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CID 2745687

Names

[ CAS No. ]:
264233-05-8

[ Name ]:
CID 2745687

[Synonym ]:
1H-Pyrazole-4-carboxylic acid, 1-(2,4-difluorophenyl)-5-[(E)-[2-[[(1,1-dimethylethyl)amino]thioxomethyl]hydrazinylidene]methyl]-, methyl ester
ASTA 3746
Ciclonium bromide
Methyl 1-(2,4-difluorophenyl)-5-[(E)-{[(2-methyl-2-propanyl)carbamothioyl]hydrazono}methyl]-1H-pyrazole-4-carboxylate
Cicloniumbromid

Biological Activity

[Description]:

CID 2745687 acts as a specific, reversible and competitive GPR35 antagonist with a Ki of 12.8 nM[1].

[Related Catalog]:

Research Areas >> Cardiovascular Disease
Signaling Pathways >> Others >> Others
Research Areas >> Inflammation/Immunology

[In Vitro]

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: Six-week-old male C57BL/6 mice[3] Dosage: 1 mg/kg Administration: Oral administration, every day for 4 weeks Result: Inhibited Lodoxamide-mediated protective effects.

[References]

[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.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
493.6±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C17H19F2N5O2S

[ Molecular Weight ]:
395.427

[ Flash Point ]:
252.3±31.5 °C

[ Exact Mass ]:
395.122742

[ PSA ]:
119.67000

[ LogP ]:
3.05

[ Vapour Pressure ]:
0.0±1.3 mmHg at 25°C

[ Index of Refraction ]:
1.591

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds