1. GPCR/G Protein
    Neuronal Signaling
  2. mAChR
    Adrenergic Receptor
  3. Navafenterol

Navafenterol (Synonyms: AZD-8871; LAS191351)

Cat. No.: HY-120802
Handling Instructions

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.

For research use only. We do not sell to patients.

Navafenterol Chemical Structure

Navafenterol Chemical Structure

CAS No. : 1435519-06-4

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Description

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].

In Vitro

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].

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

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].

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

Animal Model: Male Dunkin Hartley guinea pigs (body weight 340-600 g) bearing bronchoconstriction model[1]
Dosage: 10, 30, 100, and 300 μg/mL
Administration: Administered by aerosol
Result: Inhibited the bronchoconstriction in a concentration-response manner with the IC50 value of 2.1 µg/mL.
Exhibited the antisialagogue effect with a maximal inhibition of sialorrhea of 65%±11% at 300 µg/mL and an estimated IC50 of 138.4 µg/mL.
Animal Model: Male anesthetized Beagle dogs[1]
Dosage: 0.3, 1, 3, or 10 µg/kg
Administration: Administered as nebulized liquid aerosols; the administration volume was 3 mL
Result: Showed significant effects over 24 hours at all the doses tested (0.3-10 µg/kg).
Showed long-lasting effects at 10 µg/kg, with a 79% ± 3.6% of bronchoprotection at 24 hours and a calculated half-life longer than 24 hours. 
Molecular Weight

742.91

Formula

C₃₈H₄₂N₆O₆S₂

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Navafenterol
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HY-120802
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