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经验配方 C₂₀H₁₇F₃N₂O₂S 描述 概述 A pyrimidine small molecule that acts as a GLP-1 allosteric agonist that induces cAMP signaling in HEK293 cells expressing the GLP-1 receptor with EC50 = 0.66 µM and 99% efficacy (similar data with rat GLP-1 receptor), does not compete with radiolabelled GLP-1 in receptor binding assays, and is not active in cells expressing the GLP-2, GIP, PTH, or glucagon receptors. In rodent islets, insulin secretion increases in a dose-dependent and glucose-dependent manner, either alone or in an additive fashion when combined with the endogenous GLP-1 peptide. In vivo, this molecule exhibits insulinotropic effects when dosed at 10mg/kg in SD rats undergoing an IVGTT and a hyperglycemic clamp. It is also shown to increase insulin secretion in perifusion assays involving normal and diabetic human islets ex vivo, at concentrations between 1 and 10 µM. 产品目录编号 346007 品牌系列 Calbiochem®
同义词 4-(3-(benzyloxy)phenyl)-2-(ethylsulfinyl)-6-(trifluoromethyl)pyrimidine , Glucagon-Like Peptide 1 Receptor Agonist II, Compound B 参考 参考 Sloop, KW., et al. 2010. Diabetes. 59, 3099. 产品信息 形式 Off-white solid Hill配方 C₂₀H₁₇F₃N₂O₂S 化学配方 C₂₀H₁₇F₃N₂O₂S Molar Mass 406.42 结构配方图像 生物信息 纯度 >95% by HPLC 理化信息 溶解度 DMSO 储存和货运信息 货运代码 Shipped with Blue Ice or with Dry Ice
毒性 Standard Handling
储存 -20°C
避光 Protect from light
无需冷冻 No
特殊指南 Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. 包装信息 惰性气体下包装 Packaged under inert gas
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