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Cat. No.: HY-186252

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GPR133 agonist 1

GPR133 agonist 1 is an orally active GPR133/ADGRD1 agonist with an EC₅₀ of 1.6 nM (293T cells). GPR133 agonist 1 activates GPR133, thereby regulating the downstream cAMP signaling pathway. GPR133 agonist 1 enhances muscle strength and endurance in mice. GPR133 agonist 1 can be used in research related to muscular atrophy, myasthenia, sarcopenia, erectile dysfunction, vestibular dysfunction, obesity, and non-alcoholic fatty liver disease.

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

CAS No.: 3103571-04-3
Formula: C₂₅H₃₄N₄O₃
Molecular Weight:438.56

Storage:

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

GPR133 agonist 1 Chemical Structure

CAS No.: 3103571-04-3

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Use of MCE Products

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

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

Description

In Vitro

GPR133 agonist 1 (Compound 1) exhibits potent GPR133 agonist activity in HEK293 cells overexpressing GPR133, with an EC₅₀ of 1.6 nM^[1].
GPR133 agonist 1 (1 μM; 15 min) exhibits significantly improved stability in mouse liver microsomes, with 90% remaining after incubation at 1 μM for 15 min^[1].

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

In Vivo

GPR133 agonist 1 (20 mg/kg; p.o.; daily; 5 days) increases mouse muscle strength and endurance, with an average suspension stay time of 53.6 seconds, which is significantly greater than that of the positive control AP503^[1].

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

Animal Model:

C57BL/6 (male, 5 weeks old, 16-20g)^[1]
Dosage:

20 mg/kg
Administration:

p.o.; daily; 5 days
Result:

Increased average suspension stay time to 53.6 seconds.

Chemical Information

CAS No. 3103571-04-3
Molecular Weight 438.56
Formula C₂₅H₃₄N₄O₃
SMILES

O=C(N(C)C)C1=CC=C(N2CCN(CC2)CC)C(NC(COC3=CC=C(C)C=C3C)=O)=C1
Shipping

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]. Li Zheng, et al. A novel benzamide derivative, its preparation method and its use as medicine. CN120247837A. 2025-07-04.

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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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100 mg

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