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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
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
TCS 3035 (compound 10) 是一种有效的 GPR35 激动剂,pEC50 为 5.86。
Cas No.871085-49-3
化学名(Z)-2-(4-((2,4-dioxothiazolidin-5-ylidene)methyl)phenoxy)acetic acid
Canonical SMILESO=C(/C(S1)=C/C2=CC=C(OCC(O)=O)C=C2)NC1=O
分子式C12H9NO5S
分子量279.27
溶解度<27.93mg/ml in DMSO
储存条件Store at -20℃
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

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.