| Identification | Back Directory | [Name]
TCS-3035 | [CAS]
871085-49-3 | [Synonyms]
TCS-3035
2-[4-[(Z)-(2,4-Dioxo-5-thiazolidinylidene)methyl]phenoxyacetic acid
(Z)-2-(4-((2,4-dioxothiazolidin-5-ylidene)methyl)phenoxy)acetic acid | [Molecular Formula]
C12H9NO5S | [MDL Number]
MFCD01835940 | [MOL File]
871085-49-3.mol | [Molecular Weight]
279.27 |
| Hazard Information | Back Directory | [Uses]
TCS 3035 is a potent and selective GPR35 agonist. | [Biological Activity]
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]. | [target]
gpr35 | [storage]
Store at -20°C | [References]
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. |
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