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抑制剂描述:

产品名称:GSK1016790A

产品别名:见爱必信官网

英文别名:GSK1016790A

靶点:TRP Channel

CAS:942206-85-1

纯度:>98 %

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:GSK1016790A (GSK101) is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34nM in choroid plexus epithelial cells.

溶解性:DMSO : ≥ 33 mg/mL (50.33 mM)

体外研究:

GSK1016790A elicits Ca²⁺ influx in mouse and human TRPV4 expressing HEK cells (EC₅₀ values of 18 and 2.1 nM, respectively), and evokes a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM. It stimulates TRPV4 in multiple cell types including endothelial cells, urinary smooth muscle cells, urothelial cells and HEK-293 cells over-expressing TRPV4. GSK1016790A specifically activates TRPV4 channels, leading to a rapid partial desensitization and downregulation of the channel expression on the plasma membrane.

体内研究:GSK1016790A can produce marked decreases in systemic vascular resistance and pulmonary vascular resistance under high pulmonary vascular tone conditions.The activation of TRPV4 by GSK1016780A leads to vasodilation, vascular leakage, and tissue hemorrhage.

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