GSK205
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- CAS号:
- 1263068-83-2
- 英文名:
- GSK205 HBr
- 英文别名:
- GSK205;GSK205 HBr;N-(4-(2-(Benzyl(methyl)amino)ethyl)phenyl)-5-(pyridin-3-yl)thiazol-2-amine hydrobromide
- 中文名:
- GSK205
- 中文别名:
- 化合物 T11480;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
- CBNumber:
- CB25494080
- 分子式:
- C24H25BrN4S
- 分子量:
- 481.46
- MOL File:
- 1263068-83-2.mol
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GSK205化学性质
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: 250 mg/mL (519.26 mM)
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GSK205性质、用途与生产工艺
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 (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:
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T3-F442A adipocytes
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Concentration:
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5 μM
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Incubation Time:
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4 days
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Result:
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Resulted in increased expression of thermogenic genes and is also accompanied by a decrease in the proinflammatory gene program.
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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:
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Male C57BL/6J mice with high-fat diet
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Dosage:
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10 mg/kg
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Administration:
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Intraperitoneal injection; twice daily; for 7 days
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Result:
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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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GSK205
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/01/25 | HY-120691A | GSK205 | | 1 mg | 863元 |
2024/01/25 | HY-120691A | GSK205 GSK205 | 1263068-83-2 | 5mg | 1900元 |
1263068-83-2, GSK205 相关搜索:
- 化合物 T11480
- 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
- 1263068-83-2
- N-(4-(2-(Benzyl(methyl)amino)ethyl)phenyl)-5-(pyridin-3-yl)thiazol-2-amine hydrobromide
- GSK205
- GSK205 HBr