gpr35

GPR35 agonist 2 (TC-G 1001) is a potent GPR35 agonist.The EC50 values of GPR35 agonist 2 in the β-arrestin and Ca2+ release assays were 26 and 3.2 nM, respectively.

GPR35 agonist 3 is a synthetic GPR35 agonist with an EC50 value of 1.4 μg in the β-arrestin recruitment assay.GPR35 agonist 3 is used in the study of cancer, type 2 diabetes, and cardiovascular disease.

YE 120 is a highly potent GPR35 agonist (EC50: 32.5 nM) with potential anti-inflammatory and anti-cancer activities, which can be used to study G protein-coupled receptor-related diseases.

ML 145 is a selective and potent antagonist of human GPR35, with no significant activity against GPR35 in any of its immediate rodent homologs.ML 145 has potential anti-inflammatory activity for the study of immunoinflammation.ML 145 is a novel non-steroidal anti-inflammatory agent for the study of rheumatoid arthritis.

Tyrphostin A25 (Tyrphostin AG 82) is a specific EGFR tyrosine kinase inhibitor and GPR35 agonist with an IC50 value of 0.94 μM for GPR35 and an EC50 value of 5.3 μM for GPR35.

Kynurenic acid (Quinurenic acid) is an endogenous tryptophan active metabolite, a triple antagonist of NMDA, glutamate, α7 nicotinic acetylcholine receptor, and an agonist of GPR35/CXCR8 with neuroprotective and anticonvulsant properties. It has neuroprotective and anticonvulsant properties and can be used to study neurodegeneration and metabolism-related diseases.

Pamoic acid is the orphan G protein-coupled receptor GPR35 agonist. Pamoic acid activates ERK and beta-arrestin2 and causes antinociceptive activity.

CID1231538 is a potent GPR35 antagonist.

GPR35 agonist 1 is a highly effective and specific GPR35/CXCR8 agonist (EC50: 5.8 nM).

Gpr35modulator 3 (Example 105) is a Gpr35 regulator with an IC50 of less than 1 μM. It is utilized in research related to proliferation, immune response, and inflammation.

Gpr35modulator 2 (compound 52) serves as a modulator for GPR35. It is utilized in researching a variety of diseases related to GPR35.

Gpr35modulator 1 (compound 1-18) acts as an effective modulator of Gpr35, demonstrating an IC50 of less than or equal to 100 nM in HEK293 cells stably transfected with human GPR35.

GPR35activator-1 (example 5) is an effective activator of GPR35, exhibiting a Ki of 0.08 nM for human GPR35.

Compound 6 (3,5-dinitro-bisphenol A), also known as GPR35 agonist 5, exhibits weak GPR35 agonistic activity. This compound causes G1/Go phase arrest in CHO-S cells [1].

CID 2745687 is a moderately potent, concentration-dependent antagonist at human GPR35 with pIC50 = 6.70. CID 2745687 cannot effectively antagonize the agonist effects of either Zaprinast or Cromolyn disodium at rodent ortholog of GPR35 in vitro[1]. However, CID 2745687 can reverse lodoxamide-mediated anti-fibrotic effects in mice in vivo[2].

Pamoic acid disodium is a GPR35 agonist.

NSC-299202 is a novel potent agonist of Human G Protein-Coupled Receptor-35 (hGPR35) (EC50 8 nM).

DHICA (5,6-Dihydroxyindole-2-carboxylic acid) is an intermediate in melanin synthesis and a component of eumelanin, as well as acting as a moderate potency agonist of GPR35. In the U2OS cell line, DHICA demonstrates the ability to induce β-arrestin translocation signaling with an EC50 value of 23.2 μM. Additionally, it plays a significant role in promoting and protecting against DNA damage.

Zaprinast is a cGMP-selective phosphodiesterase (PDE) inhibitor and a GPR35 agonist. It has a strong activating effect on rat GPR35 and a certain activating effect on human GPR35. It reduces vascular remodeling through anti-proliferative and pro-apoptotic effects.

ML-193 (CID 1261822) is a potent and selective GPR55 antagonist (IC50: 221 nM) with over 27-fold selectivity for GPR55 over GPR35, CB1, and CB2. It can ameliorate motor and sensorimotor deficits in Parkinson's disease (PD) rats.

GPR35 agonist 4 (compound 10) demonstrates high potency as a GPR35 agonist with a pEC50 of 5.86, effective on both human and rat GPR35; mutation of arginine at position 3.36 results in loss of its agonist function on GPR35 [1].

Kynurenic acid sodium salt is an endogenous tryptophan metabolite that acts as a broad-spectrum antagonist targeting ionotropic glutamate receptors (NMDA), other glutamate receptors, and the α7 nicotinic acetylcholine receptor, while also functioning as a potent agonist for the G-protein coupled receptor GPR35/CXCR8.

Bufrolin, an analog of Cromoglycate (histamine release inhibitor) and a potent agonist of GPR35, enhances the interaction between β-arrestin-2 and both human GPR35a and rat GPR35. It stabilizes mast cells, exhibiting antiallergic properties, and inhibits anti-inflammatory responses triggered by internalization peptides. Furthermore, Bufrolin is researched for its anti-inflammatory properties in pharmaceutic applications associated with internalization peptides [1] [2] [3].

Kynurenic acid, an active metabolite of tryptophan, is synthesized through a kynurenine intermediate by kynurenine aminotransferases (KATs). It acts as an antagonist of both NMDA and AMPA receptors, as well as α7 nicotinic acetylcholine receptors (nAChRs; EC50s = 235, 101, and 7 µM, respectively), and functions as an agonist for the aryl hydrocarbon receptor (AhR) and G protein-coupled receptor 35 (GPR35; EC50s = 1.4 and 39 µM, respectively). In a neonatal rat model of cerebral hypoxic-ischemia, induced by carotid artery ligation, administration of kynurenic acid at 300 mg/kg prevents weight loss in the lesioned hemisphere. Additionally, at concentrations of 1 and 5 mg/ml, it protects against neurodegeneration in the rhabdomere of the eye in an Htt93QtransgenicDrosophila model of Huntington's disease. Elevated levels of kynurenic acid in the cerebrospinal fluid have been observed in patients with schizophrenia.