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TGR5 Receptor Agonist
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
TGR5 Receptor Agonist图片
CAS NO:1197300-24-5

TGR5 Receptor Agonist (CCDC) 是一种有效的武田 G 蛋白偶联受体 5 (TGR5；GPCR19) 激动剂，在 U2-OS 细胞和黑色素细胞中显示出提高的效力，pEC50 分别为 6.8 和 7.5。
Cas No.1197300-24-5
别名CCDC
化学名3-(2-chlorophenyl)-N-(4-chlorophenyl)-N,5-dimethylisoxazole-4-carboxamide
Canonical SMILESCC1=C(C(N(C2=CC=C(Cl)C=C2)C)=O)C(C3=CC=CC=C3Cl)=NO1
分子式C18H14Cl2N2O2
分子量361.22
溶解度DMF: 50 mg/ml,DMSO: 50 mg/ml,DMSO:PBS(pH 7.2) (1:4): 0.2 mg/ml,Ethanol: 30 mg/ml
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

TGR5 Receptor Agonist is a potent and selective agonist of TGR5 G-protein receptor with a pEC50 value of 6.8 in the U2-OS cell assay [1].

TGR5 Receptor Agonist has been shown the activated potency of TGR5 receptor with pEC50 values of 6.8 and 7.5 in the U2-OS cells and melanophire cells assay, respectively. In addition, TGR5 Receptor Agonist has been found to be fully specific for the human TGR5 receptor in the U2-OS and melanophore cell lines and also selective against other 7TM receptors. Besides, TGR5 Receptor Agonist has been reported to have physicochemical properties and no measurable activity against the common cytochrome P450 (CYP450) isoforms or hERG dofetilide binding with a pIC50 value of<4.3.

References:
[1] Evans KA1, Budzik BW, Ross SA, Wisnoski DD, Jin J, Rivero RA, Vimal M, Szewczyk GR, Jayawickreme C, Moncol DL, Rimele TJ, Armour SL, Weaver SP, Griffin RJ, Tadepalli SM, Jeune MR, Shearer TW, Chen ZB, Chen L, Anderson DL, Becherer JD, De Los Frailes M, Colilla FJ. Discovery of 3-aryl-4-isoxazolecarboxamides as TGR5 receptor agonists. J Med Chem. 2009 Dec 24;52(24):7962-5.

 
 
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