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GSK205

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Chemical Structure| 1263068-83-2 同义名 : -
CAS号 : 1263068-83-2
货号 : A1196015
分子式 : C24H25BrN4S
纯度 : 99%+
分子量 : 481.451
MDL号 : MFCD28160554
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(519.26 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 GSK205 is a potent and selective TRPV4 antagonist with an IC50 value of 4.19 μM for inhibition of TRPV4-mediated Ca2+ influx[1][2].Acting at a concentration of 5 μM for 4 days, GSK205 leads to an increase in the expression of thermogenic genes, such as for example Mcp1, Mip1α, Mcp3, Rantes, and Vcam, and is accompanied by a decrease in pro-inflammatory gene programs[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.08mL

0.42mL

0.21mL

10.39mL

2.08mL

1.04mL

20.77mL

4.15mL

2.08mL
参考文献

[1]Ye L, et al. TRPV4 is a regulator of adipose oxidative metabolism, inflammation, and energy homeostasis. Cell. 2012 Sep 28;151(1):96-110.

[2]Kanju P, et al. Small molecule dual-inhibitors of TRPV4 and TRPA1 for attenuation of inflammation and pain. Sci Rep. 2016 Jun 1;6:26894.