GSK205

GSK205 是一种高效的，选择性的 TRPV4 拮抗剂，IC50 值为 4.19 μM，可抑制 TRPV4 介导的 Ca2+ 内流。

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库存: 现货

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1mg

￥550.00

440.00

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5mg

￥2062.00

1650.00

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10mg

￥3600.00

2880.00

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25mg

￥7662.00

6130.00

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50mg

￥12825.00

10260.00

- +
100mg

￥22437.00

17950.00

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200mg

￥0.00

0.00

- +
500mg

￥0.00

0.00

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Background

GSK205 is a potent, selective TRPV4 antagonist with an IC50 of 4.19 μM for inhibiting TRPV4-mediated Ca2+ influx[1][2].

GSK205 (100 μM) potently antagonizes TRPV4 in 3T3-F442A adipocytes, as it effectively blocks the calcium influx caused by TRPV4 agonist[1].GSK205 (5 μM; 4 days; T3-F442A adipocytes) treatment results in increases expression of thermogenic genes (Mcp1, Mip1α, Mcp3, Rantes and Vcam, et al.) and is also accompanied by a decrease in the proinflammatory gene program. This shift resembles the gene expression changes seen in TRPV4-deficient adipocytes[1]. RT-PCR[1] Cell Line: T3-F442A adipocytes

GSK205 (10 mg/kg; intraperitoneal injection; twice daily; for 7 days; for 4 weeks; male C57BL/6J mice) treatment shows significantly increases expression of thermogenic genes such as Ucp1, Pgc1a, Cidea and Cox8b. GSK205 treatment causes a reduced expression of the proinflammatory chemokines, macrophage marker and Tnfa in the EPI fat. GSK205 treatment significantly improves glucose tolerance in diet-induced obese (DIO) mice. There are no apparent sign of sickness or weight loss[1]. GSK205 has a relatively short half-life of 2 hours in the plasma and adipose tissues[1]. Animal Model: Male C57BL/6J mice with high-fat diet[1]

[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.