gpr35

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.

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.

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].

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

Pamoic acid disodium is a GPR35 agonist.

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.

CID1231538 is a potent GPR35 antagonist.

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.

ML314 is a brain-permeable nonpeptide β-inhibin-biased neurotensin NTR1 receptor agonist (EC50: 1.9 μM), a biased neurotensin receptor ligand for methamphetamine abuse that inhibits NTR2 and GPR35.

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].

ML-184 (CID2440433) is a potent synthetic agonist of GPR55 with an EC50 of 0.26 μM.

CID 2745687 is a GPR35 antagonist that inhibited the effects at human GPR35 of cromolyn disodium and zaprinast, two agonists that share an overlapping binding site.

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.

ML 145 is a selective antagonist of GPR35/CXCR8 (IC50/EC50 of 20.1 nM)

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.

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-d5 is a deuterated compound of Kynurenic Acid. Kynurenic Acid has a CAS number of 492-27-3. Kynurenic acid, a natural metabolite of tryptophan via the kynurenine pathway, is a broad-spectrum excitatory amino acid antagonist.

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, 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.

broad spectrum EAA antagonist