GPR109A
HM74A; PUMA-G; HCA2; HCAR2
GPR109A is a G-protein-coupled receptor for nicotinate but recognizes butyrate with low affinity. GPR109A is expressed in the lumen-facing apical membrane of colonic and intestinal epithelial cells and that the receptor recognizes butyrate as a ligand. The expression of GPR109A is silenced in colon cancer in humans, in a mouse model of intestinal/colon cancer, and in colon cancer cell lines. The tumor-associated silencing of GPR109A involves DNA methylation directly or indirectly. Reexpression of GPR109A in colon cancer cells induces apoptosis, but only in the presence of its ligands butyrate and nicotinate. Butyrate is an inhibitor of histone deacetylases, but apoptosis induced by activation of GPR109A with its ligands in colon cancer cells does not involve inhibition of histone deacetylation. The primary changes in this apoptotic process include down-regulation of Bcl-2, Bcl-xL, and cyclin D1 and up-regulation of death receptor pathway. In addition, GPR109A/butyrate suppresses nuclear factor-kappaB activation in normal and cancer colon cell lines as well as in normal mouse colon. These studies show that GPR109A mediates the tumor-suppressive effects of the bacterial fermentation product butyrate in colon.
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GPR109A Verwandte Produkte (19)
Verwandte Produkte (19)
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Mepenzolate bromide
0 ImagesMepenzolate bromide is an orally administered muscarinic receptor antagonist with Kis of 0.68 and 2.6 nM for hM2R and hM3R, respectively. Mepenzolate bromide can be used to suppress the gastrointestinal hypermotility associated with irritable bowel syndrome.Mepenzolate bromide is a GPR109A inhibitor.
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Monomethyl fumarate
0 ImagesMonomethyl fumarate, an active metabolite of Dimethyl fumarate (DMF), is a potent GPR109A agonist. Monomethyl fumarate has the potential for multiple neuroprotective pathways and other models of retinal disease.
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GSK256073
0 ImagesGSK256073 is a potent, selective and orally active GPR109A agonist and a long-lasting and non-flushing HCA2 full agonist with a pEC50 of 7.5 (human HCA2). GSK256073 acutely improves glucose homeostasis via inhibition of lipolysis and has the potential for the study of type 2 diabetes mellitus (T2DM)and dyslipidemia. GPR109A: G-protein coupled receptor 109A; HCA2: hydroxy-carboxylic acid receptor 2
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MK-1903
0 ImagesMK-1903 is an orally active full agonist of GPR109a/HCAR2, with an EC50 of 12.9 nM. MK-1903 activates antilipolytic and vasodilatory pathways, reduces plasma free fatty acid levels, and induces skin flushing. MK-1903 stimulates the expression of HCAR2 protein and regulates the inflammatory response of microglia. MK-1903 prevents the enhanced firing activity of spinal nociceptive neurons. MK-1903 triggers the release of MMP-9 and the formation of NET. MK-1903 can be used in the research of dyslipidemia and neuroinflammation-based central nervous system diseases.
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GPR109 receptor agonist-1
0 ImagesGPR109 receptor agonist-1 is a highly selective agonist of the human orphan G protein-coupled receptor GPR109b, and does not activate the mouse homologous receptor PUMA-G. GPR109 receptor agonist-1 functionally modulates the human GPR109b receptor via the cAMP signaling pathway, with an EC50 of 400 nM. GPR109 receptor agonist-1 inhibits isoproterenol (HY-B0468)-stimulated lipolysis in human subcutaneous adipocytes, with efficacy comparable to that of Niacin (HY-B0143), and does not act on β-adrenergic receptors. GPR109 receptor agonist-1 can be used in studies related to dyslipidemia and atherosclerosis.
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Monomethyl fumarate-d3
0 ImagesMonomethyl fumarate-d3 is a deuterium labeled Monomethyl fumarate (HY-103252). Monomethyl fumarate, an active metabolite of Dimethyl fumarate (DMF) (HY-17363), is a potent GPR109A agonist. Monomethyl fumarate has the potential for multiple neuroprotective pathways and other models of retinal disease.
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GPCR agonist-2
0 ImagesGPCR agonist-2 (Compound 5j) is a GPCR GPR109b (HM74) agonist, with a pEC50 value of 6.51. GPCR agonist-2 can be used for research of lipid disorders.
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Monomethyl fumarate-d2
0 ImagesMonomethyl fumarate-d2 is a deuterium labeled Monomethyl fumarate (HY-103252). Monomethyl fumarate, an active metabolite of Dimethyl fumarate (DMF) (HY-17363), is a potent GPR109A agonist. Monomethyl fumarate has the potential for multiple neuroprotective pathways and other models of retinal disease.
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GPR109 receptor agonist-3
0 ImagesArt. -Nr.: HY-176817CAS. Nr.: 944559-31-3GPR109 receptor agonist-3 is an orally active GPR109 receptor agonist, with an IC50 of 310 nM. GPR109 receptor agonist-3 retains the antioxidation and cytoprotection of Lipoic acid (HY-18733). GPR109 receptor agonist-3 reduces total cholesterol (TC), triglyceride (TG), low-density lipoprotein cholesterol (LDL-C) and increases high-density lipoprotein cholesterol (HDL-C) in high-fat diet-fed rats. GPR109 receptor agonist-3 can be used for the study of atherosclerosis.
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Monomethyl fumarate (Standard)
0 ImagesArt. -Nr.: HY-103252RCAS. Nr.: 2756-87-8Monomethyl fumarate (Standard) is the analytical standard of Monomethyl fumarate. This product is intended for research and analytical applications. Monomethyl fumarate, an active metabolite of Dimethyl fumarate (DMF), is a potent GPR109A agonist. Monomethyl fumarate has the potential for multiple neuroprotective pathways and other models of retinal disease[1][2][3].
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Acifran (Standard)
0 ImagesArt. -Nr.: HY-107579RCAS. Nr.: 72420-38-3Synonyms: AY 25712 (Standard)(2S,5R,6R)-Ticarcillin (disodium) (Standard) is the analytical standard of (2S,5R,6R)-Ticarcillin (disodium). This product is intended for research and analytical applications. (2S,5R,6R)-Ticarcillin disodium is an injectable antibiotic for the treatment of Gram-negative bacteria, particularly Pseudomonas aeruginosa. It is also one of the few antibiotics capable of treating Stenotrophomonas maltophilia infections.
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GSK256073 tris
0 ImagesArt. -Nr.: HY-119222ACAS. Nr.: 1228650-42-7GSK256073 tris is a potent, selective and orally active GPR109A agonist and a long-lasting and non-flushing HCA2 full agonist with a pEC50 of 7.5 (human HCA2). GSK256073 tris acutely improves glucose homeostasis via inhibition of lipolysis and has the potential for the study of type 2 diabetes mellitus (T2DM)and dyslipidemia. GPR109A: G-protein coupled receptor 109A; HCA2: hydroxy-carboxylic acid receptor 2
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MK-1903 (Standard)
0 ImagesMK-1903 (Standard) is the analytical standard of MK-1903 (HY-107581). This product is intended for research and analytical applications. MK-1903 is an orally active full agonist of GPR109a/HCAR2, with an EC50 of 12.9 nM. MK-1903 activates antilipolytic and vasodilatory pathways, reduces plasma free fatty acid levels, and induces skin flushing. MK-1903 stimulates the expression of HCAR2 protein and regulates the inflammatory response of microglia. MK-1903 prevents the enhanced firing activity of spinal nociceptive neurons. MK-1903 triggers the release of MMP-9 and the formation of NET. MK-1903 can be used in the research of dyslipidemia and neuroinflammation-based central nervous system diseases.
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Monomethyl fumarate-d5
0 ImagesArt. -Nr.: HY-103252S1CAS. Nr.: 1616345-45-9Monomethyl fumarate-d5 is deuterium labeled Monomethyl fumarate (HY-103252). Monomethyl fumarate, an active metabolite of Dimethyl fumarate (DMF) (HY-17363), is a potent GPR109A agonist. Monomethyl fumarate has the potential for multiple neuroprotective pathways and other models of retinal disease.
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MK-6892 (Standard)
0 ImagesArt. -Nr.: HY-10680RCAS. Nr.: 917910-45-3MK-6892 (Standard) is the analytical standard of MK-6892 (HY-10680). This product is intended for research and analytical applications. MK-6892 is a potent, selective, and full agonist for the high affinity nicotinic acid (NA) receptor GPR109A. Ki and GTPγS EC50 of MK-6892 on the Human GPR109A is 4 nM and 16 nM, respectively.
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