化合物GSK1016790A T6848

Product Introduction
Bioactivity


英文名: GSK1016790A

描述: GSK1016790A (GSK101) 是选择性瞬时受体电位香草酸 4 通道激活剂，可引起 HEK 细胞中 Ca2+流入并升高细胞内 Ca2+。

细胞实验: CPECs are treated for 20 minutes with vehicle(DMSO), 10 nM GSK, or 10 nM GSK following the pretreatment with 1 mM HC. Then the cells are fixed and stained with Coomassie Brilliant Blue.(Only for Reference)

体外活性: 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[1]. 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[2].

体内活性: GSK1016790A在高肺血管张力条件下能显著降低全身血管阻力和肺血管阻力[3]。通过激活TRPV4，GSK1016780A引起血管舒张、血管渗漏和组织出血[4]。

存储条件: store at low temperaturePowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 58 mg/mL(88.5 mM)
DMSO : 93 mg/mL (141.9 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: GSK1016790A | inhibit | Ca2+ channels | Inhibitor | embryonic | GSK-101 | GSK-1016790A | Ca channels | HEK | vanilloid | transient | potential | receptor | GSK 101 | TRP Channel | kidney | Calcium Channel | human | Transient receptor potential channels

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相关库: Ion Channel Inhibitor Library | Anti-Hypertension Compound Library | Calcium Channel Compound Library | Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Metabolism Compound Library | Reprogramming Compound Library | Anti-Cardiovascular Disease Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途