GSK1016790ACAS号： 942206-85-1分子式： C28H32Cl2N4O6S2分子量： 655.61描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
| 产品描述 | |
| 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.
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| 纯度 |
>98%
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| 储存/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.
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| 基本信息 | |
| 别名 |
GSK-1016790A；GSK 1016790A
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| 外观 |
white solid
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| 可溶性/溶解性 |
DMSO : ≥ 33 mg/mL (50.33 mM)
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| 生物活性 | |
| 靶点 |
hTRPV4 ,mTRPV4
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| In vitro(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.
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| In vivo(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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分子结构图
