Chemical Structure : APLNR agonist 35
CAS No.:
APLNR agonist 35
Catalog No.: PC-25632Not For Human Use, Lab Use Only.
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.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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499.83
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Formula
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C20H15ClF5N7O
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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2-(2-Butyl-1-(3-(trifluoromethyl)pyridin-2-yl)-1H-imidazol-4-yl)-5-((5-chloropyrimidin-2-yl)difluoromethyl)-1,3,4-oxadiazole
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References
1. Narayanan S, et al. J Med Chem. 2025 Oct 20. doi: 10.1021/acs.jmedchem.5c01176.
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