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GSK205

CAS No. : 1263068-83-2

MCE 站：GSK205

产品活性：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。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：TRP Channel

In Vitro: GSK205 (100 μM) potently antagonizes TRPV4 in 3T3-F442A adipocytes, as it effectively blocks the calcium influx caused by TRPV4 agonist.
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.

In Vivo: 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.
GSK205 has a relatively short half-life of 2 hours in the plasma and adipose tissues.

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