Navafenterol
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.
- CAS No.: 1435519-06-4
- Formula: C38H42N6O6S2
- Molecular Weight:742.91
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
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mAChR3 |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Dunkin Hartley guinea pigs (body weight 340-600 g) bearing bronchoconstriction model[1]
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Dosage:10, 30, 100, and 300 μg/mL
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Administration:Administered by aerosol
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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.
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Animal Model:Male anesthetized Beagle dogs[1]
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Dosage:0.3, 1, 3, or 10 µg/kg
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Administration:Administered as nebulized liquid aerosols; the administration volume was 3 mL
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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.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1435519-06-4
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Molecular Weight 742.91
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Formula C38H42N6O6S2
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SMILES
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
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Synonyms
AZD-8871; LAS191351
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Navafenterol Related Classifications
HY-120802 Related Classifications
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