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You are here:Home-Inhibitors & Agonists-GPCR-GPR119

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GPR119 (G protein-coupled receptor 119) is a G protein-coupled receptor that in humans is encoded by the GPR119 gene. GPR119, along with GPR55 and GPR18, have been implicated as novel cannabinoid receptors. GPR119 is expressed predominantly in the pancreas and gastrointestinal tract in rodents and humans, as well as in the brain in rodents. Activation of the receptor has been shown to cause a reduction in food intake and body weight gain in rats. GPR119 has also been shown to regulate incretin and insulin hormone secretion. As a result, new drugs acting on the receptor have been suggested as novel treatments forobesity and diabetes.

Cat. No. Product Name CAS No. Information
H3365

MK-8282

MK-8282 is a potent, selective, oral GPR119 agonist with EC50 of 10 and 58 nM for hGPR119 and mGPR119, respectively; shows >150 fold selectivity over other receptors (Eurofin panlabs assay), transporters and ion channels; exhibits improved glucose tolerance in multiple animal models and has excellent off-target profile.

H3364

GSK1292263

 		1032823-75-8

GSK1292263 is a novel potent, selective GPR119 agonist, elevates circulating glucose-dependent insulinotropic peptide, GLP-1 and peptide tyrosine-tyrosine in nonclinical models of diabetes, with no effect on plasma glucose.
H3363

GSK 2041706

 		1032824-43-3

A potent, selective and orally bioavailable GPR119 agonist with EC50 of 4 nM, with good selectivity versus a battery of receptors, ion channels and enzymes; causes greater reductions in cumulative food intake and higher fed plasma GLP-1 and peptide tyrosine tyrosine levels and decreased plasma insulin and glucose-dependent insulinotropic polypeptide levels, when combined with metformin, in diet-induced obese mice.
H3362

Firuglipel

 		1371591-51-3

Firuglipel (DS-8500, DS8500a) is a novel potent, selective, orally available GPR119 agonist with EC50 of 51.5 nM in human GPR119-expressing CHO-K1 cells, displays no significant effect on 66 receptors, channels, or transporters; enhances glucose-stimulated insulin secretion in Sprague-Dawley rats and promotes GLP-1 secretion in Zucker fatty rats, preserved β cell function and prevented increases in glycohemoglobin concentrations in rodent models of type 2 diabetes.
H3361

AS-1269574

 		330981-72-1

AS-1269574 is a selective, orally available GPR119 agonist with EC50 of 2.5 uM in cell-based cAMP assays; displays no effect towards the other GPCRs, including the β-adrenergic and GLP-1 receptors; enhances insulin secretion in the mouse pancreatic β-cell line MIN-6 only under high-glucose (16.8mM) conditions; reduces blood glucose levels, does not affect fed and fasting plasma glucose levels in mice.

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