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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.

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CAS No.: 1430210-54-0
Formule: C₃₁H₃₁FN₄O₃S
Masse moléculaire:558.67

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

Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
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Activité biologique

Description

Voir tous les produits spécifiques à Isoform Cytochrome P450 :

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
Masse moléculaire 558.67
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[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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Activité biologique
- Description
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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ZY12201

Voir tous les produits spécifiques à Isoform Cytochrome P450

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

ZY12201 Related Classifications

HY-182582 Related Classifications