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Cat. No.: HY-188129

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GLP-1R modulator-2

GLP-1R modulator-2 is a GLP-1R positive allosteric modulator with an EC₅₀ of 106 nM. GLP-1R modulator-2 simultaneously binds to the extracellular pocket of GLP-1R and the peptide ligand GLP-1 (9-36) through a molecular glue-like allosteric effect, and selectively enhances GLP-1 (9-36)-induced G protein-dependent cAMP signaling. When used in combination with GLP-1 (9-36) under high-glucose conditions, GLP-1R modulator-2 enhances glucose-dependent insulin secretion in wild-type rat pancreatic islets. GLP-1R modulator-2 exhibits strong probe dependence and significantly potentiates the activity of GLP-1 (9-36). GLP-1R modulator-2 can be used for research on type 2 diabetes and obesity .

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

CAS No.: 2889348-10-9
Formula: C₂₃H₂₁N₅
Molecular Weight:367.45

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

GLP-1R modulator-2 Chemical Structure

CAS No.: 2889348-10-9

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

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Biological Activity

Description

In Vitro

GLP-1R modulator-2 (compound 3-24) potently enhances the GLP-1 (9-36)-induced cAMP signaling pathway in CHO-K1 cells expressing human GLP-1R, with an EC₅₀ of 106 nM, while exerting only a weak effect on the activity of GLP-1 (7-36)^[1].
GLP-1R modulator-2 does not potentiate glucagon-induced cAMP signaling pathways in CHO-K1 cells expressing human GCGR^[1].
GLP-1R modulator-2 activates GLP-1R activity in rat INS-1E β cells and enhances the GLP-1 (7-36)-induced cAMP signaling pathway; at a concentration of 10 μM, it produces a 7.7-fold leftward shift in the EC₅₀ value^[1].
GLP-1R modulator-2 (1-30 μM) requires interactions with GLP-1R residues L142, Y145, and K202, as well as GLP-1 (9-36) residues V16 and L20, to enhance the cAMP signaling pathway in CHO-K1 cells transfected with GLP-1R^[1].

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

Chemical Information

CAS No. 2889348-10-9
Molecular Weight 367.45
Formula C₂₃H₂₁N₅
SMILES

CC(C1=CNC2=C1C=CC=C2)(C)CN3N=NC(C4=C5C=CC=CC5=NC=C4)=C3
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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]. Xin Y, et al. Affinity selection of double-click triazole libraries for rapid discovery of allosteric modulators for GLP-1 receptor. Proceedings of the National Academy of Sciences of the United States of America. 2023 Mar 14;120(11):e2220767120.

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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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