Avanafil

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

Avanafil Chemical Structure

Avanafil Chemical Structure

CAS No. 330784-47-9

Purity & Quality Control

Avanafil Related Products

Signaling Pathway

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
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]
Animal Research Animal Models Male mongrel dogs
Dosages 1-300 μg/kg
Administration Intraduodenal treatment or i.v.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04374994 Completed
Erectile Dysfunction
University of Alexandria
September 1 2018 Phase 4
NCT01095601 Completed
Healthy
VIVUS LLC
April 2010 Phase 1
NCT01117038 Completed
Erectile Dysfunction
VIVUS LLC
April 2010 Phase 1
NCT01054430 Completed
Erectile Dysfunction
VIVUS LLC
January 2010 Phase 1
NCT01054261 Completed
Renal
VIVUS LLC
January 2010 Phase 1
NCT00914511 Completed
Avanfil ADME|Semen Exposure|Sperm Function
VIVUS LLC
May 2009 Phase 1

Chemical Information & Solubility

Molecular Weight 483.95 Formula

C23H26ClN7O3

CAS No. 330784-47-9 SDF Download Avanafil SDF
Smiles COC1=C(C=C(C=C1)CNC2=NC(=NC=C2C(=O)NCC3=NC=CC=N3)N4CCCC4CO)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 97 mg/mL ( (200.43 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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.

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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