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Sildenafil-d3

Catalog No.GC48078

An internal standard for the quantification of sildenafil

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Sildenafil-d3 Chemical Structure

Cas No.: 1126745-90-1

Size Price Stock Qty
500 μg
$102.00
In stock
1 mg
$194.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

Sildenafil-d3 is intended for use as an internal standard for the quantification of sildenafil by GC- or LC-MS. Sildenafil is a potent inhibitor of phosphodiesterase 5 (PDE5) with IC50 values of 3.6 and 3 nM for PDE5 activity in isolated rabbit platelets and human corpus cavernosum, respectively.1 It is selective for PDE5 over PDE1 and PDE3 (IC50s = 0.26 and 65 μM, respectively). Sildenafil reverses glucose-induced decreases in angiopoietin 1 (Ang1) expression and reduction of capillary-like tube formation by mouse dermal endothelial cells in vitro and increases the number of functional blood vessels and regional blood flow in the sciatic nerve in a db/db mouse model of diabetic peripheral neuropathy.2 It increases the ratio of maximum intracavernosal pressure to mean arterial blood pressure (ICP/MAP), a measure of erectile function, in castrated rats when administered at a dose of 20 mg/kg per day.3 Sildenafil (0.5 mg/kg) also reduces cardiac arrest and resuscitation-induced increases in angiotensin II , angiotensin converting enzyme (ACE), ACE2, and various angiotensin receptors and increases survival in a porcine model of ischemia/reperfusion injury.4 Formulations containing sildenafil have been used in the treatment of erectile dysfunction, pulmonary arterial hypertension, and high-altitude pulmonary edema associated with altitude sickness.

1.Terrett, N.K., Bell, A.S., Brown, D., et al.Sildenafil (ViagraT), a potent and selective inhibitor of type 5 cGMP phosphodiesterase with utility for the treatment of male erectile dysfunctionBioorganic & Medicinal Chemistry Letters6(15)1819-1824(1996) 2.Wang, L., Chopp, M., Szalad, A., et al.Sildenafil ameliorates long term peripheral neuropathy in type II diabetic micePLoS One10(2)e0118134(2015) 3.Mulhall, J.P., Verma, N., Deveci, S., et al.Sildenafil citrate improves erectile function after castration in a rat modelBJU Int.113(4)656-661(2014) 4.Wang, G., Zhang, Q., Yuan, W., et al.Sildenafil protects against myocardial ischemia-reperfusion injury following cardiac arrest in a porcine model: Possible role of the renin-angiotensin systemInt. J. Mol. Sci.16(11)27015-27031(2015)

Chemical Properties

Cas No. 1126745-90-1 SDF
Canonical SMILES CCOC1=C(C(NC2=C3N(C)N=C2CCC)=NC3=O)C=C(C=C1)S(N4CCN(C([2H])([2H])[2H])CC4)(=O)=O
Formula C22H27D3N6O4S M.Wt 477.6
Solubility DMF: 5 mg/ml,DMSO: 10 mg/ml Storage Store at -20°C, protect from light, stored under nitrogen
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.0938 mL 10.469 mL 20.938 mL
5 mM 0.4188 mL 2.0938 mL 4.1876 mL
10 mM 0.2094 mL 1.0469 mL 2.0938 mL
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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.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 19 reference(s) in Google Scholar.)

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