Sildenafil Citrate

Catalog No.S1431 1 Product Citations

Sildenafil, a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5), is a well-tolerated and highly effective treatment for erectile dysfunction.

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In DMSO USD 90 In stock
USD 70 In stock
USD 110 In stock
USD 670 In stock
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Sildenafil Citrate Chemical Structure

Sildenafil Citrate Chemical Structure
Molecular Weight: 666.7

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Sildenafil Citrate is available in the following compound libraries:

Product Information

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Product Description

Biological Activity

Description Sildenafil, a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5), is a well-tolerated and highly effective treatment for erectile dysfunction.
Targets PDE5 [1] PDE6 [1]
IC50 3.5 nM 33 nM
In vitro Sildenafil citrate is a potent PDE type 5 reversible and selective inhibitor that blocks cGMP hydrolysis effectively (Ki ∼3 nM). Sildenafil exhibited high affinity for PDE type 5 and type 6 with inhibition constants (Ki) of ∼3.5 and 33 nM, respectively. Sildenafil enhances sodium nitroprusside- or transmural electrical stimulation-induced relaxation of precontracted corpus cavernosum muscle strips in organ baths, suggesting that sildenafil augments the activity of NO-mediated relaxation. Sildenafil citrate increases intracellular cGMP concentrations in cultured smooth muscle cells treated with sodium nitroprusside and in rabbit corpus cavernosum in vitro. Sildenafil is metabolized in the liver by cytochrome P450 and is converted into an active metabolite with characteristics similar to the parent compound. [1]
In vivo Sildenafil citrate enhances erectile function following pelvic nerve stimulation in anesthetized dogs as measured by increased intracavernosal pressure. [1] Sildenafil citrate significantly reverses impaired carbachol-stimulated relaxation and inhibits superoxide formation by cavernosal tissue from hypercholesterolaemic rabbits. [2] Sildenafil improves erectile function in a time- and dose-dependent fashion with maximization of erectile function recovery occurring with daily 20 mg/kg at the 28-day time point in Sprague-Dawley rats. Sildenafil use results in smooth muscle-collagen ratio protection and CD31 and eNOS expression preservation in Sprague-Dawley rats. Sildenafil reduces apoptotic indices significantly compared with control, and increases phosphorylation of akt and eNOS in Sprague-Dawley rats. [3]
Features

Protocol(Only for Reference)

1

References

[1] Nehra A, et al. World J Urol, 2001, 19(1), 40-45.

[2] Shukla N, et al. Eur J Pharmacol, 2005, 517(3), 224-231.

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Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02057458 Not yet recruiting Cystic Fibrosis National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) 2014-04 Phase 2
NCT01954524 Not yet recruiting Cirrhosis University of Maryland 2014-05 Phase 1
NCT02114775 Not yet recruiting Traumatic Brain Injury The University of Texas, Galveston 2014-06 Phase 1
NCT02060487 Not yet recruiting Pulmonary Arterial Hypertension Pfizer 2014-08 Phase 4
NCT01132482 Withdrawn Cystic Fibrosis National Jewish Health 2014-10 Phase 2

Chemical Information

Download Sildenafil Citrate SDF
Molecular Weight (MW) 666.7
Formula

C22H30N6O4S.C6H8O7

CAS No. 171599-83-0
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms
Solubility (25°C) * In vitro DMSO 23 mg/mL (34 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% PEG400/0.5% Tween80/5% propylene glycol, 30 mg/mL
* <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 1-[[3-(6,7-Dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-ethoxyphenyl]sulfonyl]-4-methylpiperazine, 2-hydroxy-1,2,3-propanetricarboxylate

Research Area

Product Citations (1)

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