AZD-8871
- Product Name
- AZD-8871
- CAS No.
- 1435519-06-4
- Chemical Name
- AZD-8871
- Synonyms
- AZD-8871;LAS191351;Navafenterol;Navafenterol/AZD-8871/LAS191351;2-Thiopheneacetic acid, α-hydroxy-α-2-thienyl-, 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 ester
- CBNumber
- CB14667295
- Molecular Formula
- C38H42N6O6S2
- Formula Weight
- 742.91
- MOL File
- 1435519-06-4.mol
AZD-8871 Property
- Boiling point:
- 988.8±65.0 °C(Predicted)
- Density
- 1.45±0.1 g/cm3(Predicted)
- pka
- 8.88±0.20(Predicted)
AZD-8871 Chemical Properties,Usage,Production
Uses
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 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: | 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.? |
IC 50
mAChR3
References
[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. DOI:10.1124/jpet.118.255620
AZD-8871 Preparation Products And Raw materials
Raw materials
Preparation Products
AZD-8871 Suppliers
- Tel
- 010-88886666-01 13112345678
- Fax
- CDXH21@126.com
- loyson@tcypharm.com
- Country
- China
- ProdList
- 597
- Advantage
- 55
- Tel
- 0513-66337626 18051384581
- sales@chemhifuture.com
- Country
- China
- ProdList
- 5929
- Advantage
- 58
- Tel
- 15363639686
- heshuoyiyao@hotmail.com
- Country
- China
- ProdList
- 2377
- Advantage
- 58
- Tel
- 15002134094
- marketing@targetmol.cn
- Country
- China
- ProdList
- 29257
- Advantage
- 58
- Tel
- +1-781-999-5354;
- support@targetmol.com
- Country
- United States
- ProdList
- 39035
- Advantage
- 58