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GSK205 is a potent, selective TRPV4 antagonist with an IC50 of 4.19? μM for inhibiting TRPV4-mediated Ca2+ influx[1][2]. | [Biological Activity]
GSK205 is a potent and selective TRPV4 antagonist with IC50 of 4.19 μM, inhibits TRPV4-mediated Ca2+ influx. | [in vitro]
GSK205 HBr (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. < /p> 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 decre ase in the proinflammatory gene program. | | [in vivo]
GSK205 HBr (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 . It 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.
It has a relatively short half-life of 2 hours in the plasma and adipose tissues. | Animal Model: | Male C57BL/ 6J mice with high-fat diet | | Dosage: | 10 mg/kg | < /tr> | Administration: | Intraperitoneal injection; twice daily; for 7 days < /td> | | 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. | | [storage]
Store at -20°C | [References]
[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. DOI:10.1016/j.cell.2012.08.034
[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. DOI:10.1038/srep26894 |
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