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CAS No. : 870823-12-4
MCE 国际站:MK 0893
产品活性:MK 0893 是一种有效,选择性的胰高血糖素受体拮抗剂,IC50 值为 6.6 nM。
研究领域:GPCR/G Protein
作用靶点:GCGR
In Vitro: MK 0893 is selective for glucagon receptor relative to other family B GPCRs, showing IC50 values of 1020 nM for GIPR, 9200 nM for PAC1, and >10000 nM for GLP-1R, VPAC1, and VPAC2. MK 0893 is active against the rhesus monkey GCGR, showing an IC50 of 56 nM in a cAMP assay with CHO cells expressing the rhesus GCGR.
In Vivo: MK 0893 blunts glucagon-induced glucose elevation in hGCGR mice and rhesus monkeys. It also lowers ambient glucose levels in both acute and chronic mouse models: in hGCGR ob/ob mice it reduces glucose (AUC 0-6 h) by 32% and 39% at 3 and 10 mpk single doses, respectively. In hGCGR mice on a high fat diet, MK 0893 at 3, and 10 mpk po in feed lowers blood glucose levels by 89% and 94% at day 10, respectively, relative to the difference between the vehicle control and lean hGCGR mice.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Clinical Compound Library | Drug Repurposing Compound Library | Anti-diabetic Compound Library | Anti-COVID-19 Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | Dulaglutide | PF-06291874 | Neuropeptide Y, porcine | HAEGTFTSDVS | Glucagon receptor antagonists-5 | Oxyntomodulin TFA | Tirzepatide TFA | Liraglutide | GLP-1R agonist 1 | Exendin-4 acetate | GLP-1(7-37) acetate | Glucagon (1-29), bovine, human, porcine | GPCR modulator-1 | Oxyntomodulin (swine) | VU0453379 | Cotadutide | Elsiglutide | GLP-1 receptor agonist 7 | Exendin(9-39) amide | Glucagon-like peptide 1 (1-37), human TFA | Semaglutide TFA | Retatrutide acetate | GLP-1R modulator C5 | Glucagon (19-29), human | [Des-His1,Glu9]-Glucagon amide TFA | FC382K10W15 TFA | Exendin-3/4 (59-86) | FTSDVSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
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