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Cat. No.: HY-182582

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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.

For research use only. We do not sell to patients.

CAS No.: 1430210-54-0
Formula: C₃₁H₃₁FN₄O₃S
Molecular Weight:558.67

Storage:

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

ZY12201 Chemical Structure

CAS No.: 1430210-54-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
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Biological Activity

Description

All Cytochrome P450 Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	EC₅₀	0.057 nM Compound: 6g	Agonist activity at human TGR5 expressed in CHO-K1 cells after 5 hrs by luciferase reporter gene assay Agonist activity at human TGR5 expressed in CHO-K1 cells after 5 hrs by luciferase reporter gene assay	[PMID: 26819665]

In Vitro

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.

In Vivo

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.

Chemical Information

CAS No. 1430210-54-0
Molecular Weight 558.67
Formula C₃₁H₃₁FN₄O₃S
SMILES

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
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Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[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. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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ZY12201

All Cytochrome P450 Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

ZY12201 Related Classifications

HY-182582 Related Classifications