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Navafenterol saccharinate

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Catalog No. T30265Cas No. 1648550-37-1
Alias LAS-191351 saccharinate, LAS191351 saccharinate, AZD-8871 saccharinate, AZD8871 saccharinate

Navafenterol saccharinate (AZD-887 saccharinate) is an inhaled, dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist that demonstrates high affinity for the human M3 receptor with a pIC50 of 9.5 and strong β2-adrenoceptor agonism with a pEC50 of 9.5. Navafenterol provides a sustained bronchoprotective and antisialagogue effects with a favorable cardiovascular safety profile, and serving as a valuable investigational compound for chronic obstructive pulmonary disease research.

Navafenterol saccharinate

Navafenterol saccharinate

😃Good
Purity: 98.67%
Catalog No. T30265Alias LAS-191351 saccharinate, LAS191351 saccharinate, AZD-8871 saccharinate, AZD8871 saccharinateCas No. 1648550-37-1
Navafenterol saccharinate (AZD-887 saccharinate) is an inhaled, dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist that demonstrates high affinity for the human M3 receptor with a pIC50 of 9.5 and strong β2-adrenoceptor agonism with a pEC50 of 9.5. Navafenterol provides a sustained bronchoprotective and antisialagogue effects with a favorable cardiovascular safety profile, and serving as a valuable investigational compound for chronic obstructive pulmonary disease research.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$293-In Stock
5 mg$722-In Stock
10 mg$987-In Stock
25 mg$1,520-In Stock
50 mg$1,980-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:98.67%
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Product Introduction

Bioactivity
Description
Navafenterol saccharinate (AZD-887 saccharinate) is an inhaled, dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist that demonstrates high affinity for the human M3 receptor with a pIC50 of 9.5 and strong β2-adrenoceptor agonism with a pEC50 of 9.5. Navafenterol provides a sustained bronchoprotective and antisialagogue effects with a favorable cardiovascular safety profile, and serving as a valuable investigational compound for chronic obstructive pulmonary disease research.
In vitro
In binding and functional assays, Navafenterol saccharinate acted as a human M3 receptor antagonist (pIC50 9.5) and β2-adrenoceptor agonist (pEC50 9.5) [1].
In vivo
In preclinical models using guinea pigs and Beagle dogs, inhaled Navafenterol saccharinate prevents acetylcholine-induced bronchoconstriction. In dogs, a dosage of 10 ug/kg resulted in a bronchoprotective half-life exceeding 24 hours. The estimated IC50 for antisialagogue activity (138.4 ug/mL) was higher than the IC50 for bronchoconstriction inhibition (2.1 ug/mL). At doses providing bronchoprotection, minimal effects on heart rate or salivation were observed in these models [2].
SynonymsLAS-191351 saccharinate, LAS191351 saccharinate, AZD-8871 saccharinate, AZD8871 saccharinate
Chemical Properties
Molecular Weight926.09
FormulaC45H47N7O9S3
Cas No.1648550-37-1
SmilesO=S1(=O)C=2C(C(=O)N1)=CC=CC2.C(C(O[C@H]1CC[C@H](N(CCCN2C=3C(N=N2)=CC(CNC[C@H](O)C4=C5C(=C(O)C=C4)NC(=O)C=C5)=CC3)C)CC1)=O)(O)(C6=CC=CS6)C7=CC=CS7
Relative Density.no data available
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
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