GSK205
- CAS号:1263068-83-2
- 英文名:GSK205 HBr
- 中文名:GSK205
- CBNumber:CB25494080
- 分子式:C24H25BrN4S
- 分子量:481.46
- MOL File:1263068-83-2.mol
- 储存条件 :Store at -20°C
- 溶解度 :DMSO: 250 mg/mL (519.26 mM)
- 形态 :Solid
- 颜色 :Light yellow to yellow
GSK205性质、用途与生产工艺
- 生物活性 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。
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靶点
IC50: 4.19 μM (TRPV4)
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体外研究
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. -
体内研究
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.
- 更新日期：2024/04/30
- 产品编号：HY-120691A
- 产品名称：GSK205
- CAS编号：
- 包装：1 mg
- 价格：863元
- 更新日期：2024/04/30
- 产品编号：HY-120691A
- 产品名称：GSK205 GSK205
- CAS编号：1263068-83-2
- 包装：5mg
- 价格：1900元
- 公司名称：TargetMol Chemicals Inc.
- 联系电话：+1-781-999-5354 +1-00000000000
- 电子邮件：marketing@targetmol.com
- 国家：美国
- 产品数：19892
- 优势度：58
- 公司名称：Aladdin Scientific
- 联系电话：+1-+1(833)-552-7181
- 电子邮件：sales@aladdinsci.com
- 国家：美国
- 产品数：52927
- 优势度：58
- 公司名称：MedChemExpress
- 联系电话：--
- 电子邮件：sales@medchemexpress.com
- 国家：美国
- 产品数：6398
- 优势度：58
