ZY12201 | TGR5 agonist | Probechem Biochemicals

Chemical Structure : ZY12201

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ZY12201 (ZY 12201, TGR5 agonist 6g)

货号: PC-72133Not For Human Use, Lab Use Only.

ZY12201 (TGR5 agonist 6g) is a highly potent, selective and orally efficacious TGR5 agonist with EC50 of 57 pM and 62 pM for hTGR5 and mTGR5, respectively.

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生物&药学活性

ZY12201 (TGR5 agonist 6g) is a highly potent, selective and orally efficacious TGR5 agonist with EC50 of 57 pM and 62 pM for hTGR5 and mTGR5, respectively.
TGR5 agonist 6g showed dose-dependent activation of a cAMP responsive element-driven luciferase reporter in TGR5 overexpressing CHO K1 cells (EC50=14 nM).
TGR5 agonist 6g modulated GLP-1 secretion in vitro at 10 and 30 μM concentration in NCI-H716 cells.
TGR5 agonist 6g exhibited good selectivity against FXR (EC50=6.4 uM).
TGR5 agonist 6g showed a dose-dependent inhibition of TNF-α in an LPS-induced cytokine release assay in human whole blood, similar to prednisolone (IC50=251 nM).
TGR5 agonist 6g (30 mg/kg, p.o.) increased plasma GLP-1 levels by 3.8-fold with respect to vehicle control in C57 mice, robustly lowered the blood glucose excursion in a dose-proportional manner with ED50 of 7.9 mg/kg and ED90 of 29.2 mg/kg.

物理化学性质&存储条件

分子量	558.672
分子式	C31H31FN4O3S
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	2-((2-(4-(1H-imidazol-1-yl)phenoxy)ethyl) thio)-5-(2-(3,4-dimethoxyphenyl) propan-2-yl)-1-(4-fluoro phenyl)-1H-imidazole

参考文献

1. Sojitra C, et al. SN Appl Sci. 2021;3(6):660.

3. Joshi VM, et al. Org Process Res Dev. 2020;8:1508–1514.

4. Agarwal S, et al. ACS Med Chem Lett. 2016;7(1):51–55.

ZY12201 (ZY 12201, TGR5 agonist 6g)

生物&药学活性

物理化学性质&存储条件

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ZY12201 (ZY 12201, TGR5 agonist 6g)

生物&药学活性

物理化学性质&存储条件

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