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CAS No.: 942206-85-1

GSK1016790A Catalog No. CSN18613

Synonyms: GSK-101

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

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

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.
参考文献

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.

[1] Thorneloe KS, Sulpizio AC, et al. N-((1S)-1-{[4-((2S)-2-{[(2,4-dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide (GSK1016790A), a novel and potent transient receptor potential vanilloid 4 channel agonist induces urinary bladder contraction and hyperactivity: Part I. J Pharmacol Exp Ther. 2008 Aug;326(2):432-42.
[2] Billert M, Skrzypski M, et al. TRPV4 regulates insulin mRNA expression and INS-1E cell death via ERK1/2 and NO-dependent mechanisms. Cell Signal. 2017 Jul;35:242-249.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.5253 mL
- 7.6265 mL
- 15.2529 mL
- 5 mM
- 0.3051 mL
- 1.5253 mL
- 3.0506 mL
- 10 mM
- 0.1525 mL
- 0.7626 mL
- 1.5253 mL

技术信息

CAS号

942206-85-1

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H32Cl2N4O6S2

运输

蓝冰

分子量

655.61

别名

GSK-101

溶解度

DMSO	99.0 mg/mL (151.0 mM)
Water	Insoluble
Ethanol	100.0 mg/mL (152.5 mM)

动物实验配方

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GSK1016790A Catalog No. CSN18613

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