Cayman
Showing 44101–44250 of 45550 results
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Voriconazole is a triazole antifungal agent and a derivative of fluconazole (Item No. 11594).{48762,48763} It is active against a variety of yeast and fungi, including clinical isolates of A. flavus, A. fumigatus, F. oxysporum, F. solani, C. albicans, and C. neoformans (MICs = C. albicans (MICs = 0.015-8 µg/ml).{48763} It inhibits ergosterol biosynthesis in C. albicans, C. glabrata, A. fumigatus, and A. flavus (IC50s = 0.03-1 µg/ml).{24400} Voriconazole (10 mg/kg twice per day, i.v.) decreases the number of lung colony-forming units (CFUs), reduces alveolar collapse and lung inflammatory cell infiltration and necrosis, and increases survival in a rat model of invasive pulmonary aspergillosis.{48764} Formulations containing voriconazole have been used in the treatment of fungal infections.
Brand:CaymanSKU:- Voriconazole is a triazole antifungal agent and a derivative of fluconazole (Item No. 11594).{48762,48763} It is active against a variety of yeast and fungi, including clinical isolates of A. flavus, A. fumigatus, F. oxysporum, F. solani, C. albicans, and C. neoformans (MICs = C. albicans (MICs = 0.015-8 µg/ml).{48763} It inhibits ergosterol biosynthesis in C. albicans, C. glabrata, A. fumigatus, and A. flavus (IC50s = 0.03-1 µg/ml).{24400} Voriconazole (10 mg/kg twice per day, i.v.) decreases the number of lung colony-forming units (CFUs), reduces alveolar collapse and lung inflammatory cell infiltration and necrosis, and increases survival in a rat model of invasive pulmonary aspergillosis.{48764} Formulations containing voriconazole have been used in the treatment of fungal infections.
Brand:CaymanSKU:- Voriconazole is a triazole antifungal agent and a derivative of fluconazole (Item No. 11594).{48762,48763} It is active against a variety of yeast and fungi, including clinical isolates of A. flavus, A. fumigatus, F. oxysporum, F. solani, C. albicans, and C. neoformans (MICs = C. albicans (MICs = 0.015-8 µg/ml).{48763} It inhibits ergosterol biosynthesis in C. albicans, C. glabrata, A. fumigatus, and A. flavus (IC50s = 0.03-1 µg/ml).{24400} Voriconazole (10 mg/kg twice per day, i.v.) decreases the number of lung colony-forming units (CFUs), reduces alveolar collapse and lung inflammatory cell infiltration and necrosis, and increases survival in a rat model of invasive pulmonary aspergillosis.{48764} Formulations containing voriconazole have been used in the treatment of fungal infections.
Brand:CaymanSKU:-
Voriconazole N-oxide is a major metabolite of the triazole antifungal voriconazole (Item No. 15633).{48321} It is formed via oxidation of voriconazole by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2C19.
Brand:CaymanSKU:28047 - 1 mgAvailable on backorder
Voriconazole N-oxide is a major metabolite of the triazole antifungal voriconazole (Item No. 15633).{48321} It is formed via oxidation of voriconazole by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2C19.
Brand:CaymanSKU:28047 - 10 mgAvailable on backorder
Voriconazole N-oxide is a major metabolite of the triazole antifungal voriconazole (Item No. 15633).{48321} It is formed via oxidation of voriconazole by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2C19.
Brand:CaymanSKU:28047 - 5 mgAvailable on backorder
Vortioxetine is a multimodal serotonergic agent that acts as a serotonin (5-HT; Item No. 14332) reuptake inhibitor (Ki = 1.6 nM) and binds to the 5-HT1A, 5-HT1B, 5-HT3A, and 5-HT7 receptors (Kis = 15, 33, 3.7, and 19 nM, respectively).{36248} It also binds to the β1-adrenergic receptor (Ki = 46 nM). It acts as an antagonist at 5-HT3A and 5-HT7, a partial agonist at 5-HT1B, and a full agonist at 5-HT1A receptors. Vortioxetine is selective for the serotonin transporter (SERT) over the dopamine and norepinephrine transporters (IC50s = 5.3, 890, and 140 nM, respectively). It has affinity for histamine H2, melanocortin 4, β2-adrenergic, 5-HT2C, and 5-HT6 receptors with Ki values greater than 180 nM, but it is selective over the majority of targets in a panel of 75 ion channels, G protein-coupled receptors, enzymes, and transporters. Vortioxetine (5 or 10 mg/kg per day) increases 5-HT levels in vivo in rat brain and decreases occupancy at SERT. At acute and chronic doses of 5 mg/kg, but not 10 mg/kg, it increases the time mice spend in the center of the open field test, increases mobility in the forced swim test, and decreases the latency to feed in the novelty suppressed feeding test.{36249} It also increases proliferation and survival of adult-born granule cells in the hippocampus. Formulations containing vortioxetine have been used in the treatment of major depressive disorder.
Brand:CaymanSKU:30183 - 10 mgAvailable on backorder
Vortioxetine is a multimodal serotonergic agent that acts as a serotonin (5-HT; Item No. 14332) reuptake inhibitor (Ki = 1.6 nM) and binds to the 5-HT1A, 5-HT1B, 5-HT3A, and 5-HT7 receptors (Kis = 15, 33, 3.7, and 19 nM, respectively).{36248} It also binds to the β1-adrenergic receptor (Ki = 46 nM). It acts as an antagonist at 5-HT3A and 5-HT7, a partial agonist at 5-HT1B, and a full agonist at 5-HT1A receptors. Vortioxetine is selective for the serotonin transporter (SERT) over the dopamine and norepinephrine transporters (IC50s = 5.3, 890, and 140 nM, respectively). It has affinity for histamine H2, melanocortin 4, β2-adrenergic, 5-HT2C, and 5-HT6 receptors with Ki values greater than 180 nM, but it is selective over the majority of targets in a panel of 75 ion channels, G protein-coupled receptors, enzymes, and transporters. Vortioxetine (5 or 10 mg/kg per day) increases 5-HT levels in vivo in rat brain and decreases occupancy at SERT. At acute and chronic doses of 5 mg/kg, but not 10 mg/kg, it increases the time mice spend in the center of the open field test, increases mobility in the forced swim test, and decreases the latency to feed in the novelty suppressed feeding test.{36249} It also increases proliferation and survival of adult-born granule cells in the hippocampus. Formulations containing vortioxetine have been used in the treatment of major depressive disorder.
Brand:CaymanSKU:30183 - 25 mgAvailable on backorder
Vortioxetine is a multimodal serotonergic agent that acts as a serotonin (5-HT; Item No. 14332) reuptake inhibitor (Ki = 1.6 nM) and binds to the 5-HT1A, 5-HT1B, 5-HT3A, and 5-HT7 receptors (Kis = 15, 33, 3.7, and 19 nM, respectively).{36248} It also binds to the β1-adrenergic receptor (Ki = 46 nM). It acts as an antagonist at 5-HT3A and 5-HT7, a partial agonist at 5-HT1B, and a full agonist at 5-HT1A receptors. Vortioxetine is selective for the serotonin transporter (SERT) over the dopamine and norepinephrine transporters (IC50s = 5.3, 890, and 140 nM, respectively). It has affinity for histamine H2, melanocortin 4, β2-adrenergic, 5-HT2C, and 5-HT6 receptors with Ki values greater than 180 nM, but it is selective over the majority of targets in a panel of 75 ion channels, G protein-coupled receptors, enzymes, and transporters. Vortioxetine (5 or 10 mg/kg per day) increases 5-HT levels in vivo in rat brain and decreases occupancy at SERT. At acute and chronic doses of 5 mg/kg, but not 10 mg/kg, it increases the time mice spend in the center of the open field test, increases mobility in the forced swim test, and decreases the latency to feed in the novelty suppressed feeding test.{36249} It also increases proliferation and survival of adult-born granule cells in the hippocampus. Formulations containing vortioxetine have been used in the treatment of major depressive disorder.
Brand:CaymanSKU:30183 - 5 mgAvailable on backorder
Vortioxetine is a multimodal serotonergic agent that acts as a serotonin (5-HT; Item No. 14332) reuptake inhibitor (Ki = 1.6 nM) and binds to the 5-HT1A, 5-HT1B, 5-HT3A, and 5-HT7 receptors (Kis = 15, 33, 3.7, and 19 nM, respectively).{36248} It also binds to the β1-adrenergic receptor (Ki = 46 nM). It acts as an antagonist at 5-HT3A and 5-HT7, a partial agonist at 5-HT1B, and a full agonist at 5-HT1A receptors. Vortioxetine is selective for the serotonin transporter (SERT) over the dopamine and norepinephrine transporters (IC50s = 5.3, 890, and 140 nM, respectively). It has affinity for histamine H2, melanocortin 4, β2-adrenergic, 5-HT2C, and 5-HT6 receptors with Ki values greater than 180 nM, but it is selective over the majority of targets in a panel of 75 ion channels, G protein-coupled receptors, enzymes, and transporters. Vortioxetine (5 or 10 mg/kg per day) increases 5-HT levels in vivo in rat brain and decreases occupancy at SERT. At acute and chronic doses of 5 mg/kg, but not 10 mg/kg, it increases the time mice spend in the center of the open field test, increases mobility in the forced swim test, and decreases the latency to feed in the novelty suppressed feeding test.{36249} It also increases proliferation and survival of adult-born granule cells in the hippocampus. Formulations containing vortioxetine have been used in the treatment of major depressive disorder.
Brand:CaymanSKU:30183 - 50 mgAvailable on backorder
Vortioxetine is a multimodal serotonergic agent that acts as a serotonin (5-HT; Item No. 14332) reuptake inhibitor (Ki = 1.6 nM) and binds to the 5-HT1A, 5-HT1B, 5-HT3A, and 5-HT7 receptors (Kis = 15, 33, 3.7, and 19 nM, respectively).{36248} It also binds to the β1-adrenergic receptor (Ki = 46 nM). It acts as an antagonist at 5-HT3A and 5-HT7, a partial agonist at 5-HT1B, and a full agonist at 5-HT1A receptors. Vortioxetine is selective for the serotonin transporter (SERT) over the dopamine and norepinephrine transporters (IC50s = 5.3, 890, and 140 nM, respectively). It has affinity for histamine H2, melanocortin 4, β2-adrenergic, 5-HT2C, and 5-HT6 receptors with Ki values greater than 180 nM, but it is selective over the majority of targets in a panel of 75 ion channels, G protein-coupled receptors, enzymes, and transporters. Vortioxetine (5 or 10 mg/kg per day) increases 5-HT levels in vivo in rat brain and decreases occupancy at SERT. At acute and chronic doses of 5 mg/kg, but not 10 mg/kg, it increases the time mice spend in the center of the open field test, increases mobility in the forced swim test, and decreases the latency to feed in the novelty suppressed feeding test.{36249} It also increases proliferation and survival of adult-born granule cells in the hippocampus. Formulations containing vortioxetine have been used in the treatment of major depressive disorder.
Brand:CaymanSKU:23694 - 1 mgAvailable on backorder
Vortioxetine is a multimodal serotonergic agent that acts as a serotonin (5-HT; Item No. 14332) reuptake inhibitor (Ki = 1.6 nM) and binds to the 5-HT1A, 5-HT1B, 5-HT3A, and 5-HT7 receptors (Kis = 15, 33, 3.7, and 19 nM, respectively).{36248} It also binds to the β1-adrenergic receptor (Ki = 46 nM). It acts as an antagonist at 5-HT3A and 5-HT7, a partial agonist at 5-HT1B, and a full agonist at 5-HT1A receptors. Vortioxetine is selective for the serotonin transporter (SERT) over the dopamine and norepinephrine transporters (IC50s = 5.3, 890, and 140 nM, respectively). It has affinity for histamine H2, melanocortin 4, β2-adrenergic, 5-HT2C, and 5-HT6 receptors with Ki values greater than 180 nM, but it is selective over the majority of targets in a panel of 75 ion channels, G protein-coupled receptors, enzymes, and transporters. Vortioxetine (5 or 10 mg/kg per day) increases 5-HT levels in vivo in rat brain and decreases occupancy at SERT. At acute and chronic doses of 5 mg/kg, but not 10 mg/kg, it increases the time mice spend in the center of the open field test, increases mobility in the forced swim test, and decreases the latency to feed in the novelty suppressed feeding test.{36249} It also increases proliferation and survival of adult-born granule cells in the hippocampus. Formulations containing vortioxetine have been used in the treatment of major depressive disorder.
Brand:CaymanSKU:23694 - 10 mgAvailable on backorder
Vortioxetine is a multimodal serotonergic agent that acts as a serotonin (5-HT; Item No. 14332) reuptake inhibitor (Ki = 1.6 nM) and binds to the 5-HT1A, 5-HT1B, 5-HT3A, and 5-HT7 receptors (Kis = 15, 33, 3.7, and 19 nM, respectively).{36248} It also binds to the β1-adrenergic receptor (Ki = 46 nM). It acts as an antagonist at 5-HT3A and 5-HT7, a partial agonist at 5-HT1B, and a full agonist at 5-HT1A receptors. Vortioxetine is selective for the serotonin transporter (SERT) over the dopamine and norepinephrine transporters (IC50s = 5.3, 890, and 140 nM, respectively). It has affinity for histamine H2, melanocortin 4, β2-adrenergic, 5-HT2C, and 5-HT6 receptors with Ki values greater than 180 nM, but it is selective over the majority of targets in a panel of 75 ion channels, G protein-coupled receptors, enzymes, and transporters. Vortioxetine (5 or 10 mg/kg per day) increases 5-HT levels in vivo in rat brain and decreases occupancy at SERT. At acute and chronic doses of 5 mg/kg, but not 10 mg/kg, it increases the time mice spend in the center of the open field test, increases mobility in the forced swim test, and decreases the latency to feed in the novelty suppressed feeding test.{36249} It also increases proliferation and survival of adult-born granule cells in the hippocampus. Formulations containing vortioxetine have been used in the treatment of major depressive disorder.
Brand:CaymanSKU:23694 - 5 mgAvailable on backorder
Vortioxetine-d8 is intended for use as an internal standard for the quantification of vortioxetine (Item No. 23694) by GC- or LC-MS. Vortioxetine is a multimodal serotonergic agent that acts as a serotonin (5-HT; Item No. 14332) reuptake inhibitor (Ki = 1.6 nM) and binds to the 5-HT1A, 5-HT1B, 5-HT3A, and 5-HT7 receptors (Kis = 15, 33, 3.7, and 19 nM, respectively).{36248} It also binds to the β1-adrenergic receptor (Ki = 46 nM). It acts as an antagonist at 5-HT3A and 5-HT7, a partial agonist at 5-HT1B, and a full agonist at 5-HT1A receptors. Vortioxetine is selective for the serotonin transporter (SERT) over the dopamine and norepinephrine transporters (IC50s = 5.3, 890, and 140 nM, respectively). It has affinity for histamine H2, melanocortin 4, β2-adrenergic, 5-HT2C, and 5-HT6 receptors with Ki values greater than 180 nM, but it is selective over the majority of targets in a panel of 75 ion channels, G protein-coupled receptors, enzymes, and transporters. Vortioxetine (5 or 10 mg/kg per day) increases 5-HT levels in vivo in rat brain and decreases occupancy at SERT. At acute and chronic doses of 5 mg/kg, but not 10 mg/kg, it increases the time mice spend in the center of the open field test, increases mobility in the forced swim test, and decreases the latency to feed in the novelty suppressed feeding test.{36249} It also increases proliferation and survival of adult-born granule cells in the hippocampus. Formulations containing vortioxetine have been used in the treatment of major depressive disorder.
Brand:CaymanSKU:28163 - 1 mgAvailable on backorder
Voruciclib is a pan-inhibitor of cyclin-dependent kinases (CDKs; Kis = 0.626-9.1 nM).{47780} It is selective for CDKs over male germ cell associated kinase (MAK) and intestinal cell kinase (ICK; Kis = 259 and 481 nM, respectively), in a panel of 48 kinases. Voruciclib decreases myeloid cell leukemia-1 (Mcl-1) levels and increases cleaved poly(ADP-ribose) polymerase (PARP) levels in six diffuse large B-cell lymphoma (DLBCL) cell lines when used at concentrations ranging from 0.5 to 5 µM. It reduces tumor growth by 56.3% in a Ri-1 mouse xenograft model when administered at a dose of 200 mg/kg.
Brand:CaymanSKU:29085 - 1 mgAvailable on backorder
Voruciclib is a pan-inhibitor of cyclin-dependent kinases (CDKs; Kis = 0.626-9.1 nM).{47780} It is selective for CDKs over male germ cell associated kinase (MAK) and intestinal cell kinase (ICK; Kis = 259 and 481 nM, respectively), in a panel of 48 kinases. Voruciclib decreases myeloid cell leukemia-1 (Mcl-1) levels and increases cleaved poly(ADP-ribose) polymerase (PARP) levels in six diffuse large B-cell lymphoma (DLBCL) cell lines when used at concentrations ranging from 0.5 to 5 µM. It reduces tumor growth by 56.3% in a Ri-1 mouse xenograft model when administered at a dose of 200 mg/kg.
Brand:CaymanSKU:29085 - 10 mgAvailable on backorder
Voruciclib is a pan-inhibitor of cyclin-dependent kinases (CDKs; Kis = 0.626-9.1 nM).{47780} It is selective for CDKs over male germ cell associated kinase (MAK) and intestinal cell kinase (ICK; Kis = 259 and 481 nM, respectively), in a panel of 48 kinases. Voruciclib decreases myeloid cell leukemia-1 (Mcl-1) levels and increases cleaved poly(ADP-ribose) polymerase (PARP) levels in six diffuse large B-cell lymphoma (DLBCL) cell lines when used at concentrations ranging from 0.5 to 5 µM. It reduces tumor growth by 56.3% in a Ri-1 mouse xenograft model when administered at a dose of 200 mg/kg.
Brand:CaymanSKU:29085 - 5 mgAvailable on backorder
Vosaroxin is an inhibitor of topoisomerase II.{58000} It induces relaxation of supercoiled DNA with an IC50 value of 3.2 µg/ml in a cell-free assay. It induces DNA double-strand breaks in CCRF-CEM cells and cell cycle arrest at the G2 phase in A549 cells in a concentration-dependent manner.{58001} Vosaroxin inhibits proliferation in a panel of 15 cancer cell lines, including cancer cells resistant to doxorubicin (Item No. 15007), etoposide (Item No. 12092), or cisplatin (Item No. 13119), with IC50 values ranging from 0.04 to 1.15 µM.{58002} It inhibits tumor growth in multidrug-resistant SBC-3/ETP or PC-14/CDDP mouse xenograft models when administered at a dose of 20 mg/kg.
Brand:CaymanSKU:30614 - 1 mgAvailable on backorder
Vosaroxin is an inhibitor of topoisomerase II.{58000} It induces relaxation of supercoiled DNA with an IC50 value of 3.2 µg/ml in a cell-free assay. It induces DNA double-strand breaks in CCRF-CEM cells and cell cycle arrest at the G2 phase in A549 cells in a concentration-dependent manner.{58001} Vosaroxin inhibits proliferation in a panel of 15 cancer cell lines, including cancer cells resistant to doxorubicin (Item No. 15007), etoposide (Item No. 12092), or cisplatin (Item No. 13119), with IC50 values ranging from 0.04 to 1.15 µM.{58002} It inhibits tumor growth in multidrug-resistant SBC-3/ETP or PC-14/CDDP mouse xenograft models when administered at a dose of 20 mg/kg.
Brand:CaymanSKU:30614 - 10 mgAvailable on backorder
Vosaroxin is an inhibitor of topoisomerase II.{58000} It induces relaxation of supercoiled DNA with an IC50 value of 3.2 µg/ml in a cell-free assay. It induces DNA double-strand breaks in CCRF-CEM cells and cell cycle arrest at the G2 phase in A549 cells in a concentration-dependent manner.{58001} Vosaroxin inhibits proliferation in a panel of 15 cancer cell lines, including cancer cells resistant to doxorubicin (Item No. 15007), etoposide (Item No. 12092), or cisplatin (Item No. 13119), with IC50 values ranging from 0.04 to 1.15 µM.{58002} It inhibits tumor growth in multidrug-resistant SBC-3/ETP or PC-14/CDDP mouse xenograft models when administered at a dose of 20 mg/kg.
Brand:CaymanSKU:30614 - 25 mgAvailable on backorder
Vosaroxin is an inhibitor of topoisomerase II.{58000} It induces relaxation of supercoiled DNA with an IC50 value of 3.2 µg/ml in a cell-free assay. It induces DNA double-strand breaks in CCRF-CEM cells and cell cycle arrest at the G2 phase in A549 cells in a concentration-dependent manner.{58001} Vosaroxin inhibits proliferation in a panel of 15 cancer cell lines, including cancer cells resistant to doxorubicin (Item No. 15007), etoposide (Item No. 12092), or cisplatin (Item No. 13119), with IC50 values ranging from 0.04 to 1.15 µM.{58002} It inhibits tumor growth in multidrug-resistant SBC-3/ETP or PC-14/CDDP mouse xenograft models when administered at a dose of 20 mg/kg.
Brand:CaymanSKU:30614 - 5 mgAvailable on backorder
Voxtalisib is a dual inhibitor of PI3K and mammalian target of rapamycin complex (mTORC; IC50s = 39, 110, 43, 9, 160, and 910 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, mTORC1, and mTORC2, respectively).{56000} It is selective for these kinases over vacuolar protein sorting 34 (VPS34; IC50 = 9,100 nM) and a panel of 130 additional protein kinases at 1.5 µM but does inhibit DNA protein kinase (DNA-PK; IC50 = 150 nM). Voxtalisib decreases EGF-induced production of PIP3, a product of PI3K-mediated PIP2 metabolism, in PC3 prostate cancer cells with an IC50 value of 290 nM. It also reduces phosphorylation of the PI3K and mTORC targets Akt and ribosomal protein S6 (S6RP) in the same model (IC50s = 250 and 120 nM, respectively). Voxtalisib inhibits proliferation and colony formation of PC3 cells (IC50s = 1,800 and 270 nM, respectively). It reduces tumor growth and increases survival in a GBM-39 glioblastoma multiforme (GBM) mouse xenograft model when administered at a dose of 30 mg/kg twice per day alone or in combination with temozolomide (Item No. 14163).{27545}
Brand:CaymanSKU:30323 - 10 mgAvailable on backorder
Voxtalisib is a dual inhibitor of PI3K and mammalian target of rapamycin complex (mTORC; IC50s = 39, 110, 43, 9, 160, and 910 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, mTORC1, and mTORC2, respectively).{56000} It is selective for these kinases over vacuolar protein sorting 34 (VPS34; IC50 = 9,100 nM) and a panel of 130 additional protein kinases at 1.5 µM but does inhibit DNA protein kinase (DNA-PK; IC50 = 150 nM). Voxtalisib decreases EGF-induced production of PIP3, a product of PI3K-mediated PIP2 metabolism, in PC3 prostate cancer cells with an IC50 value of 290 nM. It also reduces phosphorylation of the PI3K and mTORC targets Akt and ribosomal protein S6 (S6RP) in the same model (IC50s = 250 and 120 nM, respectively). Voxtalisib inhibits proliferation and colony formation of PC3 cells (IC50s = 1,800 and 270 nM, respectively). It reduces tumor growth and increases survival in a GBM-39 glioblastoma multiforme (GBM) mouse xenograft model when administered at a dose of 30 mg/kg twice per day alone or in combination with temozolomide (Item No. 14163).{27545}
Brand:CaymanSKU:30323 - 25 mgAvailable on backorder
Voxtalisib is a dual inhibitor of PI3K and mammalian target of rapamycin complex (mTORC; IC50s = 39, 110, 43, 9, 160, and 910 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, mTORC1, and mTORC2, respectively).{56000} It is selective for these kinases over vacuolar protein sorting 34 (VPS34; IC50 = 9,100 nM) and a panel of 130 additional protein kinases at 1.5 µM but does inhibit DNA protein kinase (DNA-PK; IC50 = 150 nM). Voxtalisib decreases EGF-induced production of PIP3, a product of PI3K-mediated PIP2 metabolism, in PC3 prostate cancer cells with an IC50 value of 290 nM. It also reduces phosphorylation of the PI3K and mTORC targets Akt and ribosomal protein S6 (S6RP) in the same model (IC50s = 250 and 120 nM, respectively). Voxtalisib inhibits proliferation and colony formation of PC3 cells (IC50s = 1,800 and 270 nM, respectively). It reduces tumor growth and increases survival in a GBM-39 glioblastoma multiforme (GBM) mouse xenograft model when administered at a dose of 30 mg/kg twice per day alone or in combination with temozolomide (Item No. 14163).{27545}
Brand:CaymanSKU:30323 - 5 mgAvailable on backorder
Voxtalisib is a dual inhibitor of PI3K and mammalian target of rapamycin complex (mTORC; IC50s = 39, 110, 43, 9, 160, and 910 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, mTORC1, and mTORC2, respectively).{56000} It is selective for these kinases over vacuolar protein sorting 34 (VPS34; IC50 = 9,100 nM) and a panel of 130 additional protein kinases at 1.5 µM but does inhibit DNA protein kinase (DNA-PK; IC50 = 150 nM). Voxtalisib decreases EGF-induced production of PIP3, a product of PI3K-mediated PIP2 metabolism, in PC3 prostate cancer cells with an IC50 value of 290 nM. It also reduces phosphorylation of the PI3K and mTORC targets Akt and ribosomal protein S6 (S6RP) in the same model (IC50s = 250 and 120 nM, respectively). Voxtalisib inhibits proliferation and colony formation of PC3 cells (IC50s = 1,800 and 270 nM, respectively). It reduces tumor growth and increases survival in a GBM-39 glioblastoma multiforme (GBM) mouse xenograft model when administered at a dose of 30 mg/kg twice per day alone or in combination with temozolomide (Item No. 14163).{27545}
Brand:CaymanSKU:30323 - 50 mgAvailable on backorder
Respiratory syncytial virus (RSV) is the leading cause of respiratory tract infections in humans. RSV F protein, which mediates fusion of the viral envelope with the host cell membrane, has become a target of anti-RSV treatment. VP-14637 is a small molecule inhibitor of RSV that demonstrates antiviral activity with an EC50 value of 1.4 nM.{28943,28944} It interferes directly with RSV fusion (EC50 = 5.4 nM), binding to the viral F protein, which allows simultaneous interaction with both of the heptad repeat domains of the F protein trimer.{28943,28944}
Brand:CaymanSKU:-Available on backorder
Respiratory syncytial virus (RSV) is the leading cause of respiratory tract infections in humans. RSV F protein, which mediates fusion of the viral envelope with the host cell membrane, has become a target of anti-RSV treatment. VP-14637 is a small molecule inhibitor of RSV that demonstrates antiviral activity with an EC50 value of 1.4 nM.{28943,28944} It interferes directly with RSV fusion (EC50 = 5.4 nM), binding to the viral F protein, which allows simultaneous interaction with both of the heptad repeat domains of the F protein trimer.{28943,28944}
Brand:CaymanSKU:-Available on backorder
Respiratory syncytial virus (RSV) is the leading cause of respiratory tract infections in humans. RSV F protein, which mediates fusion of the viral envelope with the host cell membrane, has become a target of anti-RSV treatment. VP-14637 is a small molecule inhibitor of RSV that demonstrates antiviral activity with an EC50 value of 1.4 nM.{28943,28944} It interferes directly with RSV fusion (EC50 = 5.4 nM), binding to the viral F protein, which allows simultaneous interaction with both of the heptad repeat domains of the F protein trimer.{28943,28944}
Brand:CaymanSKU:-Available on backorder
Sphingosine-1-phosphate (S1P; Item No. 62570) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis.{11895,12477,10628} It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8.{11895,12477} VPC 23019 is an aryl amide-containing S1P analog that acts as a competitive antagonist at both S1P1 and S1P3 receptors (pKis = 7.86 and 5.93, respectively).{12407} It can inhibit S1P-induced migration of thyroid cancer cells, ovarian cancer cells, and neural stem cells.{17724}
Brand:CaymanSKU:- Sphingosine-1-phosphate (S1P; Item No. 62570) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis.{11895,12477,10628} It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8.{11895,12477} VPC 23019 is an aryl amide-containing S1P analog that acts as a competitive antagonist at both S1P1 and S1P3 receptors (pKis = 7.86 and 5.93, respectively).{12407} It can inhibit S1P-induced migration of thyroid cancer cells, ovarian cancer cells, and neural stem cells.{17724}
Brand:CaymanSKU:- Sphingosine-1-phosphate (S1P; Item No. 62570) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis.{11895,12477,10628} It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8.{11895,12477} VPC 23019 is an aryl amide-containing S1P analog that acts as a competitive antagonist at both S1P1 and S1P3 receptors (pKis = 7.86 and 5.93, respectively).{12407} It can inhibit S1P-induced migration of thyroid cancer cells, ovarian cancer cells, and neural stem cells.{17724}
Brand:CaymanSKU:- Sphingosine-1-phosphate (S1P; Item No. 62570) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis.{11895,12477,10628} It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8.{11895,12477} VPC 23019 is an aryl amide-containing S1P analog that acts as a competitive antagonist at both S1P1 and S1P3 receptors (pKis = 7.86 and 5.93, respectively).{12407} It can inhibit S1P-induced migration of thyroid cancer cells, ovarian cancer cells, and neural stem cells.{17724}
Brand:CaymanSKU:-
Vps34-IN1 is a potent inhibitor of the class III phosphoinositide 3-kinase (PI3K) vacuolar protein sorting 34 (Vps34; IC50 = 25 nM in vitro).{31851} It does not significantly inhibit the activity of over 340 additional kinases, including class I and II PI3Ks. Vps34-IN1 dose-dependently inhibits generation of PtdIns-(3)-p, which is essential to the formation and trafficking of endsomes and autophagosomes, without affecting the ability of class I PI3K to regulate Akt. It induces a rapid and pronounced loss of phosphorylation on serum- and glucocorticoid-regulated kinase 3.
Brand:CaymanSKU:-Available on backorder
Vps34-IN1 is a potent inhibitor of the class III phosphoinositide 3-kinase (PI3K) vacuolar protein sorting 34 (Vps34; IC50 = 25 nM in vitro).{31851} It does not significantly inhibit the activity of over 340 additional kinases, including class I and II PI3Ks. Vps34-IN1 dose-dependently inhibits generation of PtdIns-(3)-p, which is essential to the formation and trafficking of endsomes and autophagosomes, without affecting the ability of class I PI3K to regulate Akt. It induces a rapid and pronounced loss of phosphorylation on serum- and glucocorticoid-regulated kinase 3.
Brand:CaymanSKU:-Available on backorder
Vps34-IN1 is a potent inhibitor of the class III phosphoinositide 3-kinase (PI3K) vacuolar protein sorting 34 (Vps34; IC50 = 25 nM in vitro).{31851} It does not significantly inhibit the activity of over 340 additional kinases, including class I and II PI3Ks. Vps34-IN1 dose-dependently inhibits generation of PtdIns-(3)-p, which is essential to the formation and trafficking of endsomes and autophagosomes, without affecting the ability of class I PI3K to regulate Akt. It induces a rapid and pronounced loss of phosphorylation on serum- and glucocorticoid-regulated kinase 3.
Brand:CaymanSKU:-Available on backorder
Vps34-IN1 is a potent inhibitor of the class III phosphoinositide 3-kinase (PI3K) vacuolar protein sorting 34 (Vps34; IC50 = 25 nM in vitro).{31851} It does not significantly inhibit the activity of over 340 additional kinases, including class I and II PI3Ks. Vps34-IN1 dose-dependently inhibits generation of PtdIns-(3)-p, which is essential to the formation and trafficking of endsomes and autophagosomes, without affecting the ability of class I PI3K to regulate Akt. It induces a rapid and pronounced loss of phosphorylation on serum- and glucocorticoid-regulated kinase 3.
Brand:CaymanSKU:-Available on backorder
VR23 is a chloroquine (Item No. 14194) derivative that functions as a proteasome inhibitor (IC50s = 1 nM, 50-100 nM, and 3 µM for trypsin-like, chymotrypsin-like, and caspase-like proteasomes, respectively).{30904} It also deregulates the activity of cyclin E and other centrosomal proteins, resulting in the induction of multiple centrosome amplification, abnormal spindle formation, uneven cytokinesis, irreversible mitotic arrest, and eventually apoptosis that is specific to cancer cells.{30904} In combination with the chymotrypsin-like proteasome inhibitor bortezomib (Item No. 10008822), VR23 can produce a synergistic effect in killing multiple myeloma cells, including those that are resistant to bortezomib.{30904}
Brand:CaymanSKU:-Available on backorder
VR23 is a chloroquine (Item No. 14194) derivative that functions as a proteasome inhibitor (IC50s = 1 nM, 50-100 nM, and 3 µM for trypsin-like, chymotrypsin-like, and caspase-like proteasomes, respectively).{30904} It also deregulates the activity of cyclin E and other centrosomal proteins, resulting in the induction of multiple centrosome amplification, abnormal spindle formation, uneven cytokinesis, irreversible mitotic arrest, and eventually apoptosis that is specific to cancer cells.{30904} In combination with the chymotrypsin-like proteasome inhibitor bortezomib (Item No. 10008822), VR23 can produce a synergistic effect in killing multiple myeloma cells, including those that are resistant to bortezomib.{30904}
Brand:CaymanSKU:-Available on backorder
VR23 is a chloroquine (Item No. 14194) derivative that functions as a proteasome inhibitor (IC50s = 1 nM, 50-100 nM, and 3 µM for trypsin-like, chymotrypsin-like, and caspase-like proteasomes, respectively).{30904} It also deregulates the activity of cyclin E and other centrosomal proteins, resulting in the induction of multiple centrosome amplification, abnormal spindle formation, uneven cytokinesis, irreversible mitotic arrest, and eventually apoptosis that is specific to cancer cells.{30904} In combination with the chymotrypsin-like proteasome inhibitor bortezomib (Item No. 10008822), VR23 can produce a synergistic effect in killing multiple myeloma cells, including those that are resistant to bortezomib.{30904}
Brand:CaymanSKU:-Available on backorder
VR23 is a chloroquine (Item No. 14194) derivative that functions as a proteasome inhibitor (IC50s = 1 nM, 50-100 nM, and 3 µM for trypsin-like, chymotrypsin-like, and caspase-like proteasomes, respectively).{30904} It also deregulates the activity of cyclin E and other centrosomal proteins, resulting in the induction of multiple centrosome amplification, abnormal spindle formation, uneven cytokinesis, irreversible mitotic arrest, and eventually apoptosis that is specific to cancer cells.{30904} In combination with the chymotrypsin-like proteasome inhibitor bortezomib (Item No. 10008822), VR23 can produce a synergistic effect in killing multiple myeloma cells, including those that are resistant to bortezomib.{30904}
Brand:CaymanSKU:-Available on backorder
Phosphatidylinositol 3-kinase (PI3K) signaling through Akt/PKB and the mammalian target of rapamycin (mTOR) controls gene expression related to cell proliferation, differentiation, and apoptosis. Increased activity of this pathway is important in many types of cancer. VS-5584 is a purine analog that inhibits mTOR (IC50 = 37 nM) and PI3K (IC50s = 16, 68, 25, and 42 nM for the α, β, γ, and δ isoforms, respectively) without relevant activity against more than 400 additional lipid and protein kinases.{27667} By inhibiting the phosphorylation of substrates downstream of PI3K and mTOR, VS-5584 demonstrates broad anti-proliferative sensitivity leading to tumor growth inhibition in human tumor models.{27667}
Brand:CaymanSKU:-Out of stock
Phosphatidylinositol 3-kinase (PI3K) signaling through Akt/PKB and the mammalian target of rapamycin (mTOR) controls gene expression related to cell proliferation, differentiation, and apoptosis. Increased activity of this pathway is important in many types of cancer. VS-5584 is a purine analog that inhibits mTOR (IC50 = 37 nM) and PI3K (IC50s = 16, 68, 25, and 42 nM for the α, β, γ, and δ isoforms, respectively) without relevant activity against more than 400 additional lipid and protein kinases.{27667} By inhibiting the phosphorylation of substrates downstream of PI3K and mTOR, VS-5584 demonstrates broad anti-proliferative sensitivity leading to tumor growth inhibition in human tumor models.{27667}
Brand:CaymanSKU:-Out of stock
Phosphatidylinositol 3-kinase (PI3K) signaling through Akt/PKB and the mammalian target of rapamycin (mTOR) controls gene expression related to cell proliferation, differentiation, and apoptosis. Increased activity of this pathway is important in many types of cancer. VS-5584 is a purine analog that inhibits mTOR (IC50 = 37 nM) and PI3K (IC50s = 16, 68, 25, and 42 nM for the α, β, γ, and δ isoforms, respectively) without relevant activity against more than 400 additional lipid and protein kinases.{27667} By inhibiting the phosphorylation of substrates downstream of PI3K and mTOR, VS-5584 demonstrates broad anti-proliferative sensitivity leading to tumor growth inhibition in human tumor models.{27667}
Brand:CaymanSKU:-Out of stock
VS-5584 analog is a dual inhibitor of PI3Kα and mammalian target of rapamycin (mTOR; IC50s = 17 and 150 nM, respectively).{46913} It is a desmethyl analog of the dual PI3K/mTOR inhibitor VS-5584 (Item No. 16294).
Brand:CaymanSKU:30324 - 1 mgAvailable on backorder
VS-5584 analog is a dual inhibitor of PI3Kα and mammalian target of rapamycin (mTOR; IC50s = 17 and 150 nM, respectively).{46913} It is a desmethyl analog of the dual PI3K/mTOR inhibitor VS-5584 (Item No. 16294).
Brand:CaymanSKU:30324 - 10 mgAvailable on backorder
VS-5584 analog is a dual inhibitor of PI3Kα and mammalian target of rapamycin (mTOR; IC50s = 17 and 150 nM, respectively).{46913} It is a desmethyl analog of the dual PI3K/mTOR inhibitor VS-5584 (Item No. 16294).
Brand:CaymanSKU:30324 - 25 mgAvailable on backorder
VS-5584 analog is a dual inhibitor of PI3Kα and mammalian target of rapamycin (mTOR; IC50s = 17 and 150 nM, respectively).{46913} It is a desmethyl analog of the dual PI3K/mTOR inhibitor VS-5584 (Item No. 16294).
Brand:CaymanSKU:30324 - 5 mgAvailable on backorder
VTP-27999 is a renin inhibitor (IC50 = 0.47 nM for the recombinant human enzyme).{53713} It is selective for renin over the aspartyl proteases β-secretase, cathepsin D, and cathepsin E at 10 µM and is greater than 1,000-fold selective for renin over a panel of more than 250 receptors, ion channels, and enzymes. VTP-27999 (10 mg/kg, p.o.) reduces mean arterial pressure in rats expressing human renin and angiotensinogen, a double-transgenic model for angiotensin II-dependent hypertension.
Brand:CaymanSKU:27689 - 1 mgAvailable on backorder
VTP-27999 is a renin inhibitor (IC50 = 0.47 nM for the recombinant human enzyme).{53713} It is selective for renin over the aspartyl proteases β-secretase, cathepsin D, and cathepsin E at 10 µM and is greater than 1,000-fold selective for renin over a panel of more than 250 receptors, ion channels, and enzymes. VTP-27999 (10 mg/kg, p.o.) reduces mean arterial pressure in rats expressing human renin and angiotensinogen, a double-transgenic model for angiotensin II-dependent hypertension.
Brand:CaymanSKU:27689 - 10 mgAvailable on backorder
VTP-27999 is a renin inhibitor (IC50 = 0.47 nM for the recombinant human enzyme).{53713} It is selective for renin over the aspartyl proteases β-secretase, cathepsin D, and cathepsin E at 10 µM and is greater than 1,000-fold selective for renin over a panel of more than 250 receptors, ion channels, and enzymes. VTP-27999 (10 mg/kg, p.o.) reduces mean arterial pressure in rats expressing human renin and angiotensinogen, a double-transgenic model for angiotensin II-dependent hypertension.
Brand:CaymanSKU:27689 - 25 mgAvailable on backorder
VTP-27999 is a renin inhibitor (IC50 = 0.47 nM for the recombinant human enzyme).{53713} It is selective for renin over the aspartyl proteases β-secretase, cathepsin D, and cathepsin E at 10 µM and is greater than 1,000-fold selective for renin over a panel of more than 250 receptors, ion channels, and enzymes. VTP-27999 (10 mg/kg, p.o.) reduces mean arterial pressure in rats expressing human renin and angiotensinogen, a double-transgenic model for angiotensin II-dependent hypertension.
Brand:CaymanSKU:27689 - 5 mgAvailable on backorder
VU0029251 is a partial antagonist of metabotropic glutamate receptor 5 (mGluR5; Ki = 1.07 µM).{47575} It inhibits calcium mobilization induced by glutamate in HEK293 cell membranes expressing rat mGluR5 (IC50 = 1.7 µM).
Brand:CaymanSKU:21987 -Out of stock
VU0029251 is a partial antagonist of metabotropic glutamate receptor 5 (mGluR5; Ki = 1.07 µM).{47575} It inhibits calcium mobilization induced by glutamate in HEK293 cell membranes expressing rat mGluR5 (IC50 = 1.7 µM).
Brand:CaymanSKU:21987 -Out of stock
VU0029251 is a partial antagonist of metabotropic glutamate receptor 5 (mGluR5; Ki = 1.07 µM).{47575} It inhibits calcium mobilization induced by glutamate in HEK293 cell membranes expressing rat mGluR5 (IC50 = 1.7 µM).
Brand:CaymanSKU:21987 -Out of stock
VU0029251 is a partial antagonist of metabotropic glutamate receptor 5 (mGluR5; Ki = 1.07 µM).{47575} It inhibits calcium mobilization induced by glutamate in HEK293 cell membranes expressing rat mGluR5 (IC50 = 1.7 µM).
Brand:CaymanSKU:21987 -Out of stock
VU0071063 is a potent and selective activator of the inward-rectifier potassium channel (Kir) 6.2 and sulfonylurea receptor (SUR) 1 (EC50 = 7 µM using whole cell patch clamp electrophysiology).{34016} It is selective for SUR1-containing Kir6.1 or Kir6.2 channels over SUR2A, Kir2.1, Kir2.2, Kir2.3, Kir3.1/3/2, and voltage-gated potassium channel 2.1. VU0071063 inhibits glucose-stimulated calcium entry in isolated mouse pancreatic β-cells.
Brand:CaymanSKU:21897 -Out of stock
VU0071063 is a potent and selective activator of the inward-rectifier potassium channel (Kir) 6.2 and sulfonylurea receptor (SUR) 1 (EC50 = 7 µM using whole cell patch clamp electrophysiology).{34016} It is selective for SUR1-containing Kir6.1 or Kir6.2 channels over SUR2A, Kir2.1, Kir2.2, Kir2.3, Kir3.1/3/2, and voltage-gated potassium channel 2.1. VU0071063 inhibits glucose-stimulated calcium entry in isolated mouse pancreatic β-cells.
Brand:CaymanSKU:21897 -Out of stock
VU0071063 is a potent and selective activator of the inward-rectifier potassium channel (Kir) 6.2 and sulfonylurea receptor (SUR) 1 (EC50 = 7 µM using whole cell patch clamp electrophysiology).{34016} It is selective for SUR1-containing Kir6.1 or Kir6.2 channels over SUR2A, Kir2.1, Kir2.2, Kir2.3, Kir3.1/3/2, and voltage-gated potassium channel 2.1. VU0071063 inhibits glucose-stimulated calcium entry in isolated mouse pancreatic β-cells.
Brand:CaymanSKU:21897 -Out of stock
VU0071063 is a potent and selective activator of the inward-rectifier potassium channel (Kir) 6.2 and sulfonylurea receptor (SUR) 1 (EC50 = 7 µM using whole cell patch clamp electrophysiology).{34016} It is selective for SUR1-containing Kir6.1 or Kir6.2 channels over SUR2A, Kir2.1, Kir2.2, Kir2.3, Kir3.1/3/2, and voltage-gated potassium channel 2.1. VU0071063 inhibits glucose-stimulated calcium entry in isolated mouse pancreatic β-cells.
Brand:CaymanSKU:21897 -Out of stock
VU0155041 is a positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4) with an EC50 value of 2.5 μM for glutamate response in a thallium flux assay.{37088} It is selective for mGluR4, exhibiting no effect on radioligand binding at 67 G protein-coupled receptors, ion channels, and transporters, and lacking antagonist activity at NMDA receptors in striatal medium spiny neurons at a concentration of 10 μM. In vivo, VU0155041 decreases catalepsy induced by haloperidol (Item No. 12014) and reverses askinesias induced by reserpine (Item No. 16474) in rat models of Parkinson’s disease. Chronic treatment with VU0155041 restores social behavior in the Oprm-/- mouse model of autism.{37089} It also increases the percentage of time spent in the open arms of the elevated plus maze, a measure of decreased anxiety, in mice.{37090}
Brand:CaymanSKU:21775 -Out of stock
VU0155041 is a positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4) with an EC50 value of 2.5 μM for glutamate response in a thallium flux assay.{37088} It is selective for mGluR4, exhibiting no effect on radioligand binding at 67 G protein-coupled receptors, ion channels, and transporters, and lacking antagonist activity at NMDA receptors in striatal medium spiny neurons at a concentration of 10 μM. In vivo, VU0155041 decreases catalepsy induced by haloperidol (Item No. 12014) and reverses askinesias induced by reserpine (Item No. 16474) in rat models of Parkinson’s disease. Chronic treatment with VU0155041 restores social behavior in the Oprm-/- mouse model of autism.{37089} It also increases the percentage of time spent in the open arms of the elevated plus maze, a measure of decreased anxiety, in mice.{37090}
Brand:CaymanSKU:21775 -Out of stock
VU0155041 is a positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4) with an EC50 value of 2.5 μM for glutamate response in a thallium flux assay.{37088} It is selective for mGluR4, exhibiting no effect on radioligand binding at 67 G protein-coupled receptors, ion channels, and transporters, and lacking antagonist activity at NMDA receptors in striatal medium spiny neurons at a concentration of 10 μM. In vivo, VU0155041 decreases catalepsy induced by haloperidol (Item No. 12014) and reverses askinesias induced by reserpine (Item No. 16474) in rat models of Parkinson’s disease. Chronic treatment with VU0155041 restores social behavior in the Oprm-/- mouse model of autism.{37089} It also increases the percentage of time spent in the open arms of the elevated plus maze, a measure of decreased anxiety, in mice.{37090}
Brand:CaymanSKU:21775 -Out of stock
VU0240551 is a K+/Cl- cotransporter 2 (KCC2) inhibitor (IC50 = 568 nM).{46717} It selectively inhibits KCC2 over Na+/K+/Cl- cotransporter 1 (NKCC1; IC50 = >50 µM) but does inhibit the activity of adenosine A1 and A3 receptors, as well as inhibits activity of L-type calcium channels at the benzothiazepine site and human ether-a-go-go-related gene (hERG) potassium channels by greater than 50% in a panel of 68 receptors, ion channels, and transporters at 10 µM. VU0240551 decreases potassium ion uptake by 70% in HEK293 cells expressing KCC2 when used at a concentration of 1 µM.
Brand:CaymanSKU:29790 - 10 mgAvailable on backorder
VU0240551 is a K+/Cl- cotransporter 2 (KCC2) inhibitor (IC50 = 568 nM).{46717} It selectively inhibits KCC2 over Na+/K+/Cl- cotransporter 1 (NKCC1; IC50 = >50 µM) but does inhibit the activity of adenosine A1 and A3 receptors, as well as inhibits activity of L-type calcium channels at the benzothiazepine site and human ether-a-go-go-related gene (hERG) potassium channels by greater than 50% in a panel of 68 receptors, ion channels, and transporters at 10 µM. VU0240551 decreases potassium ion uptake by 70% in HEK293 cells expressing KCC2 when used at a concentration of 1 µM.
Brand:CaymanSKU:29790 - 25 mgAvailable on backorder
VU0240551 is a K+/Cl- cotransporter 2 (KCC2) inhibitor (IC50 = 568 nM).{46717} It selectively inhibits KCC2 over Na+/K+/Cl- cotransporter 1 (NKCC1; IC50 = >50 µM) but does inhibit the activity of adenosine A1 and A3 receptors, as well as inhibits activity of L-type calcium channels at the benzothiazepine site and human ether-a-go-go-related gene (hERG) potassium channels by greater than 50% in a panel of 68 receptors, ion channels, and transporters at 10 µM. VU0240551 decreases potassium ion uptake by 70% in HEK293 cells expressing KCC2 when used at a concentration of 1 µM.
Brand:CaymanSKU:29790 - 5 mgAvailable on backorder
VU0240551 is a K+/Cl- cotransporter 2 (KCC2) inhibitor (IC50 = 568 nM).{46717} It selectively inhibits KCC2 over Na+/K+/Cl- cotransporter 1 (NKCC1; IC50 = >50 µM) but does inhibit the activity of adenosine A1 and A3 receptors, as well as inhibits activity of L-type calcium channels at the benzothiazepine site and human ether-a-go-go-related gene (hERG) potassium channels by greater than 50% in a panel of 68 receptors, ion channels, and transporters at 10 µM. VU0240551 decreases potassium ion uptake by 70% in HEK293 cells expressing KCC2 when used at a concentration of 1 µM.
Brand:CaymanSKU:29790 - 50 mgAvailable on backorder
VU0255035 is a competitive, orthosteric antagonist of the muscarinic M1 receptor (IC50 = 130 nM).{30840,30841} It displays at least 75-fold selectivity for M1 over other muscarinic receptors, as well as a panel of receptors, ion channels, and transporters.{30840,30841} VU0255035 is effective in cells and in vivo and brain penetrating, blocking pilocarpine-induced seizures without disrupting contextual fear conditioning in mice.{30840,30841} VU0255035 is used to examine the role of the M1 receptor in diverse situations.{25277,30842,30839}
Brand:CaymanSKU:-Available on backorder
VU0255035 is a competitive, orthosteric antagonist of the muscarinic M1 receptor (IC50 = 130 nM).{30840,30841} It displays at least 75-fold selectivity for M1 over other muscarinic receptors, as well as a panel of receptors, ion channels, and transporters.{30840,30841} VU0255035 is effective in cells and in vivo and brain penetrating, blocking pilocarpine-induced seizures without disrupting contextual fear conditioning in mice.{30840,30841} VU0255035 is used to examine the role of the M1 receptor in diverse situations.{25277,30842,30839}
Brand:CaymanSKU:-Available on backorder
VU0357017 is an allosteric agonist of M1 muscarinic acetylcholine receptors (mAChRs; Ki = 9.91 µM in CHO cells).{40723} In vitro, it is selective for M1 over M2-M5 mAChRs (Kis = 21.4-50 µM in CHO cells). VU0357017 induces concentration-dependent increases in calcium mobilization and activates the ERK signaling pathway with EC50 values of 1.6 and 37 µM, respectively, in CHO cells expressing human recombinant M1 receptors.{37300} In vivo, VU0357017 crosses the blood-brain barrier and reverses scopolamine-induced deficits in contextual fear conditioning in rats when used at a dose of 10 mg/kg.{40724}
Brand:CaymanSKU:11939 - 1 mgAvailable on backorder
VU0357017 is an allosteric agonist of M1 muscarinic acetylcholine receptors (mAChRs; Ki = 9.91 µM in CHO cells).{40723} In vitro, it is selective for M1 over M2-M5 mAChRs (Kis = 21.4-50 µM in CHO cells). VU0357017 induces concentration-dependent increases in calcium mobilization and activates the ERK signaling pathway with EC50 values of 1.6 and 37 µM, respectively, in CHO cells expressing human recombinant M1 receptors.{37300} In vivo, VU0357017 crosses the blood-brain barrier and reverses scopolamine-induced deficits in contextual fear conditioning in rats when used at a dose of 10 mg/kg.{40724}
Brand:CaymanSKU:11939 - 10 mgAvailable on backorder
VU0357017 is an allosteric agonist of M1 muscarinic acetylcholine receptors (mAChRs; Ki = 9.91 µM in CHO cells).{40723} In vitro, it is selective for M1 over M2-M5 mAChRs (Kis = 21.4-50 µM in CHO cells). VU0357017 induces concentration-dependent increases in calcium mobilization and activates the ERK signaling pathway with EC50 values of 1.6 and 37 µM, respectively, in CHO cells expressing human recombinant M1 receptors.{37300} In vivo, VU0357017 crosses the blood-brain barrier and reverses scopolamine-induced deficits in contextual fear conditioning in rats when used at a dose of 10 mg/kg.{40724}
Brand:CaymanSKU:11939 - 25 mgAvailable on backorder
VU0357017 is an allosteric agonist of M1 muscarinic acetylcholine receptors (mAChRs; Ki = 9.91 µM in CHO cells).{40723} In vitro, it is selective for M1 over M2-M5 mAChRs (Kis = 21.4-50 µM in CHO cells). VU0357017 induces concentration-dependent increases in calcium mobilization and activates the ERK signaling pathway with EC50 values of 1.6 and 37 µM, respectively, in CHO cells expressing human recombinant M1 receptors.{37300} In vivo, VU0357017 crosses the blood-brain barrier and reverses scopolamine-induced deficits in contextual fear conditioning in rats when used at a dose of 10 mg/kg.{40724}
Brand:CaymanSKU:11939 - 5 mgAvailable on backorder
VU0357121 is a positive allosteric modulator of metabotropic glutamate receptor 5 (mGluR5) that has an EC50 value of 33 nM for the rat receptor expressed in HEK293 cells in a calcium flux assay.{56042} It is selective for mGluR5 and does not modulate responses at mGluR2-4 or mGluR6-8 but does inhibit mGluR1.
Brand:CaymanSKU:22199 -Out of stock
VU0357121 is a positive allosteric modulator of metabotropic glutamate receptor 5 (mGluR5) that has an EC50 value of 33 nM for the rat receptor expressed in HEK293 cells in a calcium flux assay.{56042} It is selective for mGluR5 and does not modulate responses at mGluR2-4 or mGluR6-8 but does inhibit mGluR1.
Brand:CaymanSKU:22199 -Out of stock
VU0357121 is a positive allosteric modulator of metabotropic glutamate receptor 5 (mGluR5) that has an EC50 value of 33 nM for the rat receptor expressed in HEK293 cells in a calcium flux assay.{56042} It is selective for mGluR5 and does not modulate responses at mGluR2-4 or mGluR6-8 but does inhibit mGluR1.
Brand:CaymanSKU:22199 -Out of stock
VU0357121 is a positive allosteric modulator of metabotropic glutamate receptor 5 (mGluR5) that has an EC50 value of 33 nM for the rat receptor expressed in HEK293 cells in a calcium flux assay.{56042} It is selective for mGluR5 and does not modulate responses at mGluR2-4 or mGluR6-8 but does inhibit mGluR1.
Brand:CaymanSKU:22199 -Out of stock
VU036172 is a positive allosteric modulator of metabotropic glutamate receptor 5 (mGluR5; Ki = 195 nM).{47575} It is selective for mGluR5 over mGluR1, mGluR3, and mGluR4 at 10 µM. VU036172 (20 and 50 µM) prevents TNF-α and nitric oxide (NO) production by IFN-γ- or LPS-stimulated BV-2 and primary microglial cells.{47576} It reduces the expression of inducible nitric oxide synthase (iNOS) and increases the expression of Ym1 and arginase 1 in LPS-stimulated BV-2 cells when used at a concentration of 20 µM. VU036172 (50 mg/kg) reduces the size of cortical lesions, prevents neuronal degeneration, and improves sensorimotor deficits in the beam walk test in a mouse model of traumatic brain injury (TBI), indicating improved recovery of motor function.
Brand:CaymanSKU:22074 -Out of stock
VU036172 is a positive allosteric modulator of metabotropic glutamate receptor 5 (mGluR5; Ki = 195 nM).{47575} It is selective for mGluR5 over mGluR1, mGluR3, and mGluR4 at 10 µM. VU036172 (20 and 50 µM) prevents TNF-α and nitric oxide (NO) production by IFN-γ- or LPS-stimulated BV-2 and primary microglial cells.{47576} It reduces the expression of inducible nitric oxide synthase (iNOS) and increases the expression of Ym1 and arginase 1 in LPS-stimulated BV-2 cells when used at a concentration of 20 µM. VU036172 (50 mg/kg) reduces the size of cortical lesions, prevents neuronal degeneration, and improves sensorimotor deficits in the beam walk test in a mouse model of traumatic brain injury (TBI), indicating improved recovery of motor function.
Brand:CaymanSKU:22074 -Out of stock
VU036172 is a positive allosteric modulator of metabotropic glutamate receptor 5 (mGluR5; Ki = 195 nM).{47575} It is selective for mGluR5 over mGluR1, mGluR3, and mGluR4 at 10 µM. VU036172 (20 and 50 µM) prevents TNF-α and nitric oxide (NO) production by IFN-γ- or LPS-stimulated BV-2 and primary microglial cells.{47576} It reduces the expression of inducible nitric oxide synthase (iNOS) and increases the expression of Ym1 and arginase 1 in LPS-stimulated BV-2 cells when used at a concentration of 20 µM. VU036172 (50 mg/kg) reduces the size of cortical lesions, prevents neuronal degeneration, and improves sensorimotor deficits in the beam walk test in a mouse model of traumatic brain injury (TBI), indicating improved recovery of motor function.
Brand:CaymanSKU:22074 -Out of stock
VU036172 is a positive allosteric modulator of metabotropic glutamate receptor 5 (mGluR5; Ki = 195 nM).{47575} It is selective for mGluR5 over mGluR1, mGluR3, and mGluR4 at 10 µM. VU036172 (20 and 50 µM) prevents TNF-α and nitric oxide (NO) production by IFN-γ- or LPS-stimulated BV-2 and primary microglial cells.{47576} It reduces the expression of inducible nitric oxide synthase (iNOS) and increases the expression of Ym1 and arginase 1 in LPS-stimulated BV-2 cells when used at a concentration of 20 µM. VU036172 (50 mg/kg) reduces the size of cortical lesions, prevents neuronal degeneration, and improves sensorimotor deficits in the beam walk test in a mouse model of traumatic brain injury (TBI), indicating improved recovery of motor function.
Brand:CaymanSKU:22074 -Out of stock
Glutamate, the major excitatory neurotransmitter in the central nervous system, signals through both ionotropic and metabotropic glutamate receptors. Of the eight metabotropic glutamate receptors (mGlus) discovered thus far, development of inhibitors to mGlu5 has been given significant attention in preclinical models of disease, including pain, anxiety, gastresophageal reflux disease, Parkinson’s associated dyskinesia, and fragile X syndrome, as well as in animal models of drug addiction. VU0360223 is a noncompetitive antagonist (negative allosteric modulator) of mGlu5 that demonstrates an IC50 value of 61 nM in a calcium mobilization assay and a Ki value of 477 nM in a radioligand binding assay.{19263} A 10 μM concentration of VU0360223 results in a near complete blockade of the glutamate response in cortical astrocytes.{19263} A 30 mg/kg dose of VU0360223 in mice yields potent inhibition in a marble burying model of anxiety and is efficacious in an operant sensation seeking model of addiction.{19263}
Brand:CaymanSKU:11995 - 1 mgAvailable on backorder