Size | Price | Stock | Qty |
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5mg |
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10mg |
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50mg |
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100mg |
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Other Sizes |
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ln Vitro |
The electroretinogram (ERG) amplitude recorded from the isolated rat retina that has acclimated to darkness is increased by N-Desmethyl Sildenafil, most likely because to an improvement in the response of the photoreceptor cells[1]. By co-expressing cytochrome b5 and human P450 oxidoreductase, CYP3A supersomes are used to investigate the synthesis of N-Desmethyl Sildenafil. CYP3A4, CYP3A5, and, to a lesser extent, CYP3A7 catalyze N-Desmethyl Sildenafil[2].
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References |
[1]. Péter Barabás, et al. Sildenafil, N-desmethyl-sildenafil and Zaprinast enhance photoreceptor response in the isolated rat retina. Neurochem Int. 2003 Nov;43(6):591-5.
[2]. Rikako Takahiro, et al. Contribution of CYP3A isoforms to dealkylation of PDE5 inhibitors: a comparison between sildenafil N-demethylation and tadalafil demethylenation. Biol Pharm Bull. 2015;38(1):58-65. |
Molecular Formula |
C21H28N6O4S
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Molecular Weight |
460.55
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CAS # |
139755-82-1
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Related CAS # |
N-Desmethyl Sildenafil-d8;1185168-06-2
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
S(C1C([H])=C([H])C(=C(C2=NC3C(C([H])([H])C([H])([H])C([H])([H])[H])=NN(C([H])([H])[H])C=3C(N2[H])=O)C=1[H])OC([H])([H])C([H])([H])[H])(N1C([H])([H])C([H])([H])N([H])C([H])([H])C1([H])[H])(=O)=O
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: 250 mg/mL (542.83 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.52 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.52 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1713 mL | 10.8566 mL | 21.7132 mL | |
5 mM | 0.4343 mL | 2.1713 mL | 4.3426 mL | |
10 mM | 0.2171 mL | 1.0857 mL | 2.1713 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.