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GSK1016790A
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GSK1016790A图片
CAS NO:942206-85-1
规格:98%
分子量:655.6
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
TRPV4 agonist
CAS:942206-85-1
分子式:C28H32Cl2N4O6S2
分子量:655.6
纯度:98%
存储:Store at -20°C

Background:

GSK1016790A is a small molecule TRPV4 channel activator [1].


TRPV4 is a Ca2+-permeable, nonselective cation channel that has been involved in multiple physiologic functions, such as the regulation of systemic osmotic pressure, vascular function, skin barrier function, airway- and lung function, and in pain. The channel is activated by osmotic, mechanical, chemical cues and thermal changes. Channel activation can be sensitized by inflammation and injury. Mutations of TRPV4 may lead to premature osteoarthritis, skeletal dysplasias, and neurological motor function disorders [2].


In mouse and human TRPV4-expressing human embryonic kidney (HEK) cells, GSK1016790A elicited Ca2+ influx with the EC50 values of 18 and 2.1 nM, respectively. GSK1016790A dose-dependently evoked the activation of TRPV4 whole-cell currents at concentrations above 1 nM [1]. TRPV4 activation with GSK1016790A contracted TRPV4+/+ mouse bladders in vitro. Infusion of GSK1016790A into the bladders of TRPV4+/+ mice induced bladder overactivity with no effect in TRPV4-/- mice [1].


参考文献:
[1] Thorneloe K S, Sulpizio A C, Lin Z, 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]. Journal of Pharmacology and Experimental Therapeutics, 2008, 326(2): 432-442.
[2] Nilius B, Owsianik G, Voets T, et al.  Transient receptor potential cation channels in disease[J]. Physiological reviews, 2007, 87(1): 165-217.