| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| 1g | |||
| Other Sizes |
| Targets |
Lodenafil targets phosphodiesterase type 5, an enzyme that hydrolyzes cGMP in the corpus cavernosum. By inhibiting PDE5, it increases cGMP levels, leading to smooth muscle relaxation and increased blood flow to the penis, resulting in an erection. It is a sildenafil analog.
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|---|---|
| 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].
Lodenafil is a potent PDE5 inhibitor. It enhances acetylcholine-induced relaxation of isolated human corpus cavernosum and rabbit cavernosal strips precontracted with phenylephrine, with EC50 values of 676 and 589 nM, respectively. It is an active metabolite of lodenafil carbonate. |
| 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].
Lodenafil is used for the treatment of erectile dysfunction. It enhances male sexual function. It is a sildenafil analog. |
| Enzyme Assay |
Lodenafil is evaluated in cell-free enzymatic assays using purified PDE5. The compound is incubated with PDE5 and a substrate, and the inhibition of enzyme activity is measured. IC50 values are determined to quantify the potency of PDE5 inhibition.
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| Cell Assay |
Lodenafil is assessed in cell-based assays using corpus cavernosum smooth muscle cells. Cells are treated with Lodenafil, and cGMP levels and smooth muscle relaxation are measured.
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| Animal Protocol |
Lodenafil is administered orally in animal models to evaluate its effects on erectile function. It enhances acetylcholine-induced relaxation of isolated human corpus cavernosum and rabbit cavernosal strips.
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| ADME/Pharmacokinetics |
Lodenafil has a molecular weight of 504.60 and a molecular formula of C23H32N6O5S. It has a CAS number of 139755-85-4. The compound is a PDE5 inhibitor.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for Lodenafil. The compound is for research use only and is not intended for human therapeutic use. Its safety profile has not been extensively characterized.
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| References | |
| Additional Infomation |
A phosphodiesterase type 5 inhibitor; a vasodilator and urological drug used to treat erectile dysfunction and primary pulmonary hypertension.
Lodenafil is a potent PDE5 inhibitor. It has a CAS number of 139755-85-4. It is a sildenafil analog. It is not approved for clinical use. |
| Molecular Formula |
C23H32N6O5S
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|---|---|
| Molecular Weight |
504.606
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| Exact Mass |
504.215
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| CAS # |
139755-85-4
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| Related CAS # |
Lodenafil carbonate;398507-55-6
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| PubChem CID |
135452901
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| Appearance |
White to off-white solid powder
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| Density |
1.42g/cm3
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| Boiling Point |
730.6ºC at 760 mmHg
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| Melting Point |
183-185 °C
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| Flash Point |
395.7ºC
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| Vapour Pressure |
2.08E-22mmHg at 25°C
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| Index of Refraction |
1.667
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| LogP |
1.93
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
35
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| Complexity |
872
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NEYKRKVLEWKOBI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H32N6O5S/c1-4-6-18-20-21(27(3)26-18)23(31)25-22(24-20)17-15-16(7-8-19(17)34-5-2)35(32,33)29-11-9-28(10-12-29)13-14-30/h7-8,15,30H,4-6,9-14H2,1-3H3,(H,24,25,31)
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| Chemical Name |
5-[2-ethoxy-5-[4-(2-hydroxyethyl)piperazin-1-yl]sulfonylphenyl]-1-methyl-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-7-one
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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.
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