Navafenterol saccharinate  (Synonyms: AZD-8871 saccharinate; LAS191351 saccharinate)

Navafenterol (AZD-8871) saccharinate is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC₅₀ is 9.5 for human M3 receptor, and the pEC₅₀ is 9.5 for β2-adrenoceptor. Navafenterol saccharinate can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile^[1].

The pIC₅₀ values of Navafenterol (AZD-8871) at the human M1, M2, M3, M4, and M5 receptor are 9.9, 9.9, 9.5, 10.4, and 8.8, respectively^[1].
pEC₅₀ values of Navafenterol at theβ1, β2, and β3 adrenoceptor are 9.0, 9.5, and 8.7, respectively. It is selective for the β2-adrenoceptor over the β1 and β3 subtypes (3- and 6-fold, respectively)^[1].
Navafenterol shows kinetic selectivity for the M3 (half-life: 4.97 hours) over the M2 receptor (half-life: 0.46 hour)^[1].
Navafenterol shows dual antimuscarinic and β2-adrenoceptor functional activity in isolated guinea pig tissue (pIC₅₀ in electrically stimulated trachea: 8.6; pEC₅₀ in spontaneous tone isolated trachea: 8.8, respectively), which are sustained over time^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Navafenterol (AZD-8871) prevents acetylcholine-induced bronchoconstriction in both guinea pig and dog with minimal effects on salivation and heart rate at doses with bronchoprotective activity. Moreover, AZD8871 shows long-lasting effects in dog, with a bronchoprotective half-life longer than 24 hours. Navafenterol shows dose-proportional bronchoprotective effect, with a nonsignificantly different potency (ID₄₀ of 0.40 µg/kg)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

926.09

C₄₅H₄₇N₇O₉S₃

1648550-37-1

O=C(C(O)(C1=CC=CS1)C2=CC=CS2)O[C@H]3CC[C@@H](CC3)N(C)CCCN4N=NC5=CC(CNC[C@H](O)C6=CC=C(C7=C6C=CC(N7)=O)O)=CC=C54.O=S8(C9=CC=CC=C9C(N8)=O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Mònica Aparici, et al. Pharmacological Profile of AZD8871 (LAS191351), a Novel Inhaled Dual M3 Receptor Antagonist/ β 2-Adrenoceptor Agonist Molecule with Long-Lasting Effects and Favorable Safety Profile. J Pharmacol Exp Ther. 2019 Jul;370(1):127-136.  [Content Brief]