TCS 3035 |
カタログ番号GC15716 |
TCS 3035 (化合物 10) は、pEC50 が 5.86 の強力な GPR35 アゴニストです。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 871085-49-3
Sample solution is provided at 25 µL, 10mM.
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.
Average Rating: 5
(Based on Reviews and 16 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *