AZD0186 (AZD-0186)

Chemical Structure : AZD0186

Catalog No.: PC-25613Not For Human Use, Lab Use Only.

AZD0186 (AZD-0186) is a potent, selective glucagon-like peptide-1 receptor (GLP-1R) agonist, shows concentration-dependent potentiation of GSIS in EndoC-βH5 cells with EC50 of 0.6 nM, improves glucose control and reduces body weight.

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Biological Activity

AZD0186 (AZD-0186) is a potent, selective glucagon-like peptide-1 receptor (GLP-1R) agonist, shows concentration-dependent potentiation of GSIS in EndoC-βH5 cells with EC50 of 0.6 nM, improves glucose control and reduces body weight.

AZD0186 concentration dependently binds to the hGLP-1R displacing radiolabeled GLP-1(7–36)NH2 as well as potentiates cAMP accumulation in hGLP-1R overexpressing cells.

AZD0186 is a partial agonist in the β-arrestin-2 assay and full agonist in GLP-1R internalization assay.

AZD0186 exhibits a concentration-dependent effect on potentiating insulin secretion at 11 mM glucose in EndoC-βH5 cell line.

AZD0186 improves glucose control and reduces body weight in a human glucagon-like peptide-1 receptor mouse model.

Physicochemical Properties

M.Wt	636.53
Formula	C32H31Cl2N5O5
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-chloro-2-(((1R,6R)-5-((S)-2-(5-chloropyridin-2-yl)-2-methylbenzo[d][1,3]dioxol-4-yl)-2,5-diazabicyclo[4.2.0]octan-2-yl)methyl)-1-(((S)-oxetan-2-yl)methyl)-1H-benzo[d]imidazole-6-carboxylic acid

References

1. Weier Qi, et al. J Pharmacol Exp Ther. 2025 Aug 28;392(10):103683.

2. Patent WO2023057427.

AZD0186 (AZD-0186)

Biological Activity

Physicochemical Properties

References

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