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

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

目录号: HY-120802A
产品使用指南

摩尔计算器

Navafenterol (AZD-8871) 是一种吸入型的双效、选择性和持久的 M3-拮抗剂/β2-激动剂 (MABA)，具有持久作用和良好的安全性。对人 M3 受体的 pIC50 为 9.5，β2-肾上腺素受体的 pEC50 为 9.5。Navafenterol 可用于慢性阻塞性肺疾病 (COPD) 的研究。具有支气管保护和抗唾液分泌作用，且具有良好的心血管特征。

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Navafenterol saccharinate Chemical Structure

Navafenterol saccharinate Chemical Structure

CAS No. : 1648550-37-1

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Other Forms of Navafenterol saccharinate:

Navafenterol saccharinate 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(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.

Navafenterol saccharinate 相关抗体:
体内研究
(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. 
Clinical Trial
分子量

926.09

Formula

C45H47N7O9S3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Navafenterol saccharinate 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Navafenterol1648550-37-1AZD-8871LAS191351AZD8871AZD 8871LAS 191351LAS-191351mAChRAdrenergic ReceptorMuscarinic acetylcholine receptorBeta ReceptorInhaleddual-acting,long-lastingM3-antagonist,β2-agonistMABAchronicobstructivepulmonarydiseaseCOPDBronchoprotectiveantisialagogueInhibitorinhibitorinhibit

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