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Chemical Structure : ZY12201
Catalog No.: 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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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.
| M.Wt | 558.672 | |
| Formula | C31H31FN4O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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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.
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