CAS:942206-85-1GSK1016790A

Synonyms: GSK-101

GSK1016790A is a potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34nM in choroid plexus epithelial cells.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

技术信息

CAS号

942206-85-1

储存条件

分子式

C28H32Cl2N4O6S2

运输

蓝冰

分子量

655.61

别名

GSK-101

溶解度

动物实验配方

生物活性

描述GSK1016790A is a potent TRPV4 agonist with EC50 values of 18nM and 2.1nM for eliciting Ca²⁺ influx mediated by TRPV4 in mouse and HEK cells expressed hTRPV4, respectively. GSK1016790A concentration-dependently activated TRPV4 whole-cell currents at concentrations>1nM, much potent than TRPV4 activator 4α-PDD. GSK1016790A at concentration of 100nM increased TRPV4-mediated Ca²⁺ levels in INS-1E cells. As it is reported that TRPV4 is implicated in controlling peripheral insulin sensitivity, insulin secretion and apoptosis of pancreatic beta cells, insulin mRNA expression could be increased post 1-3h but be suppressed after 24h. Increased ERK1/2 phosphorylation and NO production but not ROS production, could be observed at 10min and 24h post treatment, respectively. GSK1016790A at 100nM increased insulin mRNA levels after 3 h without inducing cytotoxicity after 24 h.
动物研究
剂量
Rat: 20 μg/kg, 40 μg/kg^[3] (i.v.), 0.01 mg/kg - 0.2 mg/kg^[4] (i.v.), 0.025 mg/kg^[5] (i.v.); 10 mg/kg^[6] (p.o.)

给药途径
i.v., p.o.

动物研究
剂量	Rat: 20 μg/kg, 40 μg/kg^[3] (i.v.), 0.01 mg/kg - 0.2 mg/kg^[4] (i.v.), 0.025 mg/kg^[5] (i.v.); 10 mg/kg^[6] (p.o.)
给药途径	i.v., p.o.