GSK205

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

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

RT-PCR Cell Line:T3-F442A adipocytes Concentration:5 μM Incubation Time:4 days Result:Resulted in increased expression of thermogenic genes and is also accompanied by a decrease in the proinflammatory gene program.

Animal Model:Male C57BL/6J mice with high-fat dietDosage:10 mg/kg Administration:Intraperitoneal injection; twice daily; for 7 days Result:Caused a reduced expression of the proinflammatory chemokines, macrophage marker and Tnfa in the EPI fat. Significantly improved glucose tolerance in diet-induced obese (DIO) mice.

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GPCR/G Protein

Calcium Channel

Calcium Channel | TRP/TRPV Channel

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1263068-83-2

481.45

C24H25BrN4S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 250 mg/mL (519.26 mM; 超声助溶 )

Br.CN(CCc1ccc(Nc2ncc(s2)-c2cccnc2)cc1)Cc1ccccc1

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(-20℃)

With Ice Pack

≥ 2 years