Molecular structure of CID 2745687, CAS Number: 264233-05-8
CID 2745687 (CAS 264233-05-8)
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Alternate Names:
1-(2,4-Difluorophenyl)-5-[[2-[[(1,1 -dimethylehyl)amino]thioxomethyl]hydrazinylidene]methyl]-1H-pyrazole-4-carboxylic acid methyl ester
Application:
CID 2745687 is a reversible and competitive orphan receptor GPR35 antagonist
CAS Number:
264233-05-8
Molecular Weight:
395.43
Molecular Formula:
C17H19F2N5O2S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
CID 2745687 is a competitive, reversible antagonist of the orphan receptor GPR35. It blocks the GPR35-mediated increase in ERK1/2 phosphorylation and beta-arrestin recruitment induced by pamoic acid (sc-212523). It less potently blocks activation of GPR35 by zaprinast (IC50 = 160 nM) and shows about 57-fold selectivity for GPR35 over the related receptor GPR55 (IC50 = 9.08 µM). CID 2745687 is expressed predominantly in immune cells and in the gastrointestinal tract. In addition, it is overexpressed in gastric cancer cells.
CID 2745687 (CAS 264233-05-8) References
- Thieno[3,2-b]thiophene-2-carboxylic acid derivatives as GPR35 agonists. | Deng, H., et al. 2012. Bioorg Med Chem Lett. 22: 4148-52. PMID: 22572579
- Antagonists of GPR35 display high species ortholog selectivity and varying modes of action. | Jenkins, L., et al. 2012. J Pharmacol Exp Ther. 343: 683-95. PMID: 22967846
- PI3K/p110α inhibition selectively interferes with arterial thrombosis and neointima formation, but not re-endothelialization: potential implications for drug-eluting stent design. | Holy, EW., et al. 2014. Eur Heart J. 35: 808-20. PMID: 24334406
- G protein-coupled receptor 35: an emerging target in inflammatory and cardiovascular disease. | Divorty, N., et al. 2015. Front Pharmacol. 6: 41. PMID: 25805994
- The emerging pharmacology and function of GPR35 in the nervous system. | Mackenzie, AE. and Milligan, G. 2017. Neuropharmacology. 113: 661-671. PMID: 26232640
- G-Protein-Coupled Receptor 35 Mediates Human Saphenous Vein Vascular Smooth Muscle Cell Migration and Endothelial Cell Proliferation. | McCallum, JE., et al. 2015. J Vasc Res. 52: 383-95. PMID: 27064272
- Kynurenic acid and zaprinast induce analgesia by modulating HCN channels through GPR35 activation. | Resta, F., et al. 2016. Neuropharmacology. 108: 136-43. PMID: 27131920
- Exercised accelerated the production of muscle-derived kynurenic acid in skeletal muscle and alleviated the postmenopausal osteoporosis through the Gpr35/NFκB p65 pathway. | Shi, T., et al. 2022. J Orthop Translat. 35: 1-12. PMID: 35846727
- Changes in mRNA and miRNA expression in the prelimbic cortex related to depression-like syndrome induced by chronic social defeat stress in mice. | Chen, Y., et al. 2023. Behav Brain Res. 438: 114211. PMID: 36368442
- Aminosalicylates target GPR35, partly contributing to the prevention of DSS-induced colitis. | Otkur, W., et al. 2023. Eur J Pharmacol. 949: 175719. PMID: 37054942
- GPR35 antagonist CID-2745687 attenuates anchorage-independent cell growth by inhibiting YAP/TAZ activity in colorectal cancer cells. | Otkur, W., et al. 2023. Front Pharmacol. 14: 1126119. PMID: 37113762
- Label-free cell phenotypic assessment of the molecular mechanism of action of epidermal growth factor receptor inhibitors | Huayun Deng,a Chaoming Wangab and Ye Fang*a. 2013. RSC Adv.,.,3,: 10370-10378.
- Human Milk Oligosaccharide L-N-Tetraose Activates GPR35 on Vagal Afferent Neurons In Vitroand Reduces High Fat Diet-Induced Obesity in Male Mice | and Danielle L. Zumpano Brucia. May 2022. The FASEB Journal. Volume36, IssueS1.
Inhibitor of:
GPR35, and TDAG51.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
CID 2745687, 10 mg | sc-362725 | 10 mg | $200.00 | |||
CID 2745687, 50 mg | sc-362725A | 50 mg | $800.00 |