TGR5 agonist MN6

Chemical Structure : TGR5 agonist MN6

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货号: PC-20412Not For Human Use, Lab Use Only.

TGR5 agonist MN6 is a potent and selective TGR5 agonist with cAMP EC50 values of 15.9 nM and 17.9 nM on hTGR5 and mTGR5, respectively.

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生物&药学活性

TGR5 agonist MN6 is a potent and selective TGR5 agonist with cAMP EC50 values of 15.9 nM and 17.9 nM on hTGR5 and mTGR5, respectively.
MN6 shows EC50 values of 1.5 and 18 nM on hTGR5 and mTGR5, respectively, by a CRE-driven luciferase reporter gene assay in either the hTGR5/CRE/HEK293 or mTGR5/CRE/HEK293 stable cell line.
MN6 significantly promoted GLP-1 secretion in human enteroendocrine NCI-H716 cells in a dose-dependent manner.
MN6 increased the plasma active GLP-1 level in CD1 mice following a glucose bolus, with a 68.5% or 89.3% increase after a single dose of 50 or 100 mg/kg MN6, respectively.
MN6 exhibited a synergistic effect combined with DPP-4 inhibitor BI-1356 (Cat. PC-42508).
MN6 (50 mg/kg) improved glucose homeostasis in ob/ob mice, improved metabolic abnormalities and increased the insulinstimulated glucose uptake in the skeletal muscles of DIO mice.

物理化学性质&存储条件

分子量	440.32
分子式	C23H19Cl2N3O2
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	(4-cyclopropyl-3,4-dihydroquinoxalin-1(2H)-yl)(4-(2,5-dichlorophenoxy)pyridin-3-yl)methanone

参考文献

1. Suling Huang, et al. Metabolism. 2019 Oct;99:45-56.

TGR5 agonist MN6

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TGR5 agonist MN6

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