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Azelaprag

(Synonyms: AMG 986) Copy Product Info
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Synonyms: AMG 986

Catalog No. T14390 Copy Product Info
Purity: 99.67%
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Azelaprag (AMG 986) is an oral apelin receptor agonist (EC50 = 0.32 nM). Azelaprag may be used to treat neurological disorders, cardiovascular diseases, and obesity with metabolic syndrome.
Azelaprag
Cas No. 2049980-18-7
Pack SizePriceUSA StockGlobal StockQuantity
1 mg$107In StockIn Stock
5 mg$263In StockIn Stock
10 mg$413In StockIn Stock
25 mg$629In StockIn Stock
1 mL x 10 mM (in DMSO)$336In StockIn Stock
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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Purity:99.67%
ee:100%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Azelaprag (AMG 986) is an oral apelin receptor agonist (EC50 = 0.32 nM). Azelaprag may be used to treat neurological disorders, cardiovascular diseases, and obesity with metabolic syndrome.
Targets & IC50
RAGE:12.7 ± 7.6 nM (kd), apelin receptor:0.32 nM (EC50)
In vitro
Methods: Primary human ADPKD renal epithelial cells were cultured in 3D collagen matrices and treated with 1 nmol/L to 1 μmol/L of Azelaprag; cyst growth was then assessed.
Results: Azelaprag inhibited cyst volume in a dose-dependent manner and reduced the number of cysts. [3]
In vivo
Methods: Pkd1^(RC/RC);Pkd2^(+/-) polycystic kidney mice were administered 2 mg/kg of Azelaprag via intraperitoneal injection daily for 27 days.
Results: Azelaprag reduced cyst count but did not significantly improve the corticomedullary ratio, cyst index, or renal function. [3]
SynonymsAMG 986
Chemical Properties
Molecular Weight523.61
FormulaC25H29N7O4S
Cas No.2049980-18-7
SmilesN(S([C@H]([C@H](C)C=1N=CC(C)=CN1)C)(=O)=O)C=2N(C(=NN2)C=3C=C(C)C=NC3)C4=C(OC)C=CC=C4OC
Relative Density.1.35 g/cm3 (Predicted)
Storage & Solubility Information
StorageStore at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 69.3 mg/mL (132.35 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.9098 mL9.5491 mL19.0982 mL95.4909 mL
5 mM0.3820 mL1.9098 mL3.8196 mL19.0982 mL
10 mM0.1910 mL0.9549 mL1.9098 mL9.5491 mL
20 mM0.0955 mL0.4775 mL0.9549 mL4.7745 mL
50 mM0.0382 mL0.1910 mL0.3820 mL1.9098 mL
100 mM0.0191 mL0.0955 mL0.1910 mL0.9549 mL
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
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.
1 Enter information below:
mg/kg
g
µL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

Related Tags: Azelaprag chemical structure | Azelaprag in vivo | Azelaprag in vitro | Azelaprag formula | Azelaprag molecular weight