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TCS 3035
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。
TCS 3035图片
CAS NO:871085-49-3
规格:98%
分子量:279.27
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
GPR35 agonist
CAS:871085-49-3
分子式:C12H9NO5S
分子量:279.27
纯度:98%
存储:Store at -20°C

Background:

Target: GPR35


IC50: N/A


TCS3035, a GPR35 agonist, shows significantly high potency at rat and human GPR35 orthologs with pEC50 values of 5.13 and 5.86, respectively [1]. G protein-coupled receptors (GPCRs) are the largest and most studied group of transmembrane polypeptides. GPR35 is a poorly characterized G protein-coupled receptor that plays an important role in immune-modulation, gastric function and the regulation of insulin secretion. GPR35 is predominantly expressed in the gastro-intestinal tract and immune tissues. The tryptophan metabolite kynurenic acid has been suggested to be the endogenous ligand for GPR35 [1].


In vitro: Mutation to alanine of the conserved arginine at position 3.36 in either FLAG-hGPR35-eYFP or FLAG-rGPR35-eYFP resulted in a complete loss of agonist function of TCS3035 [1]. In addition, TCS3035-induced internalization of GPR35 is correlated with TCS3035 potency in receptor-β-arrestin-2 interaction BRET assays. Mutation to alanine of tyrosine 3.32 in transmembrane domain III abolished β-arrestin-2 recruitment in response to TCS3035 [1].


In vivo: N/A


Reference:
1.  Jenkins L, Alvarez-Curto E, Campbell K, de Munnik S, Canals M, Schlyer S, et al. Agonist activation of the G protein-coupled receptor GPR35 involves transmembrane domain III and is transduced via Galpha(1)(3) and beta-arrestin-2. Br J Pharmacol. 2011;162(3):733-48.