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AZD8871

Chemical Structure : AZD8871

CAS No.: 1435519-06-4

AZD8871 (AZD-8871, Navafenterol)

Catalog No.: PC-72979Not For Human Use, Lab Use Only.

AZD8871 (AZD-8871, Navafenterol) is a potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with pIC50 9.5 for human M3 receptor, pEC50 9.5 for β2-adrenoceptor.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

AZD8871 (AZD-8871, Navafenterol) is a potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with pIC50 9.5 for human M3 receptor, pEC50 9.5 for β2-adrenoceptor.
AZD8871 is selective for the β2-adrenoceptor over the β1 and β3 subtypes (3- and 6-fold, respectively) and shows dual antimuscarinic and β2-adrenoceptor functional activity in isolated guinea pig tissue (pIC50=8.6).
AZD8871 exhibits a higher muscarinic component than batefenterol in human bronchi, with a shift in potency under propranolol blockade of 2- and 6-fold, respectively.
AZD8871 prevents acetylcholine-induced bronchoconstriction in both guinea pig and dog with minimal effects on salivation and heart rate at doses with bronchoprotective activity.

Physicochemical Properties

M.Wt 742.91
Formula C38H42N6O6S2
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

trans-4-[[3-[5-[[[(2R)-2-(1,2-Dihydro-8-hydroxy-2-oxo-5-quinolinyl)-2-hydroxyethyl]amino]methyl]-1H-benzotriazol-1-yl]propyl]methylamino]cyclohexyl α-hydroxy-α-2-thienyl-2-thiopheneacetate

References

1. Singh D, et al. Respir Res. 2020 Sep 9;21(Suppl 1):102.

2. Balaguer V, et al. Respir Res. 2020 Sep 9;21(Suppl 1):212.

3. Aparici M, et al. J Pharmacol Exp Ther. 2019 Jul;370(1):127-136.

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