For research use only. Not for therapeutic Use.
CID 2745687 acts as a specific, reversible and competitive GPR35 antagonist with a Ki of 12.8 nM[1].
For ERK1/2 phosphorylation with 1 μM Pamoic acid as the agonist, the CID 2745687 (CID2745687) Ki is 18 nM[1].
CID 2745687 (CID-2745687) is a potent antagonist in β-arrestin-2 interaction assays only at human GPR35[2].
Using the BRET-based GPR35-β-arrestin-2 interaction assay and an EC80 concentration of Zaprinast (20 μM) as agonist, CID 2745687 behaved as a moderately potent, concentration-dependent antagonist at human GPR35 with pIC50=6.70±0.09[2].
CID 2745687 (pIC50=6.27±0.08) fully reverses the agonist action of Cromolyn disodium [2].
CID 2745687 (CID2745687; 1 mg/kg; administrated orally every day for the last 4 weeks), a specific GPR35 antagonist, reverses Lodoxamide-mediated anti-fibrotic effects[3].
| Catalog Number | R041663 |
| CAS Number | 264233-05-8 |
| Synonyms | methyl 5-[(E)-(tert-butylcarbamothioylhydrazinylidene)methyl]-1-(2,4-difluorophenyl)pyrazole-4-carboxylate |
| Molecular Formula | C17H19F2N5O2S |
| Purity | ≥95% |
| InChI | InChI=1S/C17H19F2N5O2S/c1-17(2,3)22-16(27)23-20-9-14-11(15(25)26-4)8-21-24(14)13-6-5-10(18)7-12(13)19/h5-9H,1-4H3,(H2,22,23,27)/b20-9+ |
| InChIKey | CYNLZIBKERMMOA-AWQFTUOYSA-N |
| SMILES | CC(C)(C)NC(=S)NN=CC1=C(C=NN1C2=C(C=C(C=C2)F)F)C(=O)OC |
| Reference | [1]. Pingwei Zhao, et al. Targeting of the orphan receptor GPR35 by pamoic acid: a potent activator of extracellular signal-regulated kinase and β-arrestin2 with antinociceptive activity. Mol Pharmacol. 2010 Oct;78(4):560-8. [2]. Laura Jenkins, et al. Antagonists of GPR35 display high species ortholog selectivity and varying modes of action. J Pharmacol Exp Ther. 2012 Dec;343(3):683-95. [3]. Mi-Jeong Kim, et al. Lodoxamide Attenuates Hepatic Fibrosis in Mice: Involvement of GPR35. Biomol Ther (Seoul). 2019 Jun 13;28(1):92-97. |
