CAS:1336960-13-4GSK2193874

GSK2193874 is a selective transient receptor potential vanilloid 4 (TRPV4) blocker with IC50 value of 0.04 μM.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

1336960-13-4

储存条件

分子式

C37H38BrF3N4O

运输

蓝冰

分子量

691.62

别名

溶解度

DMSO	150.0 mg/mL (216.9 mM)
Water	insoluble

动物实验配方

生物活性

描述GSK2193874 is a potent and selective TRPV4 blocker with 40nM and 2nM for hTRPV4 and rTRPV4, respectively, in a FLIPR assay. GSK2193874 dose-dependently blocked Ca²⁺ influx mediated by hTRPV4, rTRPV4 and hypotonic stretch hTRPV4 with IC50 values of 40nM, 2nM and 50nM, respectively. GSK2193874 at concentration of 100nM prevented the cellular contraction and detachment induced by TRPV4 activation with GSK1016790 in HUVECs, as well as eliminated reduced endothelial monolayer resistance by GSK1016790 in confluent HUVEC cultures. Also, it inhibited native endothelial TRPV4 currents induced by GSK1016790. Infusion with GSK2193874 37 and 219ng/min/kg inhibited formation of pulmonary edema in rat heart failure models without effect on blood pressure or heart rate.

动物研究

剂量

Rat: 30 mg/kg^[1] (p.o.); 0.3 mg/kg^[3] (i.v.) Mice: 5 mg/kg, 10 mg/kg^[4] (i.p.)

给药途径

p.o., i.v., i.p.

动物药代数据