Avanafil

Catalog No.S4019

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

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Avanafil Chemical Structure

Avanafil Chemical Structure
Molecular Weight: 483.95

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Quality Control & MSDS

Product Information

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Product Description

Biological Activity

Description Avanafil is a highly selective PDE5 inhibitor with IC50 of 5.2 nM, >121-fold selectivity over other PDEs.
Targets PDE5 [1]
IC50 1 nM
In vitro
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]
Features Highly selective for PDE5.

Protocol(Only for Reference)

Kinase Assay: [1]

PDE Assay PDE1, 2, 3, 4, 5 and 6 activity is assayed using 1 μM cGMP, 1 μM cGMP, 1 μM cAMP, 1 μM cAMP, 1 μM cGMP and 10 μM cGMP, respectively, as the substrate. PDE7, 8, 9, 10 and 11 activity is assayed using 0.1 μM cAMP, 0.05 μM cAMP, 0.05 μM cGMP, 0.25 μM cAMP and 1 μM cGMP, respectively, as the substrate. PDE assay is done by the radiolabeled nucleotide method.7 PDE enzyme (100 μl) in 50 mM Tris-HCl (pH 8.) is added to 200 μl assay buffer composed of 50 mM Tris-HCl (pH 8.0), 12.5 mM MgCl2, 10 mM 2-mercaptoethanol and 0.825 mg/ml bovine serum albumin. The enzyme reaction is started by adding 200 μl substrate solution containing [3H]cGMP plus unlabeled cGMP or [3H]cAMP plus unlabeled cAMP in 50 mM Tris-HCl (pH 8.0). Reaction mixtures are incubated at 37C for 30 minutes and then boiled for 1.5 minutes. Subsequently 100 μl 1 mg/ml Crotalus atrox snake venom are added and incubated at 37C for 30 minutes. The reaction is stopped by adding 500 μl methanol. Resultant solutions are applied to a Dowex (1 × 8, 200 to 400) column (volume 0.225 ml). Eluate radioactivity is measured with 5 ml aqueous scintillation cocktails. DMSO solution without the compounds served as a control. The final concentration of DMSO in the reaction mixture is 1% volume per volume.

Animal Study: [1]

Animal Models Male mongrel dogs
Formulation 0.05N HCl (intraduodenal); Saline containing 0.01N HCl (i.v.)
Dosages 1-300 μg/kg
Administration Intraduodenal treatment or i.v.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Kotera J, et al. J Urol. 2012, 188(2), 668-674.

[2] Yilmaz D, et al. Urology. 2014, 83(2), 508, e7-12.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-23)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02503306 Completed Sexual Function and Fertility Disorders NEC-Erectile Dysfunction Sanofi July 2015 Phase 3
NCT01768676 Completed Erectile Dysfunction VIVUS, Inc. December 2012 Phase 4
NCT01698684 Completed Erectile Dysfunction VIVUS, Inc. September 2012 Phase 4
NCT01705197 Completed Erectile Dysfunction JW Pharmaceutical February 2012 Phase 3
NCT01095601 Completed Healthy VIVUS, Inc. April 2010 Phase 1

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Chemical Information

Download Avanafil SDF
Molecular Weight (MW) 483.95
Formula

C23H26ClN7O3

CAS No. 330784-47-9
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 97 mg/mL (200.43 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or 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 Name 5-Pyrimidinecarboxamide, 4-[[(3-chloro-4-methoxyphenyl)methyl]amino]-2-[(2S)-2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2-pyrimidinylmethyl)-

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.

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