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Chemical Structure : AMG 986
CAS No.: 2049980-18-7
Catalog No.: PC-38136Not For Human Use, Lab Use Only.
AMG 986 (Azelaprag, AMG986) is a small-molecule agonist of Apelin receptor (APJ, APLNR), inhibits forskolin-stimulated cAMP production (pEC50=9.64) and promoted Gα protein activation (pEC50=9.54).
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AMG 986 (Azelaprag, AMG986) is a small-molecule agonist of Apelin receptor (APJ, APLNR), inhibits forskolin-stimulated cAMP production (pEC50=9.64) and promoted Gα protein activation (pEC50=9.54).
AMG 986 is a full APJ agonist that exhibits slight differences in potency relative to one another and may be more potent when compared with the endogenous ligand pyr-apelin-13.
AMG 986 exhibited a potentcy to recruit β-arrestin using the PathHunter arrestin assay with pC50 of 9.61.
AMG 986 altered cardiac hemodynamics and increased cardiac reserve during dobutamine challenge in a rat model of impaired metabolic function and exhibited improved pharmacokinetic profile relative to pyr-apelin-13.
| M.Wt | 523.612 | |
| Formula | C25H29N7O4S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(2S,3R)-N-(4-(2,6-dimethoxyphenyl)-5-(5-methyl-3-pyridinyl)-4H-1,2,4-triazol-3-yl)-3-(5-methyl-2-pyrimidinyl)-2-butanesulfonamide |
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1. Brandon Ason, et al. JCI Insight. 2020 Apr 23;5(8):e132898.
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