APLNR agonist 35

Chemical Structure : APLNR agonist 35

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货号: PC-25632Not For Human Use, Lab Use Only.

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生物&药学活性

APLNR agonist 35 is a potent, CNS-penetrant biased agonist of peptidergic GPCR apelin receptor (APLNR, APJ) with cAMP EC50 of 10 nM, shows significant bias (∼8-fold) for G-protein over β-arrestin 2 signaling.
APLNR agonist 35 has a binding affinity (Ki) = 39.2 nM in radioligand displacement studies.
APLNR agonist 35 displays clear selectivity against a panel of high-risk receptors (Eurofins PanLabs, SafetyScreen) at 10 μM concentration.
APLNR agonist 35 (7.5 mpk, 15 mpk, or 30 mpk) significantly lowers the area under the curve (AUC) of oral glucose in obese mice.

物理化学性质&存储条件

分子量	499.83
分子式	C20H15ClF5N7O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-(2-Butyl-1-(3-(trifluoromethyl)pyridin-2-yl)-1H-imidazol-4-yl)-5-((5-chloropyrimidin-2-yl)difluoromethyl)-1,3,4-oxadiazole

参考文献

1. Narayanan S, et al. J Med Chem. 2025 Oct 20. doi: 10.1021/acs.jmedchem.5c01176.

APLNR agonist 35

生物&药学活性

物理化学性质&存储条件

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APLNR agonist 35

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物理化学性质&存储条件

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