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Avanafil PDE inhibitor

Name: Avanafil
Brand: Selleck Chemicals
SKU: S4019
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S4019

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

Chemical Structure

Molecular Weight: 483.95

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.91%

99.91

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Chemical Information, Storage & Stability

Molecular Weight	483.95	Formula	C₂₃H₂₆ClN₇O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	330784-47-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	COC1=C(C=C(C=C1)CNC2=NC(=NC=C2C(=O)NCC3=NC=CC=N3)N4CCCC4CO)Cl

Solubility

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.850mg/ml (10.02mM)	Taking the 1 mL working solution as an example, add 50 μL of 97 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.800mg/ml (1.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 16 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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.

Mechanism of Action

Features	Highly selective for PDE5.
Targets/IC₅₀/Ki	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 this compound potentiates pelvic nerve stimulation induced changes in intracavernous pressure and duration. ^[1] The cavernous injection of this chemical (1 μM) in T2DM rats results in partial improvement in erectile responses. ^[2]
References	https://pubmed.ncbi.nlm.nih.gov/22704456/ https://pubmed.ncbi.nlm.nih.gov/24331245/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

Tech Support

Handling Instructions

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