GPR35

G Protein-Coupled Receptor 35

GPR35 is an orphan G protein-coupled receptor (GPCR) that is highly expressed in the gastrointestinal (GI) tract, predominantly in colon epithelial cells (CEC). Kynurenic acid, a metabolite of L-tryptophan, has been proposed to be the endogenous ligand of GPR3535. Upon kynurenic acid-mediated GPR35 activation, β-arrestin 2 translocates to the cell membrane to mediate GPR35 internalization, resulting in receptor desensitization. Single nucleotide polymorphisms of GPR35 have linked this receptor to inflammatory bowel disease and primary sclerosing cholangitis, suggesting a role in gastrointestinal inflammation. In addition, in conjunction with previous findings that link agonism of GPR35 with significant reduction in nociceptive pain, GPR35 has emerged as a potential effector of regulation of mechanical sensitivity and analgesia of the Ret tyrosine kinase, and as a receptor involved in the transmission of anti-inflammatory effects of aspirin– potentially through affecting leukocyte rolling, adhesion and extravasation.

GPR35 Agonists (15)

GPR35 Related Products (17):

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-100806

Kynurenic acid	Agonist	99.58%
Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.

HY-W008613

Pamoic acid	Agonist	98.63%
Pamoic acid (Embonic acid) is a potent GPR35 agonist with an EC₅₀ of 79 nM. Pamoic acid exhibits neuroprotective and anti-inflammatory properties.

HY-B1816

Zaprinast	Agonist	99.95%
Zaprinast (M&B 22948) is a selective inhibitor of cGMP-selective Phosphodiesterase (PDE5). Zaprinast causes a significant increase in cGMP levels in myocytes. Zaprinast is a G protein-coupled receptor 35 (GPR35) agonist which activates rat GPR35 strongly and activates human GPR35 moderately. Zaprinast reduces vessel remodeling through antiproliferative and proapoptotic effects.

HY-107536

ML 145
ML 145 is a selective and competitive human GPR35/CXCR8 antagonist with an IC₅₀/EC₅₀ of 20.1 nM. ML 145 has over 1000-fold more selective for GPR35 compared to GPR55 (IC₅₀/EC₅₀=21.7 μM). ML 145 has no significant activity for GPR35 at either rodent ortholog.

HY-107537

CID 2745687	Agonist	98.07%
CID 2745687 acts as a specific, reversible and competitive GPR35 antagonist with a K_i of 12.8 nM.

HY-100806R

Kynurenic acid (Standard)	Agonist
Kynurenic acid (Standard) is the analytical standard of Kynurenic acid. This product is intended for research and analytical applications. Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.

HY-W010907

Pamoic acid disodium	Agonist	≥98.0%
Pamoic acid disodium is a potent GPR35 agonist with an EC₅₀ value of 79 nM. Pamoic acid disodium induces GPR35 internalization and activates ERK1/2 with EC₅₀ values of 22 nM and 65 nM, respectively. Pamoic acid disodium potently recruits β-arrestin2 to GPR35 and has an antinociceptive effect.

HY-100806S

Kynurenic acid-d₅	Agonist	98.35%
Kynurenic acid-d₅ is the deuterium labeled Kynurenic acid. Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8[1][2].

HY-107512

Kynurenic acid sodium	Agonist	99.79%
Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8.

HY-134801

CID1231538		99.74%
CID1231538, a benzothiazole analogue, is a potent GPR35 antagonist (IC₅₀=0.55 μM). GPR35 is a G protein-coupled receptor (GPCR).

HY-149190

GPR35 agonist 5	Agonist	98.86%
GPR35 agonist 5 (3,5-dinitro-bisphenol A; compound 6) is a weak GPR35 agonist. GPR35 agonist 5 arrests CHO-S cells at the G1/Gophase.

HY-15705

GPR35 agonist 2	Agonist	98.84%
GPR35 agonist 2 (compound 11) is a potent agonist of GPR35, with EC₅₀s of 26 and 3.2 nM in the β-arrestin and Ca²⁺ release assay, respectively.

HY-107538

YE120	Agonist
YE120 is a potent GPR35 agonist with an EC₅₀ of 32.5 nM.

HY-107539

GPR35 agonist 4	Agonist	≥99.0%
GPR35 agonist 4 (compound 10) is a potent GPR35 agonist with an pEC₅₀ of 5.86. GPR35 agonist 4 shows high potency human and rat GPR35. Mutation of arginine 3.36 eliminates agonist function of GPR35 agonist 4.

HY-101958

Tyrphostin 25	Agonist
Tyrphostin 25 (AG82) is a specific inhibitor of the EGFR tyrosine kinase. Tyrphostin 25 is also a GPR35 agonist with an IC₅₀ of 0.94 µM and an EC₅₀ of 5.3 µM.

HY-131728

GPR35 agonist 3	Agonist
GPR35 agonist 3 is a synthetic GPR35 agonist with an EC₅₀value of 1.4 μM. GPR35 agonist 3 can be used for the research of various diseases, such as gastric cancer, type 2 diabetes, cardiovascular diseases, immune system and peripheral nervous system.

HY-106481

Bufrolin	Agonist
Bufrolin is a Cromoglycate (histamine release inhibitor) analog and a high potency agonist of GPR35. Bufrolin promotes interactions between β-arrestin-2 and either human GPR35a or rat GPR35. Bufrolin also serves as antiallergic mast cell stabilizer and inhibit an anti-inflammatory response inducible by the internalization peptide. Bufrolin acts as an anti-inflammatory agent to be used in research of delivering pharmacol linked with internalization peptide.

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