GSK205 is a potent, selective TRPV4 antagonist with an IC 50 of 4.19 μM for inhibiting TRPV4 -mediated Ca 2+ influx 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. RT-PCRCell 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. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male C57BL/6J mice with high-fat diet Dosage: 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. Form:Solid IC50& Target:IC50: 4.19 μM (TRPV4)
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GSK205
Dangerous GoodsCAS number：1263068-83-2 molecular formula：C24H25BrN4S
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| Chinese alias | - | ||
| English alias | gsk205 | F77231 | AKOS040733311 | N-[4-[2-[benzyl(methyl)amino]ethyl]phenyl]-5-pyridin-3-yl-1,3-thiazol-2-amine;hydrobromide | HY-120691A | 1263068-83-2 | AC-36949 | GSK 205 | N-(4-(2-(benzyl(methyl)amino)ethyl)phenyl)-5-(pyridin-3-yl)thiazol-2-amine hydr | ||
| CAS number | 1263068-83-2 | molecular formula | C24H25BrN4S |
| molecular weight | 481.5 g/mol | Exact mass | ≥99% |
| PSA | 69.300 Ų | logp | - |
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Safety information
pictogram：
GHS07
Signal word：
Warning
Hazard Statement：
H302: 吞食有害
Statement of Preventive Measures：
P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P330: 漱口 P301+P317: 如果被吞咽：请寻求医疗帮助。
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