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Azapetine

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Catalog No. T218848 Copy Product Info
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Azapetine is an α-adrenergic receptor antagonist with an IC50 of 0.205 μM for rat α1-adrenergic receptors and 1.3 μM for rat α2-adrenergic receptors. It effectively inhibits α1/α2-adrenergic receptor-mediated vasoconstriction in vascular smooth muscle. Azapetine is utilized in the study of peripheral vascular diseases.

Azapetine

Cas No. 146-36-1
Pack SizePriceUSA StockGlobal StockQuantity
10 mgInquiry10-14 weeks10-14 weeks
50 mgInquiry10-14 weeks10-14 weeks
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction

Bioactivity
Description
Azapetine is an α-adrenergic receptor antagonist with an IC50 of 0.205 μM for rat α1-adrenergic receptors and 1.3 μM for rat α2-adrenergic receptors. It effectively inhibits α1/α2-adrenergic receptor-mediated vasoconstriction in vascular smooth muscle. Azapetine is utilized in the study of peripheral vascular diseases.
Targets & IC50
α1-adrenoceptor (rat):0.205 μM
In vitro
Azapetine (45-60 min) exhibits a higher binding affinity for α1-adrenergic receptors compared to α2-adrenergic receptors in isolated rat brain cell membranes, with an IC50 of 0.205 μM for α1-adrenergic receptors and 1.3 μM for α2-adrenergic receptors.
In vivo
When administered via intravenous injection, Azapetine demonstrates in vivo functional blockade selectivity for α1-adrenergic receptors over α2-adrenergic receptors in decerebrospinal, normotensive Wistar rats, with a log selectivity ratio of 1.21.
Chemical Properties
Molecular Weight235.32
FormulaC17H17N
Cas No.146-36-1
SmilesC=CCN1CC=2C=CC=CC2C=3C=CC=CC3C1
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

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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:
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2 Enter the in vivo formulation:
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Related Tags: Azapetine in vivo | Azapetine in vitro | Azapetine formula | Azapetine molecular weight