3011682-49-5
Chemical Structure
Elecoglipron
Synonym(s): ECC5004; AZD5004
- CAS No.: 3011682-49-5
- Formula:C48H46F2N10O5
- Molecular Weight:880.94
InChIKey: JMKBTILBGROESC-WNJJXGMVSA-N
SMILES: O=C(N1[C@H](C2=C(N3C(N(C4=CC=C(N(N=C5)C)C5=C4F)C=C3)=O)N(C6=CC(C7CC7)=C(C=C6)F)N=C2CC1)C)C8=C(N9C(C=C([C@@H]%10CC(C)(OCC%10)C)C=C9)=C8)C%11(C%12=NOC(N%12)=O)CC%11
Biological Activity:
Elecoglipron (AZD5004) is an orally active small-molecule GLP-1R agonist. Its IC50 against human GLP-1R is 2.4 nM. It activates the cAMP signaling pathway in HEK293 cells overexpressing human GLP-1R with a potency of 2.1 nM, and enhances glucose-stimulated insulin secretion in EndoC-βH5 cells with an EC50 of 5.9 nM, with no detectable β-arrestin-2 recruitment or GLP-1R internalization. Elecoglipron can be used in research related to obesity, overweight and type 2 diabetes[1][2][3].
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Elecoglipron | Elecoglipron (AZD5004) is an orally active small-molecule GLP-1R agonist. Its IC50 against human GLP-1R is 2.4 nM. It activates the cAMP signaling pathway in HEK293 cells overexpressing human GLP-1R with a potency of 2.1 nM, and enhances glucose-stimulated insulin secretion in EndoC-βH5 cells with an EC50 of 5.9 nM, with no detectable β-arrestin-2 recruitment or GLP-1R internalization. Elecoglipron can be used in research related to obesity, overweight and type 2 diabetes. |
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- [1]. Ren Z, et al. Substituted imidazoles as GLP-1 receptor agonists. United States, US 11584751 B1. 2023-02-21.
- [2]. Davies MJ, et al. Elecoglipron, an oral small molecule GLP-1 receptor agonist in adults with obesity or overweight (VISTA): a multicentre, phase 2, randomised, placebo-controlled clinical trial. Lancet (London, England). 2026 Jun 20;407(10547):2503-2514.
- [3]. Haggag AZ, et al. Non-clinical and first-in-human characterization of ECC5004/AZD5004, a novel once-daily, oral small-molecule GLP-1 receptor agonist. Diabetes, obesity & metabolism. 2025 Feb;27(2):551-562.
Keywords
