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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
814 Results for "
GPR
" in MedChemExpress (MCE) Product Catalog:
Products (814)
814 Results for "GPR" in MCE Product Catalog:
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ML-193 (CID 1261822) is a potent and selective antagonist of GPR55, with an IC50 of 221 nM. ML-193 shows more than 27-fold selectivity for GPR55 over GPR35, CB1 and CB2. ML-193 can improve the motor and the sensorimotor deficits of Parkinson’s disease (PD) rats .
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Zaprinast (M&B 22948) is a selective inhibitor of cGMP-selective Phosphodiesterase (PDE5). Zaprinast causes a significant increase in cGMP levels in myocytes. Zaprinast is a G protein-coupled receptor 35 (GPR35) agonist which activates rat GPR35 strongly and activates human GPR35 moderately. Zaprinast reduces vessel remodeling through antiproliferative and proapoptotic effects .
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3 Cited Publications
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DC260126 is a potent antagonist of GPR40 (FFAR1). DC260126 dose-dependently inhibits GPR40-mediated Ca 2+ elevations stimulated by linoleic acid, oleic acid, palmitoleic acid and lauric acid (IC50: 6.28, 5.96, 7.07, 4.58 μM, respectively) . DC260126 could protect MIN6 β cells from palmitate-induced ER stress and apoptosis .
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cis-Epoxysuccinic acid is a succinate receptor (SUCNR1/GPR91) agonist. cis-Epoxysuccinic acid inhibits cAMP levels with an EC50 value of 2.7 μM. cis-Epoxysuccinic acid can be used for the research of cardiovascular system .
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3 Cited Publications
Cat. No.: HY-13967
CAS No.: 865231-46-5
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AMG 837 is an orally active, selective GPR40/FFA1 agonist with an EC50 of 1.5 nM against human GPR40. AMG 837 stimulates insulin secretion in a glucose-dependent manner, and effectively improves glycemic control in both normal and diabetic rodent models . AMG 837 binds to the BacA protein and impairs the survival and replication of Brucella. AMG 837 can be used in research related to type 2 diabetes and brucellosis .
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AMG 837 calcium hydrate is an orally active, selective GPR40/FFA1 agonist with an EC50 of 1.5 nM against human GPR40. AMG 837 calcium hydrate stimulates insulin secretion in a glucose-dependent manner, and effectively improves glycemic control in both normal and diabetic rodent models . AMG 837 calcium hydrate binds to the BacA protein and impairs the survival and replication of Brucella. AMG 837 calcium hydrate can be used in research related to type 2 diabetes and brucellosis .
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SCO-267 is an allosteric GPR40 full agonist. SCO-267 can be used for the research of chronic diseases including diabetes .
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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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AR 231453 is a potent, specific and orally available GPR119 agonist. AR 231453 can stimulate β-cell replication and improve islet graft function s .
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TUG-770 is a potent, selective and orally active GPR40/FFA1 agonist with an EC50 of 6 nM for human FFA1. TUG-770 shows a high selectivity for FFA1 over FFA2, FFA3, FFA4, PPARγ, other receptors, transporters, and enzymes. TUG-770 can be uesd for type 2 diabetes research . TUG-770 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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3 Cited Publications
Cat. No.: HY-P1197
CAS No.: 478507-53-8
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Cat. No.: HY-P1197A
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Ogerin, a chemical probe, is a selective GPR68 positive aliasing modulator (PAM) (pEC50=6.83) with a moderate antagonistic effect on A2A (Ki=220 nM). Ogerin inhibits the fear conditioning reflex in mice and also inhibits TGF-β-induced myofibroblast differentiation of fibroblasts from multiple organ systems. Ogerin can be used in the studies of fibrotic diseases and neurological disorders .
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AM-1638 is an orally active full agonist of GPR40 (EC50: 0.16 μM). AM-1638 increases the expression of antioxidant molecules (HO-1 and NQO-1). AM1638 blocks Palmitate (HY-N0830)-mediated superoxide production and ER stress. AM-1638 has antidiabetic activity and improves glycemic control in BDF mice with diet-induced obesity (DIO). AM-1638 demonstrates excellent oral bioavailability (mouse, >100%; rat, 72%; and cyno, 71%) .
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GPR120 Agonist 3 is a selective Gpr120 agonist with a logEC50 of 7.62.
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GPR41 agonist-1 (compound 9) is a potent GPR41 agonist. GPR41 agonist-1 can be used for researching insulin-related disorders .
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Synonyms: OGM; GPR68-IN-1; OGM-8345
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Ogremorphin (OGM) is a G protein coupled sensor GPR68 inhibitor with anti-inflammatory and anti-tumor activities. Ogremorphin can inhibit the migration of human melanoma cells and induce ferroptosis in glioblastoma cells .
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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
