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264233-05-8

264233-05-8 structure
264233-05-8 structure
  • Name: CID 2745687
  • Chemical Name: Methyl 1-(2,4-difluorophenyl)-5-[(E)-{[(2-methyl-2-propanyl)carba mothioyl]hydrazono}methyl]-1H-pyrazole-4-carboxylate
  • CAS Number: 264233-05-8
  • Molecular Formula: C17H19F2N5O2S
  • Molecular Weight: 395.427
  • Catalog: Research Areas Cardiovascular Disease
  • Create Date: 2017-01-05 04:23:12
  • Modify Date: 2024-01-09 16:55:54
  • CID 2745687 acts as a specific, reversible and competitive GPR35 antagonist with a Ki of 12.8 nM[1].
Name Methyl 1-(2,4-difluorophenyl)-5-[(E)-{[(2-methyl-2-propanyl)carba mothioyl]hydrazono}methyl]-1H-pyrazole-4-carboxylate
Synonyms 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
Description CID 2745687 acts as a specific, reversible and competitive GPR35 antagonist with a Ki of 12.8 nM[1].
Related Catalog
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.
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
Hazard Codes Xi

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title: CAS No. 264233-05-8 | Chemsrc address: https://m.chemsrc.com/en/baike/1120207.html

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