GSK205
| 中文名称 | GSK205 |
|---|---|
| 中文同义词 | N-(4-(2-(苄基(甲基)氨基)乙基)苯基)-5-(吡啶-3-基)噻唑-2-胺氢溴酸盐;化合物 T11480 |
| 英文名称 | GSK205 HBr |
| 英文同义词 | GSK205 HBr;GSK205;N-(4-(2-(Benzyl(methyl)amino)ethyl)phenyl)-5-(pyridin-3-yl)thiazol-2-amine hydrobromide |
| CAS号 | 1263068-83-2 |
| 分子式 | C24H25BrN4S |
| 分子量 | 481.46 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1263068-83-2.mol |
| 结构式 |  |
GSK205 性质
| 储存条件 | Store at -20°C |
|---|---|
| 溶解度 | 二甲基亚砜：250 mg/mL（519.26 mM） |
IC50: 4.19 μM (TRPV4)
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.
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. |
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.
| 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. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-120691A | GSK205 | 1 mg | 863元 | |
| 2024/01/25 | HY-120691A | GSK205 GSK205 | 1263068-83-2 | 5mg | 1900元 |