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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
29 Results for "
GPR109
" in MedChemExpress (MCE) Product Catalog:
Products (29)
29 Results for "GPR109" in MCE Product Catalog:
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Mepenzolate 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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8 Publications Verification
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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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 .
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4 Cited Publications
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GPR81 agonist 1 is a potent and highly selective GPR81 agonist, with EC50s of 58 nM and 50 nM for human and mouse GPR81, respectively. GPR81 agonist 1 inhibits lipolysis in differentiated 3T3-L1 adipocytes. GPR81 agonist 1 suppresses lipolysis in mice without cutaneous flushing. GPR81 agonist 1 displays remarkable selectivity for GPR81 over GPR109a .
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3 Cited Publications
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GSK256073 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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2 Cited Publications
MK-0354 is a specific GPR109a receptor agonist with EC50 values of 1.65 μM and 1.08 μM for hGPR109a and mGPR109a, respectively. MK-0354 can be used in liver cancer research .
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1 Cited Publications
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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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1 Cited Publications
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1 Cited Publications
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SCH-900271 is an orally active, potent nicotinic acid receptor (NAR) agonist with an EC50 of 2 nM in the hu-GPR109a assay. SCH-900271 exhibits dose-dependent inhibition of plasma free fatty acid (FFA) .
Cat. No.: HY-W014502
CAS No.: 13441-51-5
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Research Areas:
Cardiovascular Disease Metabolic Disease Inflammation/Immunology
GPR109 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 .
Category:
Microorganisms Ketones, Aldehydes, Acids Other Diseases Endogenous metabolite Disease Research Fields
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Cat. No.: HY-W004049
CAS No.: 99-06-9
Cat. No.: HY-176817
CAS No.: 944559-31-3
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GPR109 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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Cat. No.: HY-W095200
CAS No.: 957129-38-3
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GPR109 receptor agonist-2 (Compound 5) is a selective GPR109a agonist with a pEC50 of 5.53 .
Cat. No.: HY-103252S2
CAS No.: 253122-44-0
Cat. No.: HY-W004049R
CAS No.: 99-06-9
Cat. No.: HY-47823
CAS No.: 291528-35-3
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GPCR 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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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
