Size | Price | Stock | Qty |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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Lodenafil (also known as hydroxyhomosildenafil; trade name Helleva), an analog of sildenafil, is a novel and potent phosphodiesterase PDE5 inhibitor with the potential to treat erectile dysfunction (ED).
ln Vitro |
Lodenafil (0-100 µM, 20 minutes) causes relaxation of rabbit and human corpus cavernosum strips precontracted with deoxygenate (10 µM) [1]. Lodenafil (0-1 μM, 5 minutes) suppresses cGMP (IC50: 0.022 μM)[1].
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ln Vivo |
Lodenafil (10 mg) showed a T1/2 of 4.32 hours, a Cmax of 1357 ng/mL, and an AUC0-24 of 9091 ng/h/mL in the tough Beagle dog PK experiment [1].
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References |
[1]. Toque HA, et al. Pharmacological characterization of a novel phosphodiesterase type 5 (PDE5) inhibitor lodenafil carbonate on human and rabbit corpus cavernosum. Eur J Pharmacol. 2008 Sep 4;591(1-3):189-95.
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Molecular Formula |
C23H32N6O5S
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Molecular Weight |
504.606
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Exact Mass |
504.2155
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CAS # |
139755-85-4
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Related CAS # |
Lodenafil carbonate;398507-55-6
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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(C([H])([H])C([H])([H])O[H])C([H])([H])C1([H])[H])(=O)=O
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Synonyms |
trade name Helleva; hydroxyhomosildenafil; Lodenafil
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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 (~495.44 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.12 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 (4.12 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.9817 mL | 9.9086 mL | 19.8173 mL | |
5 mM | 0.3963 mL | 1.9817 mL | 3.9635 mL | |
10 mM | 0.1982 mL | 0.9909 mL | 1.9817 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.