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首页-小分子抑制剂&激动剂-GPCR-Glucagon Receptor-MK-0893
MK-0893

Chemical Structure : MK-0893

CAS No.: 870823-12-4

MK-0893 (MK0893;MK 0893)

货号: PC-45831Not For Human Use, Lab Use Only.

A potent, selective, reversible and competitive antagonist of glucagon receptor with high binding affinity (IC(=50=6.6 nM) and functional cAMP activity (IC50=15.7 nM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

MK-0893 is a potent, selective, reversible and competitive antagonist of glucagon receptor with high binding affinity (IC(=50=6.6 nM) and functional cAMP activity (IC50=15.7 nM).
MK-0893 displays selectivity for glucagon receptor relative to other family B GPCRs, IC50 of 1020 nM for GIPR, 9200 nM for PAC1, and >10000 nM for GLP-1R, VPAC1, and VPAC2.
MK-0893 blunts glucagon-induced glucose elevation in hGCGR mice and rhesus monkeys, also lowers ambient glucose levels in both acute and chronic mouse models.

物理化学性质&存储条件

分子量 588.4805
分子式 C32H27Cl2N3O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

.beta.-Alanine, N-[4-[(1S)-1-[3-(3,5-dichlorophenyl)-5-(6-methoxy-2-naphthalenyl)-1H-pyrazol-1-yl]ethyl]benzoyl]-

参考文献

1. Xiong Y, et al. J Med Chem. 2012 Jul 12;55(13):6137-48.

2. Guan HP, et al. J Lipid Res. 2015 Nov;56(11):2183-95.

3. Jazayeri A, et al. Nature. 2016 May 12;533(7602):274-7.

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