ZY12201 

ZY12201 is a selective and orally active TGR5 agonist and pan-CYP inhibitor. ZY12201 lowers glucose levels. ZY12201 induces enzymes regulated through Aryl Hydrocarbon Receptor, Constitutive Androstane Receptor, and Pregnane X Receptor. ZY12201 can be used for the research of type 2 diabetes^[1][2].

ZY12201 potently activates human TGR5 with an EC₅₀ of 57 pM and mouse TGR5 with an EC₅₀ of 62 pM^[1].
ZY12201 (0.1-100 μM; 48 h) induces CYP1A2, CYP2B6, and CYP3A4 mRNA levels in single female donor HH1103 sandwich cultured human hepatocytes, acting as an agonist of AhR, CAR, and PXR^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ZY12201 (7.9-29.2 mg/kg) exhibits glucose-lowering activity in diet-induced obese C57BL/6 mice during an oral glucose tolerance test, with an ED₅₀ of 7.9 mg/kg and ED₉₀ of 29.2 mg/kg^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

558.67

C₃₁H₃₁FN₄O₃S

1430210-54-0

FC1=CC=C(N2C(SCCOC3=CC=C(N4C=NC=C4)C=C3)=NC=C2C(C)(C)C5=CC=C(C(OC)=C5)OC)C=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Joshi, VM, et al. Practical and Efficient Synthesis of 2-Thio-imidazole derivative - ZY12201: A Potent TGR5 Agonist. Org. Process Res. Dev. 2020; 24(8):1508-1514.

  [2]. Aluri KC, et al. Aminobenzotriazole inhibits and induces several key drug metabolizing enzymes complicating its utility as a pan CYP inhibitor for reaction phenotyping. Clin Transl Sci. 2024;17(3):e13746.