| Bioactivity | CID 2745687 acts as a specific, reversible and competitive GPR35 antagonist with a Ki of 12.8 nM[1]. | ||||||||||||
| Invitro | 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]. | ||||||||||||
| In Vivo | 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]. Animal Model: | ||||||||||||
| Name | CID 2745687 | ||||||||||||
| CAS | 264233-05-8 | ||||||||||||
| Formula | C17H19F2N5O2S | ||||||||||||
| Molar Mass | 395.43 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| 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. |