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 Related Products (24):

By Effects:	Agonists (16) Activators (2) Modulators (3)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-100806

Kynurenic acid	Agonist	99.21%
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-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-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-W018158

DHICA	Activator
DHICA (5,6-Dihydroxyindole-2-carboxylic acid) is an intermediate in melanin synthesis and a component of true black pigment, and it’s also a moderately potent GPR35 agonist. DHICA shows an ability to stimulate β-arrestin translocation signaling with an EC₅₀ value of 23.2 μM in the U2OS cell line. DHICA plays a significant role in promoting and protecting against DNA damage.

HY-W008613R

Pamoic acid (Standard)	Agonist
Pamoic acid (Standard) is the analytical standard of Pamoic acid. This product is intended for research and analytical applications. Pamoic acid (Embonic acid) is a potent GPR35 agonist with an EC₅₀ of 79 nM. Pamoic acid exhibits neuroprotective and anti-inflammatory properties.

HY-169301

Gpr35 modulator 1	Modulator
Gpr35 modulator 1 (compound 1-18) is a potent modulator of Gpr35, with the IC₅₀ of ≤ 100 nM in HEK293 cells stably transfected with human GPR35.

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-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-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-134801

CID1231538		99.74%
CID1231538, a benzothiazole analog, is a potent GPR35 antagonist with no significant activity against rodent orthologs of GPR35, which is also a G protein-coupled receptor (GPCR).

HY-101033

GPR35 agonist 1		99.22%
GPR35 agonist 1 (compound 50) is a potent and specific G protein-coupled receptor-35 (GPR35)/CXCR8 agonist with an EC₅₀ of 5.8 nM, displays good agentgability.

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	99.80%
YE120 is a potent GPR35 agonist with an EC₅₀ of 32.5 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-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	99.00%
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-169304

Gpr35 modulator 3	Modulator
Gpr35 modulator 3 (Example 105) is a Gpr35 modulator with an IC₅₀ < 1 μM. Gpr35 modulator 3 can be used in the study of proliferative, immune, and inflammatory.

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