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.
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GPR35 Related Products (35)
Related Products (35)
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DHICA (Standard)
0 ImagesCat. No.: HY-W018158RCAS No.: 4790-08-3Synonyms: 5,6-Dihydroxyindole-2-carboxylic acid (Standard)DHICA (Standard) is an analytical standard of DHICA (HY-W018158). This product is for research and analytical applications. DHICA (5,6-Dihydroxyindole-2-carboxylic acid) is an eumelanin building block, GPR35 agonist and melanin synthesis intermediate. DHICA activates GPR35, triggering dynamic mass redistribution and β-arrestin translocation. DHICA interacts with DNA and interferes with Fpg activity. DHICA promotes the generation of single-strand breaks in plasmid DNA. DHICA increases the activity and expression levels of SOD and Catalase. DHICA is applicable to research related to skin cancer and colon cancer.
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Gpr35 modulator 1
0 ImagesCat. No.: HY-169301CAS No.: 2994189-01-2Gpr35 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.
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Gpr35 modulator 3
0 ImagesCat. No.: HY-169304CAS No.: 3055887-18-5Gpr35 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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Gpr35 modulator 2
0 ImagesCat. No.: HY-169303CAS No.: 3049339-96-7Gpr35 modulator 2 (compound 52) is a GPR35 modulator. Gpr35 modulator 2 can be used for the study of a various GPR35-related disorders.
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GPR35 agonist 6
0 ImagesCat. No.: HY-W1058476CAS No.: 1443367-20-1GPR35 agonist 6 is a potent and selective agonist targeting GPR35, with an EC50 of 12.1 nM against human GPR35. GPR35 agonist 6 activates the human splice variant GPR35b with comparable efficacy, showing an EC50 of 22.1 nM. GPR35 agonist 6 also exhibits weak GPR55 antagonistic activity, with an IC50 of 21.7 μM, and its agonistic activity towards GPR35 is significantly stronger than its antagonistic activity towards GPR55. GPR35 agonist 6 initiates GPR35 downstream signaling by inducing β-arrestin recruitment. GPR35 agonist 6 is used to investigate GPR35-mediated diseases, such as gastrointestinal lesions and gastric cancer.
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CID 2745687 (Standard)
0 ImagesCat. No.: HY-107537RCAS No.: 264233-05-8CID 2745687 (Standard) is the analytical standard of CID 2745687 (HY-107537). This product is intended for research and analytical applications. CID 2745687 acts as a specific, reversible and competitive GPR35 antagonist with a Ki of 12.8 nM.
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Tyrphostin 25 (Standard)
0 ImagesCat. No.: HY-101958RCAS No.: 118409-58-8Synonyms: AG82 (Standard); Tyrphostin A 25 (Standard); Tyrphostin AG 82 (Standard); RG-50875 (Standard)Tyrphostin 25 (Standard) (AG82 (Standard)) is the analytical standard of Tyrphostin 25 (HY-101958). This product is intended for research and analytical applications. Tyrphostin 25 (AG82) is a specific inhibitor of the EGFR tyrosine kinase with an IC50 value of 3 µM in A431 cells. Tyrphostin 25 is also a GPR35 agonist with an EC50 of 5.3 µM.
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ML 145 (Standard)
0 ImagesCat. No.: HY-107536RCAS No.: 1164500-72-4ML 145 (Standard) is the analytical standard of ML 145 (HY-107536). This product is intended for research and analytical applications. 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.
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Kynurenic acid sodium (Standard)
0 ImagesKynurenic acid (sodium) (Standard) is the analytical standard of Kynurenic acid (sodium). This product is intended for research and analytical applications. 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.
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GPR35 agonist 3
0 ImagesGPR35 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.
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ML301
0 ImagesCat. No.: HY-178725CAS No.: 1531633-84-7ML301 is a small molecule G-protein agonist. ML301 can be inhibited by SR142948A with an IC50 of around 63 nM. ML301 fully competes for 125I-NT binding.
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Diethyl-Lodoxamide
0 ImagesCat. No.: HY-167706CAS No.: 53882-13-6Diethyl-Lodoxamide is a highly potent GPR35 agonist with potential to inhibit inflammatory bowel disease. Diethyl-Lodoxamide activates GPR35 in humans, mice and rats, showing similar EC50 values. Diethyl-Lodoxamide can alleviate the clinical symptoms of DSS-induced inflammatory bowel disease in mouse models, and the effect is better than the traditional drug 5-ASA. The pharmaceutical properties of Diethyl-Lodoxamide have been optimized to better meet the requirements of drug design.
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