Avanafil

Catalog No.S4019

For research use only.

Avanafil is a highly selective PDE5 inhibitor with IC50 of 5.2 nM, >121-fold selectivity over other PDEs.

Avanafil Chemical Structure

CAS No. 330784-47-9

Selleck's Avanafil has been cited by 1 Publication

Purity & Quality Control

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Biological Activity

Description Avanafil is a highly selective PDE5 inhibitor with IC50 of 5.2 nM, >121-fold selectivity over other PDEs.
Features Highly selective for PDE5.
Targets
PDE5 [1]
1 nM
In vivo Avanafil (i.v.) potentiates penile tumescence with ED200% of 37.5 μg/kg in dogs. Furthermore, intraduodenal treatment of Avanafil potentiates pelvic nerve stimulation induced changes in intracavernous pressure and duration. [1] The cavernous injection of avanafil (1 μM) in T2DM rats results in partial improvement in erectile responses. [2]

Protocol (from reference)

Animal Research:[1]
  • Animal Models: Male mongrel dogs
  • Dosages: 1-300 μg/kg
  • Administration: Intraduodenal treatment or i.v.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 97 mg/mL
(200.43 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 483.95
Formula

C23H26ClN7O3

CAS No. 330784-47-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COC1=C(C=C(C=C1)CNC2=NC(=NC=C2C(=O)NCC3=NC=CC=N3)N4CCCC4CO)Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04374994 Completed Drug: Avanafil 50 MG|Drug: Placebo oral tablet Erectile Dysfunction University of Alexandria September 1 2018 Phase 4
NCT01095601 Completed Drug: Avanafil Healthy VIVUS LLC April 2010 Phase 1
NCT01117038 Completed Drug: avanafil and enalapril|Drug: avanafil and amlodipine Erectile Dysfunction VIVUS LLC April 2010 Phase 1
NCT01054430 Completed Drug: avanafil Erectile Dysfunction VIVUS LLC January 2010 Phase 1
NCT01054261 Completed Drug: avanafil Renal VIVUS LLC January 2010 Phase 1
NCT00914511 Completed Drug: avanafil 200mg Avanfil ADME|Semen Exposure|Sperm Function VIVUS LLC May 2009 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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