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CID-2745687 (CAS 264233-05-8) LS-H83

GPR35 antagonist
LS-H83-5 / 5 mg / $215
LS-H83-10 / 10 mg / $235
LS-H83-25 / 25 mg / $345
LS-H83-50 / 50 mg / $515
USA Shipment Only
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Description: GPR35 is a G protein-coupled receptor that is activated by kynurenic acid and 2-acyl lysophosphatidic acids (e.g., 2-oleoyl lysophosphatidic acid). It is expressed predominantly on immune cells, the brain, and in the gastrointestinal tract. GPR35 is overexpressed in gastric cancer cells. CID-2745687 is a reversible, competitive antagonist of GPR35, blocking activation by the synthetic agonist pamoic acid with a Ki value of 12.8 nM. It less potently blocks activation of GPR35 by zaprinast (IC50 = 160 nM). It shows ~57-fold selectivity for GPR35 over the related receptor GPR55 (IC50 = 9.08 µM). H83_ChemicalStructureImage.png
1-(2,4-difluorophenyl)-5-[[2-[[(1,1-dimethylethyl)amino]thioxomethyl]hydrazinylidene]methyl]-1H-pyrazole-4-carboxylic acid, methyl ester
biochemical, chemical, antagonist
A crystalline solid
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: GPR35 related products

Usage Information

CID-2745687 is supplied as a crystalline solid. A stock solution may be made by dissolving the CID-2745687 in the solvent of choice. CID-2745687 is soluble in DMSO at a concentration of approximately 10 mg/ml.

  1. Oka, S., Ota, R., Shima, M., et al. GPR35 is a novel lysophosphatidic acid receptor. Biochem. Biophys. Res. Commun. 395(2), 232-237 (2010).
  2. Wang, J., Simonavicius, N., Wu, X., et al. Kynurenic acid as a ligand for orphan G protein-coupled receptor GPR35. J. Biol. Chem. 281(31), 22021-22028 (2006).
  3. MacKenzie, A.E., Lappin, J.E., Taylor, D.L., et al. GPR35 as a novel therapeutic target. Front. Endocrinol. (Lausanne) 2, 68 (2011).
  4. O’Dowd, B.F., Nguyen, T., Marchese, A., et al. Discovery of three novel G-protein-coupled receptor genes. Genomics 47, 310-313 (1998).
  5. Okumura, S., Baba, H., Kumada, T., et al. Cloning of a G-protein-coupled receptor that shows an activity to transform NIH3T3 cells and is expressed in gastric cancer cells. Cancer Sci. 95(2), 131-135 (2004).
  6. Heynen-Genel, S., Dahl, R., Shi, S., et al. Selective GPR35 antagonists: Antagonists for the orphan receptor GPR35, in Probe Reports from the NIH Molecular Libraries Program, Probe 3, 1 (2011).

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