Cayman
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Saxagliptin is a potent inhibitor of dipeptidyl peptidase 4 (DPP-4; Ki = 0.6 nM).{40437} It inhibits DPP-4 ex vivo (ED50 = 0.12 μmol/kg) in plasma from normal fasted rats. Saxagliptin (0.3-3 mg/kg) reduces plasma glucose levels in Zuckerfa/fa diabetic rats in a dose-dependent manner. Oral administration at doses ranging from 1-10 μmol/kg increases plasma insulin levels and improves glucose clearance in ob/ob mice, a transgenic model of obesity. Saxagliptin induces systolic and diastolic dysfunction, reduces contractile force, and exacerbates ischemia-reperfusion injury-induced cardiac dysfunction in isolated guinea pig hearts.{40438} Formulations containing saxagliptin have been used for the treatment of type 2 diabetes.
Brand:CaymanSKU:23697 - 25 mgAvailable on backorder
Saxagliptin is a potent inhibitor of dipeptidyl peptidase 4 (DPP-4; Ki = 0.6 nM).{40437} It inhibits DPP-4 ex vivo (ED50 = 0.12 μmol/kg) in plasma from normal fasted rats. Saxagliptin (0.3-3 mg/kg) reduces plasma glucose levels in Zuckerfa/fa diabetic rats in a dose-dependent manner. Oral administration at doses ranging from 1-10 μmol/kg increases plasma insulin levels and improves glucose clearance in ob/ob mice, a transgenic model of obesity. Saxagliptin induces systolic and diastolic dysfunction, reduces contractile force, and exacerbates ischemia-reperfusion injury-induced cardiac dysfunction in isolated guinea pig hearts.{40438} Formulations containing saxagliptin have been used for the treatment of type 2 diabetes.
Brand:CaymanSKU:23697 - 5 mgAvailable on backorder
Saxagliptin is a potent inhibitor of dipeptidyl peptidase 4 (DPP-4; Ki = 0.6 nM).{40437} It inhibits DPP-4 ex vivo (ED50 = 0.12 μmol/kg) in plasma from normal fasted rats. Saxagliptin (0.3-3 mg/kg) reduces plasma glucose levels in Zuckerfa/fa diabetic rats in a dose-dependent manner. Oral administration at doses ranging from 1-10 μmol/kg increases plasma insulin levels and improves glucose clearance in ob/ob mice, a transgenic model of obesity. Saxagliptin induces systolic and diastolic dysfunction, reduces contractile force, and exacerbates ischemia-reperfusion injury-induced cardiac dysfunction in isolated guinea pig hearts.{40438} Formulations containing saxagliptin have been used for the treatment of type 2 diabetes.
Brand:CaymanSKU:23697 - 50 mgAvailable on backorder
SB 202190 is a selective, potent, cell-permeable inhibitor of p38 MAP kinases, inhibiting p38α (SAPK2A, MAPK14) and p38β (SAPK2B, MAPK11) with IC50 values of 50 and 100 nM, respectively.{21464,12847} When tested at 10 μM, SB 202190 has negligible effects on a range of other kinases, including other MAP kinases (ERKs, JNKs).{12847} Pyridinyl imidazole inhibitors, including this compound, directly bind p38 MAP kinases in the ATP binding pocket.{15221} Recently, SB 202190 has been used to elucidate the roles of p38 MAP kinases in inflammatory cytokine expression, nicotine-induced receptor expression, and HIV-mediated depressive disorder.{21463,21466,21467}
Brand:CaymanSKU:10010399 - 10 mgAvailable on backorder
SB 202190 is a selective, potent, cell-permeable inhibitor of p38 MAP kinases, inhibiting p38α (SAPK2A, MAPK14) and p38β (SAPK2B, MAPK11) with IC50 values of 50 and 100 nM, respectively.{21464,12847} When tested at 10 μM, SB 202190 has negligible effects on a range of other kinases, including other MAP kinases (ERKs, JNKs).{12847} Pyridinyl imidazole inhibitors, including this compound, directly bind p38 MAP kinases in the ATP binding pocket.{15221} Recently, SB 202190 has been used to elucidate the roles of p38 MAP kinases in inflammatory cytokine expression, nicotine-induced receptor expression, and HIV-mediated depressive disorder.{21463,21466,21467}
Brand:CaymanSKU:10010399 - 100 mgAvailable on backorder
SB 202190 is a selective, potent, cell-permeable inhibitor of p38 MAP kinases, inhibiting p38α (SAPK2A, MAPK14) and p38β (SAPK2B, MAPK11) with IC50 values of 50 and 100 nM, respectively.{21464,12847} When tested at 10 μM, SB 202190 has negligible effects on a range of other kinases, including other MAP kinases (ERKs, JNKs).{12847} Pyridinyl imidazole inhibitors, including this compound, directly bind p38 MAP kinases in the ATP binding pocket.{15221} Recently, SB 202190 has been used to elucidate the roles of p38 MAP kinases in inflammatory cytokine expression, nicotine-induced receptor expression, and HIV-mediated depressive disorder.{21463,21466,21467}
Brand:CaymanSKU:10010399 - 25 mgAvailable on backorder
SB 202190 is a selective, potent, cell-permeable inhibitor of p38 MAP kinases, inhibiting p38α (SAPK2A, MAPK14) and p38β (SAPK2B, MAPK11) with IC50 values of 50 and 100 nM, respectively.{21464,12847} When tested at 10 μM, SB 202190 has negligible effects on a range of other kinases, including other MAP kinases (ERKs, JNKs).{12847} Pyridinyl imidazole inhibitors, including this compound, directly bind p38 MAP kinases in the ATP binding pocket.{15221} Recently, SB 202190 has been used to elucidate the roles of p38 MAP kinases in inflammatory cytokine expression, nicotine-induced receptor expression, and HIV-mediated depressive disorder.{21463,21466,21467}
Brand:CaymanSKU:10010399 - 50 mgAvailable on backorder
SB 202190 is a potent, selective, and cell-permeable inhibitor of p38 MAP kinases, inhibiting p38α (SAPK2A, MAPK14) and p38β (SAPK2B, MAPK11) with IC50 values of 50 and 100 nM, respectively.{21464,12847} When tested at 10 μM, SB 202190 has negligible effects on a range of other kinases, including other MAP kinases such as ERK and JNK.{12847} It directly binds to the ATP binding pocket of p38 MAP kinases.{15221} SB 202190 has been used to elucidate the roles of p38 MAP kinases in inflammatory cytokine expression, nicotine-induced receptor expression, and HIV-mediated depressive disorder.{21463,21466,21467}
Brand:CaymanSKU:21201 -Out of stock
SB 202190 is a potent, selective, and cell-permeable inhibitor of p38 MAP kinases, inhibiting p38α (SAPK2A, MAPK14) and p38β (SAPK2B, MAPK11) with IC50 values of 50 and 100 nM, respectively.{21464,12847} When tested at 10 μM, SB 202190 has negligible effects on a range of other kinases, including other MAP kinases such as ERK and JNK.{12847} It directly binds to the ATP binding pocket of p38 MAP kinases.{15221} SB 202190 has been used to elucidate the roles of p38 MAP kinases in inflammatory cytokine expression, nicotine-induced receptor expression, and HIV-mediated depressive disorder.{21463,21466,21467}
Brand:CaymanSKU:21201 -Out of stock
SB 202190 is a potent, selective, and cell-permeable inhibitor of p38 MAP kinases, inhibiting p38α (SAPK2A, MAPK14) and p38β (SAPK2B, MAPK11) with IC50 values of 50 and 100 nM, respectively.{21464,12847} When tested at 10 μM, SB 202190 has negligible effects on a range of other kinases, including other MAP kinases such as ERK and JNK.{12847} It directly binds to the ATP binding pocket of p38 MAP kinases.{15221} SB 202190 has been used to elucidate the roles of p38 MAP kinases in inflammatory cytokine expression, nicotine-induced receptor expression, and HIV-mediated depressive disorder.{21463,21466,21467}
Brand:CaymanSKU:21201 -Out of stock
SB 202190 is a potent, selective, and cell-permeable inhibitor of p38 MAP kinases, inhibiting p38α (SAPK2A, MAPK14) and p38β (SAPK2B, MAPK11) with IC50 values of 50 and 100 nM, respectively.{21464,12847} When tested at 10 μM, SB 202190 has negligible effects on a range of other kinases, including other MAP kinases such as ERK and JNK.{12847} It directly binds to the ATP binding pocket of p38 MAP kinases.{15221} SB 202190 has been used to elucidate the roles of p38 MAP kinases in inflammatory cytokine expression, nicotine-induced receptor expression, and HIV-mediated depressive disorder.{21463,21466,21467}
Brand:CaymanSKU:21201 -Out of stock
SB 202190 (Item No. 10010399) and SB 203580 (Item No. 13067) are potent, selective inhibitors of the MAP kinases p38α and p38β.{21464,12847} SB 202474 is a structural analog of SB 202190 and SB 203580 that is used as a negative control in studies of p38 inhibition.{16246,30206,30205}
Brand:CaymanSKU:-Available on backorder
Mitogen-activated protein kinases (MAPK) mediate signal transduction from cell surface receptors to the nucleus and are classified into various subtypes. p38 MAPK is activated by environmental stresses and inflammatory cytokines and is critical for normal immune and inflammatory responses as it regulates the expression of many cytokines, transcription factors, and cell surface receptors.{14980} SB 203580 is a pyridinyl imidazole inhibitor of p38 MAPK that specifically blocks its kinase activity. SB 203580 does not however, disrupt JNK activity, which is activated by similar stressors to those which activate p38 MAPK.{15737} p38 MAPK activity in heat-shocked HeLa cells and osmotically stressed PC12 cells is inhibited by SB 203580 with an IC50 value of 0.6 µM.{15737} SB 203580 also prevents the activation of PKB/Akt by inhibiting phosphoinositide-dependent protein kinase 1 (PDK1) at IC50 values of 3-5 µM.{15738}
Brand:CaymanSKU:- Mitogen-activated protein kinases (MAPK) mediate signal transduction from cell surface receptors to the nucleus and are classified into various subtypes. p38 MAPK is activated by environmental stresses and inflammatory cytokines and is critical for normal immune and inflammatory responses as it regulates the expression of many cytokines, transcription factors, and cell surface receptors.{14980} SB 203580 is a pyridinyl imidazole inhibitor of p38 MAPK that specifically blocks its kinase activity. SB 203580 does not however, disrupt JNK activity, which is activated by similar stressors to those which activate p38 MAPK.{15737} p38 MAPK activity in heat-shocked HeLa cells and osmotically stressed PC12 cells is inhibited by SB 203580 with an IC50 value of 0.6 µM.{15737} SB 203580 also prevents the activation of PKB/Akt by inhibiting phosphoinositide-dependent protein kinase 1 (PDK1) at IC50 values of 3-5 µM.{15738}
Brand:CaymanSKU:- Mitogen-activated protein kinases (MAPK) mediate signal transduction from cell surface receptors to the nucleus and are classified into various subtypes. p38 MAPK is activated by environmental stresses and inflammatory cytokines and is critical for normal immune and inflammatory responses as it regulates the expression of many cytokines, transcription factors, and cell surface receptors.{14980} SB 203580 is a pyridinyl imidazole inhibitor of p38 MAPK that specifically blocks its kinase activity. SB 203580 does not however, disrupt JNK activity, which is activated by similar stressors to those which activate p38 MAPK.{15737} p38 MAPK activity in heat-shocked HeLa cells and osmotically stressed PC12 cells is inhibited by SB 203580 with an IC50 value of 0.6 µM.{15737} SB 203580 also prevents the activation of PKB/Akt by inhibiting phosphoinositide-dependent protein kinase 1 (PDK1) at IC50 values of 3-5 µM.{15738}
Brand:CaymanSKU:- Mitogen-activated protein kinases (MAPK) mediate signal transduction from cell surface receptors to the nucleus and are classified into various subtypes. p38 MAPK is activated by environmental stresses and inflammatory cytokines and is critical for normal immune and inflammatory responses as it regulates the expression of many cytokines, transcription factors, and cell surface receptors.{14980} SB 203580 is a pyridinyl imidazole inhibitor of p38 MAPK that specifically blocks its kinase activity. SB 203580 does not however, disrupt JNK activity, which is activated by similar stressors to those which activate p38 MAPK.{15737} p38 MAPK activity in heat-shocked HeLa cells and osmotically stressed PC12 cells is inhibited by SB 203580 with an IC50 value of 0.6 µM.{15737} SB 203580 also prevents the activation of PKB/Akt by inhibiting phosphoinositide-dependent protein kinase 1 (PDK1) at IC50 values of 3-5 µM.{15738}
Brand:CaymanSKU:-
Mitogen-activated protein kinases (MAPKs) mediate signal transduction from cell surface receptors to the nucleus and are classified into various subtypes. p38 MAPK is activated by environmental stresses and inflammatory cytokines and is critical for normal immune and inflammatory responses as it regulates the expression of many cytokines, transcription factors, and cell surface receptors.{14980} p38 MAPK activity in heat-shocked HeLa cells and osmotically stressed PC12 cells is inhibited by SB 203580 with an IC50 value of 0.6 µM.{15737} SB 203580 also prevents the activation of PKB/Akt by inhibiting phosphoinositide-dependent protein kinase 1 (PDK1) at IC50 values of 3-5 µM.{15738} SB 203580 (hydrochloride) has a formulation with greater solubility in organic solvents than standard SB 203580 (Item No. 13067).
Brand:CaymanSKU:- Mitogen-activated protein kinases (MAPKs) mediate signal transduction from cell surface receptors to the nucleus and are classified into various subtypes. p38 MAPK is activated by environmental stresses and inflammatory cytokines and is critical for normal immune and inflammatory responses as it regulates the expression of many cytokines, transcription factors, and cell surface receptors.{14980} p38 MAPK activity in heat-shocked HeLa cells and osmotically stressed PC12 cells is inhibited by SB 203580 with an IC50 value of 0.6 µM.{15737} SB 203580 also prevents the activation of PKB/Akt by inhibiting phosphoinositide-dependent protein kinase 1 (PDK1) at IC50 values of 3-5 µM.{15738} SB 203580 (hydrochloride) has a formulation with greater solubility in organic solvents than standard SB 203580 (Item No. 13067).
Brand:CaymanSKU:- Mitogen-activated protein kinases (MAPKs) mediate signal transduction from cell surface receptors to the nucleus and are classified into various subtypes. p38 MAPK is activated by environmental stresses and inflammatory cytokines and is critical for normal immune and inflammatory responses as it regulates the expression of many cytokines, transcription factors, and cell surface receptors.{14980} p38 MAPK activity in heat-shocked HeLa cells and osmotically stressed PC12 cells is inhibited by SB 203580 with an IC50 value of 0.6 µM.{15737} SB 203580 also prevents the activation of PKB/Akt by inhibiting phosphoinositide-dependent protein kinase 1 (PDK1) at IC50 values of 3-5 µM.{15738} SB 203580 (hydrochloride) has a formulation with greater solubility in organic solvents than standard SB 203580 (Item No. 13067).
Brand:CaymanSKU:- Mitogen-activated protein kinases (MAPKs) mediate signal transduction from cell surface receptors to the nucleus and are classified into various subtypes. p38 MAPK is activated by environmental stresses and inflammatory cytokines and is critical for normal immune and inflammatory responses as it regulates the expression of many cytokines, transcription factors, and cell surface receptors.{14980} p38 MAPK activity in heat-shocked HeLa cells and osmotically stressed PC12 cells is inhibited by SB 203580 with an IC50 value of 0.6 µM.{15737} SB 203580 also prevents the activation of PKB/Akt by inhibiting phosphoinositide-dependent protein kinase 1 (PDK1) at IC50 values of 3-5 µM.{15738} SB 203580 (hydrochloride) has a formulation with greater solubility in organic solvents than standard SB 203580 (Item No. 13067).
Brand:CaymanSKU:-
SB 204990 is a cell-permeable prodrug form of SB 201076, an inhibitor of ATP citrate lyase.{37244} SB 204990 inhibits fatty acid and cholesterol synthesis in HepG2 cells in a concentration-dependent manner. Oral administration of SB 204990 (25 mg/kg) reduces plasma levels of the lipoproteins VLDL, LDL, and HDL by 21, 40, and 22%, respectively, in dogs. It also reduces VLDL synthesis and plasma cholesterol and triglyceride levels in rats in a dose-dependent manner.
Brand:CaymanSKU:- SB 204990 is a cell-permeable prodrug form of SB 201076, an inhibitor of ATP citrate lyase.{37244} SB 204990 inhibits fatty acid and cholesterol synthesis in HepG2 cells in a concentration-dependent manner. Oral administration of SB 204990 (25 mg/kg) reduces plasma levels of the lipoproteins VLDL, LDL, and HDL by 21, 40, and 22%, respectively, in dogs. It also reduces VLDL synthesis and plasma cholesterol and triglyceride levels in rats in a dose-dependent manner.
Brand:CaymanSKU:- SB 204990 is a cell-permeable prodrug form of SB 201076, an inhibitor of ATP citrate lyase.{37244} SB 204990 inhibits fatty acid and cholesterol synthesis in HepG2 cells in a concentration-dependent manner. Oral administration of SB 204990 (25 mg/kg) reduces plasma levels of the lipoproteins VLDL, LDL, and HDL by 21, 40, and 22%, respectively, in dogs. It also reduces VLDL synthesis and plasma cholesterol and triglyceride levels in rats in a dose-dependent manner.
Brand:CaymanSKU:-
SB 218078 is an inhibitor of checkpoint kinase 1 (Chk1) that blocks phosphorylation of cdc25 with an IC50 value of 15 nM.{31189} It less potently inhibits cdc2 and PKC (IC50s = 250 and 1,000 nM, respectively) and causes 85% inhibition of PKD1 at 1 µM.{31189,29520} SB 218078 releases G2 cell cycle arrest induced by γ-irradiation or the topoisomerase I inhibitor topotecan (Item No. 14129).{31189} In this way, SB 218078 enhances the cytotoxicity of DNA-damaging compounds.{24026}
Brand:CaymanSKU:-
SB 222200 is a neurokinin-3 (NK3) receptor antagonist (IC50 = 18.4 nM).{48780} It is selective for NK3 over NK1 and NK2 receptors (IC50s = 250 and >100,000 nM, respectively). SB 222200 decreases calcium mobilization induced by neurokinin B (Item No. 24542) with an IC50 value of 265 nM in HEK293 cells expressing the recombinant human receptor. It inhibits contractions induced by senktide (Item No. 16721) in isolated rabbit iris sphincter muscle when used at a concentration of 300 nM. SB 222200 (500 pmol, i.c.v.) decreases mean arterial pressure in spontaneously hypertensive, but not normotensive, rats.{48781} It prevents senktide-induced head shakes and tail whips in mice (ED50 = 5.6 mg/kg).{48780}
Brand:CaymanSKU:29422 - 10 mgAvailable on backorder
SB 222200 is a neurokinin-3 (NK3) receptor antagonist (IC50 = 18.4 nM).{48780} It is selective for NK3 over NK1 and NK2 receptors (IC50s = 250 and >100,000 nM, respectively). SB 222200 decreases calcium mobilization induced by neurokinin B (Item No. 24542) with an IC50 value of 265 nM in HEK293 cells expressing the recombinant human receptor. It inhibits contractions induced by senktide (Item No. 16721) in isolated rabbit iris sphincter muscle when used at a concentration of 300 nM. SB 222200 (500 pmol, i.c.v.) decreases mean arterial pressure in spontaneously hypertensive, but not normotensive, rats.{48781} It prevents senktide-induced head shakes and tail whips in mice (ED50 = 5.6 mg/kg).{48780}
Brand:CaymanSKU:29422 - 25 mgAvailable on backorder
SB 222200 is a neurokinin-3 (NK3) receptor antagonist (IC50 = 18.4 nM).{48780} It is selective for NK3 over NK1 and NK2 receptors (IC50s = 250 and >100,000 nM, respectively). SB 222200 decreases calcium mobilization induced by neurokinin B (Item No. 24542) with an IC50 value of 265 nM in HEK293 cells expressing the recombinant human receptor. It inhibits contractions induced by senktide (Item No. 16721) in isolated rabbit iris sphincter muscle when used at a concentration of 300 nM. SB 222200 (500 pmol, i.c.v.) decreases mean arterial pressure in spontaneously hypertensive, but not normotensive, rats.{48781} It prevents senktide-induced head shakes and tail whips in mice (ED50 = 5.6 mg/kg).{48780}
Brand:CaymanSKU:29422 - 5 mgAvailable on backorder
SB 222200 is a neurokinin-3 (NK3) receptor antagonist (IC50 = 18.4 nM).{48780} It is selective for NK3 over NK1 and NK2 receptors (IC50s = 250 and >100,000 nM, respectively). SB 222200 decreases calcium mobilization induced by neurokinin B (Item No. 24542) with an IC50 value of 265 nM in HEK293 cells expressing the recombinant human receptor. It inhibits contractions induced by senktide (Item No. 16721) in isolated rabbit iris sphincter muscle when used at a concentration of 300 nM. SB 222200 (500 pmol, i.c.v.) decreases mean arterial pressure in spontaneously hypertensive, but not normotensive, rats.{48781} It prevents senktide-induced head shakes and tail whips in mice (ED50 = 5.6 mg/kg).{48780}
Brand:CaymanSKU:29422 - 50 mgAvailable on backorder
CXCR2 (IL-8RB) is a seven-transmembrane G protein-coupled receptor whose physiological ligands include IL-8 (CXCL8) and growth related oncogene α (Gro-α; CXCL1). IL-8 and Gro-α are pro-inflammatory CXC chemokines that act as chemoattractants, especially for neutrophils, and promote angiogenesis. SB 225002 is a selective non-peptide inhibitor of CXCR2, inhibiting IL-8 binding to CXCR2 with an IC50 value of 22 nM.{17249} SB225002 inhibits neutrophil chemotaxis in response to IL-8 in vitro (IC50 = 20 nM) and blocks neutrophil margination induced by IL-8 in vivo (IC50 = 30 nM).{17249} Similarly, SB 225002 reduces neutrophil influx, the production of inflammatory mediators, and tissue damage in TNBS-induced colitis in mice.{17248}
Brand:CaymanSKU:- CXCR2 (IL-8RB) is a seven-transmembrane G protein-coupled receptor whose physiological ligands include IL-8 (CXCL8) and growth related oncogene α (Gro-α; CXCL1). IL-8 and Gro-α are pro-inflammatory CXC chemokines that act as chemoattractants, especially for neutrophils, and promote angiogenesis. SB 225002 is a selective non-peptide inhibitor of CXCR2, inhibiting IL-8 binding to CXCR2 with an IC50 value of 22 nM.{17249} SB225002 inhibits neutrophil chemotaxis in response to IL-8 in vitro (IC50 = 20 nM) and blocks neutrophil margination induced by IL-8 in vivo (IC50 = 30 nM).{17249} Similarly, SB 225002 reduces neutrophil influx, the production of inflammatory mediators, and tissue damage in TNBS-induced colitis in mice.{17248}
Brand:CaymanSKU:- CXCR2 (IL-8RB) is a seven-transmembrane G protein-coupled receptor whose physiological ligands include IL-8 (CXCL8) and growth related oncogene α (Gro-α; CXCL1). IL-8 and Gro-α are pro-inflammatory CXC chemokines that act as chemoattractants, especially for neutrophils, and promote angiogenesis. SB 225002 is a selective non-peptide inhibitor of CXCR2, inhibiting IL-8 binding to CXCR2 with an IC50 value of 22 nM.{17249} SB225002 inhibits neutrophil chemotaxis in response to IL-8 in vitro (IC50 = 20 nM) and blocks neutrophil margination induced by IL-8 in vivo (IC50 = 30 nM).{17249} Similarly, SB 225002 reduces neutrophil influx, the production of inflammatory mediators, and tissue damage in TNBS-induced colitis in mice.{17248}
Brand:CaymanSKU:- CXCR2 (IL-8RB) is a seven-transmembrane G protein-coupled receptor whose physiological ligands include IL-8 (CXCL8) and growth related oncogene α (Gro-α; CXCL1). IL-8 and Gro-α are pro-inflammatory CXC chemokines that act as chemoattractants, especially for neutrophils, and promote angiogenesis. SB 225002 is a selective non-peptide inhibitor of CXCR2, inhibiting IL-8 binding to CXCR2 with an IC50 value of 22 nM.{17249} SB225002 inhibits neutrophil chemotaxis in response to IL-8 in vitro (IC50 = 20 nM) and blocks neutrophil margination induced by IL-8 in vivo (IC50 = 30 nM).{17249} Similarly, SB 225002 reduces neutrophil influx, the production of inflammatory mediators, and tissue damage in TNBS-induced colitis in mice.{17248}
Brand:CaymanSKU:-
SB 239063 is a selective p38 MAPK inhibitor (IC50 = 44 nM for recombinant purified p38α).{30980} It displays greater than 220-fold selectivity for p38 MAPK over ERK, JNK1, and other kinases.{30980} SB 239063 has been shown to reduce inflammatory cytokine production in lipopolysaccharide-stimulated human peripheral blood monocytes (IC50s = 0.12 and 0.35 µM, respectively for IL-1 and TNF-α) and is neuroprotective following oral administration in a rat model of cerebral focal ischemia.{30980,30979}
Brand:CaymanSKU:-Available on backorder
SB 239063 is a selective p38 MAPK inhibitor (IC50 = 44 nM for recombinant purified p38α).{30980} It displays greater than 220-fold selectivity for p38 MAPK over ERK, JNK1, and other kinases.{30980} SB 239063 has been shown to reduce inflammatory cytokine production in lipopolysaccharide-stimulated human peripheral blood monocytes (IC50s = 0.12 and 0.35 µM, respectively for IL-1 and TNF-α) and is neuroprotective following oral administration in a rat model of cerebral focal ischemia.{30980,30979}
Brand:CaymanSKU:-Available on backorder
SB 239063 is a selective p38 MAPK inhibitor (IC50 = 44 nM for recombinant purified p38α).{30980} It displays greater than 220-fold selectivity for p38 MAPK over ERK, JNK1, and other kinases.{30980} SB 239063 has been shown to reduce inflammatory cytokine production in lipopolysaccharide-stimulated human peripheral blood monocytes (IC50s = 0.12 and 0.35 µM, respectively for IL-1 and TNF-α) and is neuroprotective following oral administration in a rat model of cerebral focal ischemia.{30980,30979}
Brand:CaymanSKU:-Available on backorder
CXCR2 (IL-8RB) is a seven-transmembrane G protein-coupled receptor whose physiological ligands include IL-8 (CXCL8) and many other CXC chemokines involved in the trafficking and activation of inflammatory cells. It is involved in various inflammatory diseases, including chronic obstructive pulmonary disease, psoriasis, rheumatoid arthritis, and ulcerative colitis. SB 265610 is a nonpeptide, allosteric, inverse agonist of CXCR2 (Kd = 2.51 nM) that prevents receptor activation by binding to a region distinct from the agonist binding site.{29567,29566} It does not bind to the related CXCR1 receptor.{29567} It has been shown to prevent neutrophil chemotaxis both in vitro and in a rat model of hyperoxia-induced lung injury.{29565}
Brand:CaymanSKU:-Available on backorder
CXCR2 (IL-8RB) is a seven-transmembrane G protein-coupled receptor whose physiological ligands include IL-8 (CXCL8) and many other CXC chemokines involved in the trafficking and activation of inflammatory cells. It is involved in various inflammatory diseases, including chronic obstructive pulmonary disease, psoriasis, rheumatoid arthritis, and ulcerative colitis. SB 265610 is a nonpeptide, allosteric, inverse agonist of CXCR2 (Kd = 2.51 nM) that prevents receptor activation by binding to a region distinct from the agonist binding site.{29567,29566} It does not bind to the related CXCR1 receptor.{29567} It has been shown to prevent neutrophil chemotaxis both in vitro and in a rat model of hyperoxia-induced lung injury.{29565}
Brand:CaymanSKU:-Available on backorder
CXCR2 (IL-8RB) is a seven-transmembrane G protein-coupled receptor whose physiological ligands include IL-8 (CXCL8) and many other CXC chemokines involved in the trafficking and activation of inflammatory cells. It is involved in various inflammatory diseases, including chronic obstructive pulmonary disease, psoriasis, rheumatoid arthritis, and ulcerative colitis. SB 265610 is a nonpeptide, allosteric, inverse agonist of CXCR2 (Kd = 2.51 nM) that prevents receptor activation by binding to a region distinct from the agonist binding site.{29567,29566} It does not bind to the related CXCR1 receptor.{29567} It has been shown to prevent neutrophil chemotaxis both in vitro and in a rat model of hyperoxia-induced lung injury.{29565}
Brand:CaymanSKU:-Available on backorder
SB 277011A is an antagonist of the dopamine D3 receptor (pKi = 8.0) that is at least 100-fold selective for D3 over other monoamine receptors (pKis = 6.0, 5.0, and 2, 5-HT1D and 5-HT1B respectively).{31910,31909,31908} It has high oral bioavailability and enters the central nervous system of the rat.{31910} SB 277011A has been shown to have potential benefits in animal models of schizophrenia and Parkinson’s disease.{31909,31907}
Brand:CaymanSKU:11982 - 1 mgAvailable on backorder
SB 277011A is an antagonist of the dopamine D3 receptor (pKi = 8.0) that is at least 100-fold selective for D3 over other monoamine receptors (pKis = 6.0, 5.0, and 2, 5-HT1D and 5-HT1B respectively).{31910,31909,31908} It has high oral bioavailability and enters the central nervous system of the rat.{31910} SB 277011A has been shown to have potential benefits in animal models of schizophrenia and Parkinson’s disease.{31909,31907}
Brand:CaymanSKU:11982 - 10 mgAvailable on backorder
SB 277011A is an antagonist of the dopamine D3 receptor (pKi = 8.0) that is at least 100-fold selective for D3 over other monoamine receptors (pKis = 6.0, 5.0, and 2, 5-HT1D and 5-HT1B respectively).{31910,31909,31908} It has high oral bioavailability and enters the central nervous system of the rat.{31910} SB 277011A has been shown to have potential benefits in animal models of schizophrenia and Parkinson’s disease.{31909,31907}
Brand:CaymanSKU:11982 - 25 mgAvailable on backorder
SB 277011A is an antagonist of the dopamine D3 receptor (pKi = 8.0) that is at least 100-fold selective for D3 over other monoamine receptors (pKis = 6.0, 5.0, and 2, 5-HT1D and 5-HT1B respectively).{31910,31909,31908} It has high oral bioavailability and enters the central nervous system of the rat.{31910} SB 277011A has been shown to have potential benefits in animal models of schizophrenia and Parkinson’s disease.{31909,31907}
Brand:CaymanSKU:11982 - 5 mgAvailable on backorder
The anaphylatoxin C3a induces a range of responses by activating its G protein-coupled receptor, C3aR, resulting in calcium mobilization.{25900} SB 290157 is a non-peptide antagonist of C3aR, competitively blocking C3a binding with an IC50 value of 200 nM.{25894} It potently inhibits a wide variety of C3a-induced responses in cells, including calcium increase in human neutrophils (IC50 = 28 nM) and ATP release from guinea pig platelets (IC50 = 30 nM).{25894} SB 290157 is also effective in vivo, reducing inflammation in a variety of animal models.{25894,25897,25895} It also significantly reduces or reverses diet-induced obesity in rats and accelerates the mobilization of hematopoietic progenitor cells to the peripheral blood in mice.{25896,25898} Notably, SB 290157 has C3aR agonist activity in some cell systems.{25893,25899}
Brand:CaymanSKU:- The anaphylatoxin C3a induces a range of responses by activating its G protein-coupled receptor, C3aR, resulting in calcium mobilization.{25900} SB 290157 is a non-peptide antagonist of C3aR, competitively blocking C3a binding with an IC50 value of 200 nM.{25894} It potently inhibits a wide variety of C3a-induced responses in cells, including calcium increase in human neutrophils (IC50 = 28 nM) and ATP release from guinea pig platelets (IC50 = 30 nM).{25894} SB 290157 is also effective in vivo, reducing inflammation in a variety of animal models.{25894,25897,25895} It also significantly reduces or reverses diet-induced obesity in rats and accelerates the mobilization of hematopoietic progenitor cells to the peripheral blood in mice.{25896,25898} Notably, SB 290157 has C3aR agonist activity in some cell systems.{25893,25899}
Brand:CaymanSKU:- The anaphylatoxin C3a induces a range of responses by activating its G protein-coupled receptor, C3aR, resulting in calcium mobilization.{25900} SB 290157 is a non-peptide antagonist of C3aR, competitively blocking C3a binding with an IC50 value of 200 nM.{25894} It potently inhibits a wide variety of C3a-induced responses in cells, including calcium increase in human neutrophils (IC50 = 28 nM) and ATP release from guinea pig platelets (IC50 = 30 nM).{25894} SB 290157 is also effective in vivo, reducing inflammation in a variety of animal models.{25894,25897,25895} It also significantly reduces or reverses diet-induced obesity in rats and accelerates the mobilization of hematopoietic progenitor cells to the peripheral blood in mice.{25896,25898} Notably, SB 290157 has C3aR agonist activity in some cell systems.{25893,25899}
Brand:CaymanSKU:- The anaphylatoxin C3a induces a range of responses by activating its G protein-coupled receptor, C3aR, resulting in calcium mobilization.{25900} SB 290157 is a non-peptide antagonist of C3aR, competitively blocking C3a binding with an IC50 value of 200 nM.{25894} It potently inhibits a wide variety of C3a-induced responses in cells, including calcium increase in human neutrophils (IC50 = 28 nM) and ATP release from guinea pig platelets (IC50 = 30 nM).{25894} SB 290157 is also effective in vivo, reducing inflammation in a variety of animal models.{25894,25897,25895} It also significantly reduces or reverses diet-induced obesity in rats and accelerates the mobilization of hematopoietic progenitor cells to the peripheral blood in mice.{25896,25898} Notably, SB 290157 has C3aR agonist activity in some cell systems.{25893,25899}
Brand:CaymanSKU:-
SB 297006 is an antagonist of C-C chemokine receptor 3 (CCR3; IC50 = 39 nM), which normally is activated by eotaxin, eotaxin-3, MCP-3, MCP-4, RANTES, and MIP-1δ.{32621} It is at least 250-fold selective for CCR3 over a panel of other chemokine receptors. SB 297006 blocks CCR3-mediated calcium mobilization induced by eotaxin, eotaxin-2, and MCP-4 in transfected cells.{32621} It suppresses antigen-induced accumulation of Th2 lymphocytes and eosinophils in lungs of mice when delivered subcutaneously (100 mg/kg).{32620}
Brand:CaymanSKU:11964 - 1 mgAvailable on backorder
SB 297006 is an antagonist of C-C chemokine receptor 3 (CCR3; IC50 = 39 nM), which normally is activated by eotaxin, eotaxin-3, MCP-3, MCP-4, RANTES, and MIP-1δ.{32621} It is at least 250-fold selective for CCR3 over a panel of other chemokine receptors. SB 297006 blocks CCR3-mediated calcium mobilization induced by eotaxin, eotaxin-2, and MCP-4 in transfected cells.{32621} It suppresses antigen-induced accumulation of Th2 lymphocytes and eosinophils in lungs of mice when delivered subcutaneously (100 mg/kg).{32620}
Brand:CaymanSKU:11964 - 10 mgAvailable on backorder
SB 297006 is an antagonist of C-C chemokine receptor 3 (CCR3; IC50 = 39 nM), which normally is activated by eotaxin, eotaxin-3, MCP-3, MCP-4, RANTES, and MIP-1δ.{32621} It is at least 250-fold selective for CCR3 over a panel of other chemokine receptors. SB 297006 blocks CCR3-mediated calcium mobilization induced by eotaxin, eotaxin-2, and MCP-4 in transfected cells.{32621} It suppresses antigen-induced accumulation of Th2 lymphocytes and eosinophils in lungs of mice when delivered subcutaneously (100 mg/kg).{32620}
Brand:CaymanSKU:11964 - 25 mgAvailable on backorder
SB 297006 is an antagonist of C-C chemokine receptor 3 (CCR3; IC50 = 39 nM), which normally is activated by eotaxin, eotaxin-3, MCP-3, MCP-4, RANTES, and MIP-1δ.{32621} It is at least 250-fold selective for CCR3 over a panel of other chemokine receptors. SB 297006 blocks CCR3-mediated calcium mobilization induced by eotaxin, eotaxin-2, and MCP-4 in transfected cells.{32621} It suppresses antigen-induced accumulation of Th2 lymphocytes and eosinophils in lungs of mice when delivered subcutaneously (100 mg/kg).{32620}
Brand:CaymanSKU:11964 - 5 mgAvailable on backorder
SB-200646 is a dual antagonist of the serotonin (5-HT) receptor subtypes 5-HT2C (Ki = 125 nM in isolated rat cortex) and 5-HT2B (pA2 = 7.5 in rat stomach fundus preparations).{54226} It is selective for 5-HT2C and 5-HT2B over 5-HT1A, 5-HT2A, 5-HT1D, 5-HT3, benzodiazepine, GABAA, α1-, α2A-, α2B-, β1-, and β2-adrenergic, dopamine D1 and D2, and histamine H1 receptors (Kis = >10 µM for all). SB-200646 (20 and 40 mg/kg) reverses mCPP-induced hypophagia and decreases in social interaction time, indicating anxiolytic-like behavior, in rats.
Brand:CaymanSKU:30973 - 1 mgAvailable on backorder
SB-200646 is a dual antagonist of the serotonin (5-HT) receptor subtypes 5-HT2C (Ki = 125 nM in isolated rat cortex) and 5-HT2B (pA2 = 7.5 in rat stomach fundus preparations).{54226} It is selective for 5-HT2C and 5-HT2B over 5-HT1A, 5-HT2A, 5-HT1D, 5-HT3, benzodiazepine, GABAA, α1-, α2A-, α2B-, β1-, and β2-adrenergic, dopamine D1 and D2, and histamine H1 receptors (Kis = >10 µM for all). SB-200646 (20 and 40 mg/kg) reverses mCPP-induced hypophagia and decreases in social interaction time, indicating anxiolytic-like behavior, in rats.
Brand:CaymanSKU:30973 - 10 mgAvailable on backorder
SB-200646 is a dual antagonist of the serotonin (5-HT) receptor subtypes 5-HT2C (Ki = 125 nM in isolated rat cortex) and 5-HT2B (pA2 = 7.5 in rat stomach fundus preparations).{54226} It is selective for 5-HT2C and 5-HT2B over 5-HT1A, 5-HT2A, 5-HT1D, 5-HT3, benzodiazepine, GABAA, α1-, α2A-, α2B-, β1-, and β2-adrenergic, dopamine D1 and D2, and histamine H1 receptors (Kis = >10 µM for all). SB-200646 (20 and 40 mg/kg) reverses mCPP-induced hypophagia and decreases in social interaction time, indicating anxiolytic-like behavior, in rats.
Brand:CaymanSKU:30973 - 5 mgAvailable on backorder
The indole derivative SB-207266 is a selective and potent antagonist of the serotonin (5-HT) receptor 5-HT4 with a pA2 value of 10.6 ± 0.1.{34073, 34070} In COS7 cells, 100 nM SB-207266 inhibited 5-HT4 responses to 5-HT and reduced basal agonist-independent cAMP production.{34070} In several animal models, low concentrations of SB-207266 blocked exogenous 5-HT-mediated sensitization of intestinal peristalsis.{34073, 34072, 34071} In a dog model, SB-207266 (0.1–100 pg/kg) dose-dependently reduced responses to 5-HT, with an ID50 value of 1.3 pg/kg.{34073} SB-206226 (0.5 mg/kg/24 h) improved cardiac function in a rat model of congestive heart failure.{34069}
Brand:CaymanSKU:-Available on backorder
The indole derivative SB-207266 is a selective and potent antagonist of the serotonin (5-HT) receptor 5-HT4 with a pA2 value of 10.6 ± 0.1.{34073, 34070} In COS7 cells, 100 nM SB-207266 inhibited 5-HT4 responses to 5-HT and reduced basal agonist-independent cAMP production.{34070} In several animal models, low concentrations of SB-207266 blocked exogenous 5-HT-mediated sensitization of intestinal peristalsis.{34073, 34072, 34071} In a dog model, SB-207266 (0.1–100 pg/kg) dose-dependently reduced responses to 5-HT, with an ID50 value of 1.3 pg/kg.{34073} SB-206226 (0.5 mg/kg/24 h) improved cardiac function in a rat model of congestive heart failure.{34069}
Brand:CaymanSKU:-Available on backorder
The indole derivative SB-207266 is a selective and potent antagonist of the serotonin (5-HT) receptor 5-HT4 with a pA2 value of 10.6 ± 0.1.{34073, 34070} In COS7 cells, 100 nM SB-207266 inhibited 5-HT4 responses to 5-HT and reduced basal agonist-independent cAMP production.{34070} In several animal models, low concentrations of SB-207266 blocked exogenous 5-HT-mediated sensitization of intestinal peristalsis.{34073, 34072, 34071} In a dog model, SB-207266 (0.1–100 pg/kg) dose-dependently reduced responses to 5-HT, with an ID50 value of 1.3 pg/kg.{34073} SB-206226 (0.5 mg/kg/24 h) improved cardiac function in a rat model of congestive heart failure.{34069}
Brand:CaymanSKU:-Available on backorder
The indole derivative SB-207266 is a selective and potent antagonist of the serotonin (5-HT) receptor 5-HT4 with a pA2 value of 10.6 ± 0.1.{34073, 34070} In COS7 cells, 100 nM SB-207266 inhibited 5-HT4 responses to 5-HT and reduced basal agonist-independent cAMP production.{34070} In several animal models, low concentrations of SB-207266 blocked exogenous 5-HT-mediated sensitization of intestinal peristalsis.{34073, 34072, 34071} In a dog model, SB-207266 (0.1–100 pg/kg) dose-dependently reduced responses to 5-HT, with an ID50 value of 1.3 pg/kg.{34073} SB-206226 (0.5 mg/kg/24 h) improved cardiac function in a rat model of congestive heart failure.{34069}
Brand:CaymanSKU:-Available on backorder
Glycogen synthase kinase 3 (GSK3) is a serine/threonine protein kinase that is inhibited by an assortment of extracellular stimuli including insulin, growth factors, cell specification factors, and cell adhesion. SB-216763 is a potent and selective cell permeable ATP-competitive inhibitor of GSK3α with an IC50 value of 34 nM (similar potency for GSK3β).{15623} It stimulates glycogen synthesis in Chang human liver cells with an EC50 value of 3.6 µM and induces expression of a β-catenin-LEF/Tcf regulated reporter gene in HEK293 cells.{15623} SB-216763 protects primary neurons from death induced by the PI3-kinase pathway.{15622}
Brand:CaymanSKU:10010246 - 10 mgAvailable on backorder
Glycogen synthase kinase 3 (GSK3) is a serine/threonine protein kinase that is inhibited by an assortment of extracellular stimuli including insulin, growth factors, cell specification factors, and cell adhesion. SB-216763 is a potent and selective cell permeable ATP-competitive inhibitor of GSK3α with an IC50 value of 34 nM (similar potency for GSK3β).{15623} It stimulates glycogen synthesis in Chang human liver cells with an EC50 value of 3.6 µM and induces expression of a β-catenin-LEF/Tcf regulated reporter gene in HEK293 cells.{15623} SB-216763 protects primary neurons from death induced by the PI3-kinase pathway.{15622}
Brand:CaymanSKU:10010246 - 100 mgAvailable on backorder
Glycogen synthase kinase 3 (GSK3) is a serine/threonine protein kinase that is inhibited by an assortment of extracellular stimuli including insulin, growth factors, cell specification factors, and cell adhesion. SB-216763 is a potent and selective cell permeable ATP-competitive inhibitor of GSK3α with an IC50 value of 34 nM (similar potency for GSK3β).{15623} It stimulates glycogen synthesis in Chang human liver cells with an EC50 value of 3.6 µM and induces expression of a β-catenin-LEF/Tcf regulated reporter gene in HEK293 cells.{15623} SB-216763 protects primary neurons from death induced by the PI3-kinase pathway.{15622}
Brand:CaymanSKU:10010246 - 5 mgAvailable on backorder
Glycogen synthase kinase 3 (GSK3) is a serine/threonine protein kinase that is inhibited by an assortment of extracellular stimuli including insulin, growth factors, cell specification factors, and cell adhesion. SB-216763 is a potent and selective cell permeable ATP-competitive inhibitor of GSK3α with an IC50 value of 34 nM (similar potency for GSK3β).{15623} It stimulates glycogen synthesis in Chang human liver cells with an EC50 value of 3.6 µM and induces expression of a β-catenin-LEF/Tcf regulated reporter gene in HEK293 cells.{15623} SB-216763 protects primary neurons from death induced by the PI3-kinase pathway.{15622}
Brand:CaymanSKU:10010246 - 50 mgAvailable on backorder
The transduction of neurobehavioral effects by serotonin (5-hydroxy tryptamine; 5-HT) is mediated by at least seven major 5-HT receptor subtypes. SB-224289 is a potent 5-HT1B inverse agonist (pKi = 8.16) that displays >75-fold selectivity for human 5-HT1B over all other 5-HT receptors.{27920} It has been used to study the role of 5-HT1B receptors in cocaine self-administration and cocaine-seeking behavior.{27921}
Brand:CaymanSKU:-Out of stock
The transduction of neurobehavioral effects by serotonin (5-hydroxy tryptamine; 5-HT) is mediated by at least seven major 5-HT receptor subtypes. SB-224289 is a potent 5-HT1B inverse agonist (pKi = 8.16) that displays >75-fold selectivity for human 5-HT1B over all other 5-HT receptors.{27920} It has been used to study the role of 5-HT1B receptors in cocaine self-administration and cocaine-seeking behavior.{27921}
Brand:CaymanSKU:-Out of stock
The transduction of neurobehavioral effects by serotonin (5-hydroxy tryptamine; 5-HT) is mediated by at least seven major 5-HT receptor subtypes. SB-224289 is a potent 5-HT1B inverse agonist (pKi = 8.16) that displays >75-fold selectivity for human 5-HT1B over all other 5-HT receptors.{27920} It has been used to study the role of 5-HT1B receptors in cocaine self-administration and cocaine-seeking behavior.{27921}
Brand:CaymanSKU:-Out of stock
The transduction of neurobehavioral effects by serotonin (5-hydroxy tryptamine; 5-HT) is mediated by at least seven major 5-HT receptor subtypes. SB-224289 is a potent 5-HT1B inverse agonist (pKi = 8.16) that displays >75-fold selectivity for human 5-HT1B over all other 5-HT receptors.{27920} It has been used to study the role of 5-HT1B receptors in cocaine self-administration and cocaine-seeking behavior.{27921}
Brand:CaymanSKU:-Out of stock
Serotonin (5-hydroxytryptamine, 5-HT) is a neurotransmitter that activates specific receptors located primarily in the gut and central nervous system. SB-242084 is an antagonist of the 5-HT2C receptor (pKi = 9.0), with at least 100-fold more selectivity over other 5-HT, dopamine, or adrenergic receptors.{18221,18225} In vivo, it is brain penetrant and has significant anxiolytic activity, without sedative, proconvulsant, or hyperphagic properties.{18221} SB-242084 has been used extensively in animal research to evaluate, for example, 5-HT2C receptor agonists and neurotransmitter receptor interactions in mice.{18222,18223,18224}
Brand:CaymanSKU:10096 - 1 mgAvailable on backorder
Serotonin (5-hydroxytryptamine, 5-HT) is a neurotransmitter that activates specific receptors located primarily in the gut and central nervous system. SB-242084 is an antagonist of the 5-HT2C receptor (pKi = 9.0), with at least 100-fold more selectivity over other 5-HT, dopamine, or adrenergic receptors.{18221,18225} In vivo, it is brain penetrant and has significant anxiolytic activity, without sedative, proconvulsant, or hyperphagic properties.{18221} SB-242084 has been used extensively in animal research to evaluate, for example, 5-HT2C receptor agonists and neurotransmitter receptor interactions in mice.{18222,18223,18224}
Brand:CaymanSKU:10096 - 10 mgAvailable on backorder
Serotonin (5-hydroxytryptamine, 5-HT) is a neurotransmitter that activates specific receptors located primarily in the gut and central nervous system. SB-242084 is an antagonist of the 5-HT2C receptor (pKi = 9.0), with at least 100-fold more selectivity over other 5-HT, dopamine, or adrenergic receptors.{18221,18225} In vivo, it is brain penetrant and has significant anxiolytic activity, without sedative, proconvulsant, or hyperphagic properties.{18221} SB-242084 has been used extensively in animal research to evaluate, for example, 5-HT2C receptor agonists and neurotransmitter receptor interactions in mice.{18222,18223,18224}
Brand:CaymanSKU:10096 - 5 mgAvailable on backorder
SB-258585 is a potent, selective antagonist of the serotonin 5-HT6 receptor (pKi = 8.53).{30745} It displays over 100-fold selectivity for 5-HT6 over other 5-HT, dopamine, and α-adrenergic receptors. Radiolabeled forms of SB-258585 have been used to evaluate other potential ligands of the 5-HT6 receptor.{29781} SB-258585 has been used in cells and in animals to evaluate the role of the 5-HT6 receptor in diverse processes.{30747,30744,30746}
Brand:CaymanSKU:-Available on backorder
SB-258585 is a potent, selective antagonist of the serotonin 5-HT6 receptor (pKi = 8.53).{30745} It displays over 100-fold selectivity for 5-HT6 over other 5-HT, dopamine, and α-adrenergic receptors. Radiolabeled forms of SB-258585 have been used to evaluate other potential ligands of the 5-HT6 receptor.{29781} SB-258585 has been used in cells and in animals to evaluate the role of the 5-HT6 receptor in diverse processes.{30747,30744,30746}
Brand:CaymanSKU:-Available on backorder
SB-258585 is a potent, selective antagonist of the serotonin 5-HT6 receptor (pKi = 8.53).{30745} It displays over 100-fold selectivity for 5-HT6 over other 5-HT, dopamine, and α-adrenergic receptors. Radiolabeled forms of SB-258585 have been used to evaluate other potential ligands of the 5-HT6 receptor.{29781} SB-258585 has been used in cells and in animals to evaluate the role of the 5-HT6 receptor in diverse processes.{30747,30744,30746}
Brand:CaymanSKU:-Available on backorder
SB-258585 is a potent, selective antagonist of the serotonin 5-HT6 receptor (pKi = 8.53).{30745} It displays over 100-fold selectivity for 5-HT6 over other 5-HT, dopamine, and α-adrenergic receptors. Radiolabeled forms of SB-258585 have been used to evaluate other potential ligands of the 5-HT6 receptor.{29781} SB-258585 has been used in cells and in animals to evaluate the role of the 5-HT6 receptor in diverse processes.{30747,30744,30746}
Brand:CaymanSKU:-Available on backorder
The transduction of neurobehavioral effects by serotonin (5-hydroxy tryptamine; 5-HT) is mediated by at least seven major 5-HT receptor subtypes. SB-269970 is a potent 5-HT7A antagonist (pKi = 8.9) that demonstrates >50-fold binding selectivity over 5-HT5A and >250-fold selectivity over 5-HT1, 5-HT2, 5-HT4, 5-HT6, adrenergic α1, dopamine D2, and dopamine D3 receptors.{27806} It is also reported to block adrenergic α2 receptors in guinea pig vas deferens.{27807} SB-269970 has been used to target the 5-HT7 receptor in the study of schizophrenia-like cognitive deficits.{27808}
Brand:CaymanSKU:-Out of stock
The transduction of neurobehavioral effects by serotonin (5-hydroxy tryptamine; 5-HT) is mediated by at least seven major 5-HT receptor subtypes. SB-269970 is a potent 5-HT7A antagonist (pKi = 8.9) that demonstrates >50-fold binding selectivity over 5-HT5A and >250-fold selectivity over 5-HT1, 5-HT2, 5-HT4, 5-HT6, adrenergic α1, dopamine D2, and dopamine D3 receptors.{27806} It is also reported to block adrenergic α2 receptors in guinea pig vas deferens.{27807} SB-269970 has been used to target the 5-HT7 receptor in the study of schizophrenia-like cognitive deficits.{27808}
Brand:CaymanSKU:-Out of stock
The transduction of neurobehavioral effects by serotonin (5-hydroxy tryptamine; 5-HT) is mediated by at least seven major 5-HT receptor subtypes. SB-269970 is a potent 5-HT7A antagonist (pKi = 8.9) that demonstrates >50-fold binding selectivity over 5-HT5A and >250-fold selectivity over 5-HT1, 5-HT2, 5-HT4, 5-HT6, adrenergic α1, dopamine D2, and dopamine D3 receptors.{27806} It is also reported to block adrenergic α2 receptors in guinea pig vas deferens.{27807} SB-269970 has been used to target the 5-HT7 receptor in the study of schizophrenia-like cognitive deficits.{27808}
Brand:CaymanSKU:-Out of stock
The transduction of neurobehavioral effects by serotonin (5-hydroxy tryptamine; 5-HT) is mediated by at least seven major 5-HT receptor subtypes. SB-269970 is a potent 5-HT7A antagonist (pKi = 8.9) that demonstrates >50-fold binding selectivity over 5-HT5A and >250-fold selectivity over 5-HT1, 5-HT2, 5-HT4, 5-HT6, adrenergic α1, dopamine D2, and dopamine D3 receptors.{27806} It is also reported to block adrenergic α2 receptors in guinea pig vas deferens.{27807} SB-269970 has been used to target the 5-HT7 receptor in the study of schizophrenia-like cognitive deficits.{27808}
Brand:CaymanSKU:-Out of stock
SB-271046 is an orally-available antagonist of the serotonin (5-hydroxytryptamine, or 5-HT; Item No. 14332) receptor 5-HT6 (pKi = 9.02-8.92).{29779,29781} It is at least 100-fold selective for 5-HT6 over other 5-HT receptors, as well as 55 other receptors, enzymes, and ion channels.{29781} While it does not alter basal levels of 5-HT, dopamine, or noradrenaline, SB-271046 produces a significant increase in extracellular levels of glutamate and aspartate within the frontal cortex.{29780} It has been used to evaluate the role of 5-HT6 in learning and memory.{29782}
Brand:CaymanSKU:-Available on backorder
SB-271046 is an orally-available antagonist of the serotonin (5-hydroxytryptamine, or 5-HT; Item No. 14332) receptor 5-HT6 (pKi = 9.02-8.92).{29779,29781} It is at least 100-fold selective for 5-HT6 over other 5-HT receptors, as well as 55 other receptors, enzymes, and ion channels.{29781} While it does not alter basal levels of 5-HT, dopamine, or noradrenaline, SB-271046 produces a significant increase in extracellular levels of glutamate and aspartate within the frontal cortex.{29780} It has been used to evaluate the role of 5-HT6 in learning and memory.{29782}
Brand:CaymanSKU:-Available on backorder
SB-271046 is an orally-available antagonist of the serotonin (5-hydroxytryptamine, or 5-HT; Item No. 14332) receptor 5-HT6 (pKi = 9.02-8.92).{29779,29781} It is at least 100-fold selective for 5-HT6 over other 5-HT receptors, as well as 55 other receptors, enzymes, and ion channels.{29781} While it does not alter basal levels of 5-HT, dopamine, or noradrenaline, SB-271046 produces a significant increase in extracellular levels of glutamate and aspartate within the frontal cortex.{29780} It has been used to evaluate the role of 5-HT6 in learning and memory.{29782}
Brand:CaymanSKU:-Available on backorder
SB-271046 is an orally-available antagonist of the serotonin (5-hydroxytryptamine, or 5-HT; Item No. 14332) receptor 5-HT6 (pKi = 9.02-8.92).{29779,29781} It is at least 100-fold selective for 5-HT6 over other 5-HT receptors, as well as 55 other receptors, enzymes, and ion channels.{29781} While it does not alter basal levels of 5-HT, dopamine, or noradrenaline, SB-271046 produces a significant increase in extracellular levels of glutamate and aspartate within the frontal cortex.{29780} It has been used to evaluate the role of 5-HT6 in learning and memory.{29782}
Brand:CaymanSKU:-Available on backorder
SB-328437 is a nonpeptide chemokine (C-C motif) receptor 3 (CCR3) antagonist (IC50 = 4.5 nM in a radioligand binding assay).{32621} It is selective for CCR3 over chemokine (C-X-C motif) receptor 1 (CXCR1), CXCR2, CCR7, complement 3a receptor (C3aR), and C5aR (IC50s = >27, >27, >33, >10, and >10 µM, respectively). SB-328437 (3.3-1,000 nM) inhibits calcium mobilization induced by chemokine (C-C motif) ligand 11 (CCL11), CCL24, and CCL13 in RBL-2H3-CCR3 cells and eosinophils. In vivo, SB-328437 reduces pulmonary Ccr3 mRNA expression, the number of eosinophils and monocytes in bronchoalveolar lavage fluid (BALF), and pulmonary IL-4 and TNF-α levels in a mouse model of asthma.{49498}
Brand:CaymanSKU:29677 - 1 mgAvailable on backorder