| Bioactivity | Navafenterol (AZD-8871) 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 can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile[1]. |
| Invitro | 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]. |
| In Vivo | 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]. Animal Model: |
| Name | Navafenterol |
| CAS | 1435519-06-4 |
| Formula | C38H42N6O6S2 |
| Molar Mass | 742.91 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |
Navafenterol
CAS: 1435519-06-4 F: C38H42N6O6S2 W: 742.91
Navafenterol (AZD-8871) is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA
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