulmonary collagen deposition and fibrosis, and improves lung mechanics in a mouse model of bleomycin-induced lung injury.{52224} Formulations containing sitaxentan have been used in the treatment of hypertension.  

     

    Brand:
    Cayman
    SKU:29244 - 100 mg

    Available on backorder

  • Sitaxentan is a potent nonpeptide endothelin A (ETA) receptor antagonist (IC50 = 1.4 nM).{52222} It is selective for ETA over ETB receptors (IC50 = 9,800 nM). Sitaxentan inhibits phosphoinositol hydrolysis induced by endothelin-1 (Item No. 24127) in COS-7 cells (pA2 = 8). In vivo, sitaxentan reduces blood pressure in a rat model of acute hypoxia-induced pulmonary hypertension (ED50 = 0.5 mg/kg). It reduces femoral artery neointimal lesion size in a mouse model of intraluminal injury.{52223} Sitaxentan (15 mg/kg) decreases bronchoalveolar lavage fluid (BALF) pleocytosis, as well as pulmonary collagen deposition and fibrosis, and improves lung mechanics in a mouse model of bleomycin-induced lung injury.{52224} Formulations containing sitaxentan have been used in the treatment of hypertension.  

     

    Brand:
    Cayman
    SKU:29244 - 25 mg

    Available on backorder

  • Sitaxentan is a potent nonpeptide endothelin A (ETA) receptor antagonist (IC50 = 1.4 nM).{52222} It is selective for ETA over ETB receptors (IC50 = 9,800 nM). Sitaxentan inhibits phosphoinositol hydrolysis induced by endothelin-1 (Item No. 24127) in COS-7 cells (pA2 = 8). In vivo, sitaxentan reduces blood pressure in a rat model of acute hypoxia-induced pulmonary hypertension (ED50 = 0.5 mg/kg). It reduces femoral artery neointimal lesion size in a mouse model of intraluminal injury.{52223} Sitaxentan (15 mg/kg) decreases bronchoalveolar lavage fluid (BALF) pleocytosis, as well as pulmonary collagen deposition and fibrosis, and improves lung mechanics in a mouse model of bleomycin-induced lung injury.{52224} Formulations containing sitaxentan have been used in the treatment of hypertension.  

     

    Brand:
    Cayman
    SKU:29244 - 5 mg

    Available on backorder

  • Sitostanol is a saturated sterol found in a variety of plants, including corn, wheat, and rice.{37799} It reduces cholesterol uptake in isolated rat jejunal loops when used at a concentration of 0.3 mM in a micellar solution containing cholesterol.{48000} Sitostanol decreases liver cholesterol levels and prevents abdominal aorta atheroma in rabbits when administered in a cholesterol-containing diet at 0.5%.{48001}  

     

    Brand:
    Cayman
    SKU:26094 - 1 mg

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  • Sitostanol is a saturated sterol found in a variety of plants, including corn, wheat, and rice.{37799} It reduces cholesterol uptake in isolated rat jejunal loops when used at a concentration of 0.3 mM in a micellar solution containing cholesterol.{48000} Sitostanol decreases liver cholesterol levels and prevents abdominal aorta atheroma in rabbits when administered in a cholesterol-containing diet at 0.5%.{48001}  

     

    Brand:
    Cayman
    SKU:26094 - 10 mg

    Available on backorder

  • Sitostanol is a saturated sterol found in a variety of plants, including corn, wheat, and rice.{37799} It reduces cholesterol uptake in isolated rat jejunal loops when used at a concentration of 0.3 mM in a micellar solution containing cholesterol.{48000} Sitostanol decreases liver cholesterol levels and prevents abdominal aorta atheroma in rabbits when administered in a cholesterol-containing diet at 0.5%.{48001}  

     

    Brand:
    Cayman
    SKU:26094 - 25 mg

    Available on backorder

  • Sitostanol is a saturated sterol found in a variety of plants, including corn, wheat, and rice.{37799} It reduces cholesterol uptake in isolated rat jejunal loops when used at a concentration of 0.3 mM in a micellar solution containing cholesterol.{48000} Sitostanol decreases liver cholesterol levels and prevents abdominal aorta atheroma in rabbits when administered in a cholesterol-containing diet at 0.5%.{48001}  

     

    Brand:
    Cayman
    SKU:26094 - 5 mg

    Available on backorder

  • Sitravatinib is a multi-kinase inhibitor.{53144} It inhibits 35 kinases (IC50s = 0.5-5,550 nM) in a panel of 55 receptor tyrosine kinases (RTKs). Sitravatinib reduces proliferation of A-673, LPS141, MPNST, DDLS, and Saos-2 cancer cells (IC50s = 1,750, 340.1, 705.7, 266, and 1,830 nM, respectively) and decreases phosphorylation of insulin-like growth factor 1 receptor (IGF1-R), PDGFRβ, and Akt in these same cells when used at concentrations ranging from 62.5 to 4,000 nM. It decreases tumor growth in LPS141 and MPNST mouse xenograft models when administered at a dose of 15 mg/kg per day.  

     

    Brand:
    Cayman
    SKU:27338 - 10 mg

    Available on backorder

  • Sitravatinib is a multi-kinase inhibitor.{53144} It inhibits 35 kinases (IC50s = 0.5-5,550 nM) in a panel of 55 receptor tyrosine kinases (RTKs). Sitravatinib reduces proliferation of A-673, LPS141, MPNST, DDLS, and Saos-2 cancer cells (IC50s = 1,750, 340.1, 705.7, 266, and 1,830 nM, respectively) and decreases phosphorylation of insulin-like growth factor 1 receptor (IGF1-R), PDGFRβ, and Akt in these same cells when used at concentrations ranging from 62.5 to 4,000 nM. It decreases tumor growth in LPS141 and MPNST mouse xenograft models when administered at a dose of 15 mg/kg per day.  

     

    Brand:
    Cayman
    SKU:27338 - 25 mg

    Available on backorder

  • Sitravatinib is a multi-kinase inhibitor.{53144} It inhibits 35 kinases (IC50s = 0.5-5,550 nM) in a panel of 55 receptor tyrosine kinases (RTKs). Sitravatinib reduces proliferation of A-673, LPS141, MPNST, DDLS, and Saos-2 cancer cells (IC50s = 1,750, 340.1, 705.7, 266, and 1,830 nM, respectively) and decreases phosphorylation of insulin-like growth factor 1 receptor (IGF1-R), PDGFRβ, and Akt in these same cells when used at concentrations ranging from 62.5 to 4,000 nM. It decreases tumor growth in LPS141 and MPNST mouse xenograft models when administered at a dose of 15 mg/kg per day.  

     

    Brand:
    Cayman
    SKU:27338 - 5 mg

    Available on backorder

  • Sitravatinib is a multi-kinase inhibitor.{53144} It inhibits 35 kinases (IC50s = 0.5-5,550 nM) in a panel of 55 receptor tyrosine kinases (RTKs). Sitravatinib reduces proliferation of A-673, LPS141, MPNST, DDLS, and Saos-2 cancer cells (IC50s = 1,750, 340.1, 705.7, 266, and 1,830 nM, respectively) and decreases phosphorylation of insulin-like growth factor 1 receptor (IGF1-R), PDGFRβ, and Akt in these same cells when used at concentrations ranging from 62.5 to 4,000 nM. It decreases tumor growth in LPS141 and MPNST mouse xenograft models when administered at a dose of 15 mg/kg per day.  

     

    Brand:
    Cayman
    SKU:27338 - 50 mg

    Available on backorder

  • Sivelestat is a potent and selective inhibitor of neutrophil elastase (IC50 = 44 nM).{29354} It is without effect on a panel of related proteases.{29354} Sivelestat is effective in vivo, blocking elastase-dependent acute lung injury induced by intratracheal administration of LPS.{29354,29356} Elastase inhibitors, including sivelestat, have clinical utility in protecting against direct or indirect lung injury, with or without concomitant sepsis.{29353,29355,23600}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Sivelestat is a potent and selective inhibitor of neutrophil elastase (IC50 = 44 nM).{29354} It is without effect on a panel of related proteases.{29354} Sivelestat is effective in vivo, blocking elastase-dependent acute lung injury induced by intratracheal administration of LPS.{29354,29356} Elastase inhibitors, including sivelestat, have clinical utility in protecting against direct or indirect lung injury, with or without concomitant sepsis.{29353,29355,23600}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Sivelestat is a potent and selective inhibitor of neutrophil elastase (IC50 = 44 nM).{29354} It is without effect on a panel of related proteases.{29354} Sivelestat is effective in vivo, blocking elastase-dependent acute lung injury induced by intratracheal administration of LPS.{29354,29356} Elastase inhibitors, including sivelestat, have clinical utility in protecting against direct or indirect lung injury, with or without concomitant sepsis.{29353,29355,23600}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Sivelestat is a potent and selective inhibitor of neutrophil elastase (IC50 = 44 nM).{29354} It is without effect on a panel of related proteases.{29354} Sivelestat is effective in vivo, blocking elastase-dependent acute lung injury induced by intratracheal administration of LPS.{29354,29356} Elastase inhibitors, including sivelestat, have clinical utility in protecting against direct or indirect lung injury, with or without concomitant sepsis.{29353,29355,23600}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • SJ 172550 is an inhibitor of MDMX that disrupts MDMX-p53 peptide interaction with an EC50 value of 4.3 µM.{33300} It forms a covalent, but reversible, cysteine adduct in the MDMX p53-binding domain, locking MDMX into a conformation that prevents binding to p53.{33301} SJ 172550 induces apoptosis, increases p53 target gene expression, and causes p53-dependent cell death in retinoblastoma cells.{33300}  

     

    Brand:
    Cayman
    SKU:19999 -

    Available on backorder

  • SJ 172550 is an inhibitor of MDMX that disrupts MDMX-p53 peptide interaction with an EC50 value of 4.3 µM.{33300} It forms a covalent, but reversible, cysteine adduct in the MDMX p53-binding domain, locking MDMX into a conformation that prevents binding to p53.{33301} SJ 172550 induces apoptosis, increases p53 target gene expression, and causes p53-dependent cell death in retinoblastoma cells.{33300}  

     

    Brand:
    Cayman
    SKU:19999 -

    Available on backorder

  • SJ 172550 is an inhibitor of MDMX that disrupts MDMX-p53 peptide interaction with an EC50 value of 4.3 µM.{33300} It forms a covalent, but reversible, cysteine adduct in the MDMX p53-binding domain, locking MDMX into a conformation that prevents binding to p53.{33301} SJ 172550 induces apoptosis, increases p53 target gene expression, and causes p53-dependent cell death in retinoblastoma cells.{33300}  

     

    Brand:
    Cayman
    SKU:19999 -

    Available on backorder

  • SJ000291942 is a bone morphogenic protein (BMP) signaling activator.{52365} It activates BMP4 in C33A-2D2 human cervical carcinoma clonal reporter cells (EC50 = ≤1 µM). SJ000291942 (0.1-50 µM) induces ventralization, as well as increases expression of the BMP target genes bmp2b and szl and the cooperatively-induced BMP target genes vent and vox in zebrafish embryos. It also induces BMP-dependent osteoblastic differentiation of C2C12 murine myoblasts.  

     

    Brand:
    Cayman
    SKU:29904 - 10 mg

    Available on backorder

  • SJ000291942 is a bone morphogenic protein (BMP) signaling activator.{52365} It activates BMP4 in C33A-2D2 human cervical carcinoma clonal reporter cells (EC50 = ≤1 µM). SJ000291942 (0.1-50 µM) induces ventralization, as well as increases expression of the BMP target genes bmp2b and szl and the cooperatively-induced BMP target genes vent and vox in zebrafish embryos. It also induces BMP-dependent osteoblastic differentiation of C2C12 murine myoblasts.  

     

    Brand:
    Cayman
    SKU:29904 - 25 mg

    Available on backorder

  • SJ000291942 is a bone morphogenic protein (BMP) signaling activator.{52365} It activates BMP4 in C33A-2D2 human cervical carcinoma clonal reporter cells (EC50 = ≤1 µM). SJ000291942 (0.1-50 µM) induces ventralization, as well as increases expression of the BMP target genes bmp2b and szl and the cooperatively-induced BMP target genes vent and vox in zebrafish embryos. It also induces BMP-dependent osteoblastic differentiation of C2C12 murine myoblasts.  

     

    Brand:
    Cayman
    SKU:29904 - 5 mg

    Available on backorder

  • SKA-121 is a positive-gating modulator of intermediate-conductance calcium-activated potassium channels (IKCa1/KCa3.1) with an EC50 value of 109 nM using whole-cell patch-clamp electrophysiology with calcium in the internal solution.{41411} It is selective for KCa3.1 over KCa2.1, KCa2.2 and KCa2.3 (EC50s = 8,700, 6,800, and 4,400 nM, respectively).{41410} It is also selective over KCa1.1 as well as voltage-gated potassium and sodium channels. SKA-121 (1 µM) potentiates calcium-evoked KCa currents by approximately 7-fold using whole-cell patch-clamp electrophysiology, an effect that can be blocked by the KCa3.1 inhibitor TRAM-34 (Item No. 23385).{41411} It also potentiates calcium-evoked and basal KCa currents. In large porcine coronary arteries ex vivo, SKA-121 potentiates bradykinin-induced endothelium-dependent relaxation (EC50 = 7.9 nM). It also lowers mean arterial blood pressure (MAP) by approximately 20 and 25 mm Hg in normo- and hypertensive mice when used at a dose of 100 mg/kg but has no effect on MAP in KCa3.1 knockout mice.{41410}  

     

    Brand:
    Cayman
    SKU:9003088 - 1 mg

    Available on backorder

  • SKA-121 is a positive-gating modulator of intermediate-conductance calcium-activated potassium channels (IKCa1/KCa3.1) with an EC50 value of 109 nM using whole-cell patch-clamp electrophysiology with calcium in the internal solution.{41411} It is selective for KCa3.1 over KCa2.1, KCa2.2 and KCa2.3 (EC50s = 8,700, 6,800, and 4,400 nM, respectively).{41410} It is also selective over KCa1.1 as well as voltage-gated potassium and sodium channels. SKA-121 (1 µM) potentiates calcium-evoked KCa currents by approximately 7-fold using whole-cell patch-clamp electrophysiology, an effect that can be blocked by the KCa3.1 inhibitor TRAM-34 (Item No. 23385).{41411} It also potentiates calcium-evoked and basal KCa currents. In large porcine coronary arteries ex vivo, SKA-121 potentiates bradykinin-induced endothelium-dependent relaxation (EC50 = 7.9 nM). It also lowers mean arterial blood pressure (MAP) by approximately 20 and 25 mm Hg in normo- and hypertensive mice when used at a dose of 100 mg/kg but has no effect on MAP in KCa3.1 knockout mice.{41410}  

     

    Brand:
    Cayman
    SKU:9003088 - 10 mg

    Available on backorder

  • SKA-121 is a positive-gating modulator of intermediate-conductance calcium-activated potassium channels (IKCa1/KCa3.1) with an EC50 value of 109 nM using whole-cell patch-clamp electrophysiology with calcium in the internal solution.{41411} It is selective for KCa3.1 over KCa2.1, KCa2.2 and KCa2.3 (EC50s = 8,700, 6,800, and 4,400 nM, respectively).{41410} It is also selective over KCa1.1 as well as voltage-gated potassium and sodium channels. SKA-121 (1 µM) potentiates calcium-evoked KCa currents by approximately 7-fold using whole-cell patch-clamp electrophysiology, an effect that can be blocked by the KCa3.1 inhibitor TRAM-34 (Item No. 23385).{41411} It also potentiates calcium-evoked and basal KCa currents. In large porcine coronary arteries ex vivo, SKA-121 potentiates bradykinin-induced endothelium-dependent relaxation (EC50 = 7.9 nM). It also lowers mean arterial blood pressure (MAP) by approximately 20 and 25 mm Hg in normo- and hypertensive mice when used at a dose of 100 mg/kg but has no effect on MAP in KCa3.1 knockout mice.{41410}  

     

    Brand:
    Cayman
    SKU:9003088 - 5 mg

    Available on backorder

  • SKA-121 is a positive-gating modulator of intermediate-conductance calcium-activated potassium channels (IKCa1/KCa3.1) with an EC50 value of 109 nM using whole-cell patch-clamp electrophysiology with calcium in the internal solution.{41411} It is selective for KCa3.1 over KCa2.1, KCa2.2 and KCa2.3 (EC50s = 8,700, 6,800, and 4,400 nM, respectively).{41410} It is also selective over KCa1.1 as well as voltage-gated potassium and sodium channels. SKA-121 (1 µM) potentiates calcium-evoked KCa currents by approximately 7-fold using whole-cell patch-clamp electrophysiology, an effect that can be blocked by the KCa3.1 inhibitor TRAM-34 (Item No. 23385).{41411} It also potentiates calcium-evoked and basal KCa currents. In large porcine coronary arteries ex vivo, SKA-121 potentiates bradykinin-induced endothelium-dependent relaxation (EC50 = 7.9 nM). It also lowers mean arterial blood pressure (MAP) by approximately 20 and 25 mm Hg in normo- and hypertensive mice when used at a dose of 100 mg/kg but has no effect on MAP in KCa3.1 knockout mice.{41410}  

     

    Brand:
    Cayman
    SKU:9003088 - 500 µg

    Available on backorder

  • SKA-31 is an activator of the small- and intermediate conductance calcium-activated potassium channels KCa2.1, KCa2.2, KCa2.3, and KCa3.1 (EC50s = 2.9, 1.9, 2.9, and 0.26 µM, respectively, in a patch-clamp assay).{52233} It also blocks the voltage-gated potassium (Kv) channels Kv1.3, Kv1.5, Kv3.1, and Kv3.2 by 10 to 30% and the voltage-gated sodium (Nav) channels Nav1.2, Nav1.4, and Nav1.5 by 9 to 40% in a panel of 13 ion channels when used at a concentration of 25 µM. SKA-31 increases vasodilation induced by acetylcholine (Item No. 23829) in isolated mouse carotid artery (EC50 = 93 nM) and induces relaxation of isolated rat mesenteric artery rings precontracted with phenylephrine (IC50 = 93 nM).{52233,52234} It decreases blood pressure in normotensive and angiotensin II-induced hypertensive mice when administered at a dose of 30 mg/kg.{52233}  

     

    Brand:
    Cayman
    SKU:29690 - 10 mg

    Available on backorder

  • SKA-31 is an activator of the small- and intermediate conductance calcium-activated potassium channels KCa2.1, KCa2.2, KCa2.3, and KCa3.1 (EC50s = 2.9, 1.9, 2.9, and 0.26 µM, respectively, in a patch-clamp assay).{52233} It also blocks the voltage-gated potassium (Kv) channels Kv1.3, Kv1.5, Kv3.1, and Kv3.2 by 10 to 30% and the voltage-gated sodium (Nav) channels Nav1.2, Nav1.4, and Nav1.5 by 9 to 40% in a panel of 13 ion channels when used at a concentration of 25 µM. SKA-31 increases vasodilation induced by acetylcholine (Item No. 23829) in isolated mouse carotid artery (EC50 = 93 nM) and induces relaxation of isolated rat mesenteric artery rings precontracted with phenylephrine (IC50 = 93 nM).{52233,52234} It decreases blood pressure in normotensive and angiotensin II-induced hypertensive mice when administered at a dose of 30 mg/kg.{52233}  

     

    Brand:
    Cayman
    SKU:29690 - 25 mg

    Available on backorder

  • SKA-31 is an activator of the small- and intermediate conductance calcium-activated potassium channels KCa2.1, KCa2.2, KCa2.3, and KCa3.1 (EC50s = 2.9, 1.9, 2.9, and 0.26 µM, respectively, in a patch-clamp assay).{52233} It also blocks the voltage-gated potassium (Kv) channels Kv1.3, Kv1.5, Kv3.1, and Kv3.2 by 10 to 30% and the voltage-gated sodium (Nav) channels Nav1.2, Nav1.4, and Nav1.5 by 9 to 40% in a panel of 13 ion channels when used at a concentration of 25 µM. SKA-31 increases vasodilation induced by acetylcholine (Item No. 23829) in isolated mouse carotid artery (EC50 = 93 nM) and induces relaxation of isolated rat mesenteric artery rings precontracted with phenylephrine (IC50 = 93 nM).{52233,52234} It decreases blood pressure in normotensive and angiotensin II-induced hypertensive mice when administered at a dose of 30 mg/kg.{52233}  

     

    Brand:
    Cayman
    SKU:29690 - 5 mg

    Available on backorder

  • SKA-31 is an activator of the small- and intermediate conductance calcium-activated potassium channels KCa2.1, KCa2.2, KCa2.3, and KCa3.1 (EC50s = 2.9, 1.9, 2.9, and 0.26 µM, respectively, in a patch-clamp assay).{52233} It also blocks the voltage-gated potassium (Kv) channels Kv1.3, Kv1.5, Kv3.1, and Kv3.2 by 10 to 30% and the voltage-gated sodium (Nav) channels Nav1.2, Nav1.4, and Nav1.5 by 9 to 40% in a panel of 13 ion channels when used at a concentration of 25 µM. SKA-31 increases vasodilation induced by acetylcholine (Item No. 23829) in isolated mouse carotid artery (EC50 = 93 nM) and induces relaxation of isolated rat mesenteric artery rings precontracted with phenylephrine (IC50 = 93 nM).{52233,52234} It decreases blood pressure in normotensive and angiotensin II-induced hypertensive mice when administered at a dose of 30 mg/kg.{52233}  

     

    Brand:
    Cayman
    SKU:29690 - 50 mg

    Available on backorder