| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| Targets |
Lodenafil carbonate targets phosphodiesterase type 5 (PDE5), the primary enzyme responsible for cGMP hydrolysis in corpus cavernosum smooth muscle. By inhibiting PDE5, it increases cGMP levels, leading to smooth muscle relaxation and increased penile blood flow. This mechanism is shared with other PDE5 inhibitors used for erectile dysfunction.
|
|---|---|
| ln Vitro |
In vitro activity of Lodenafil carbonate is primarily assessed through PDE5 enzyme inhibition assays. The prodrug is expected to be converted to active Lodenafil in vivo, which then inhibits PDE5 activity. Detailed in vitro IC50 values for the prodrug itself are not extensively reported, as its activity depends on metabolic conversion to the active form.
|
| ln Vivo |
In vivo, Lodenafil carbonate delivers active Lodenafil following oral administration. It is used for the treatment of erectile dysfunction. The prodrug design provides improved oral bioavailability compared to the parent compound. In vivo efficacy is demonstrated in animal models and clinical studies for ED treatment.
|
| Enzyme Assay |
Non-cell-based enzyme assays for Lodenafil carbonate involve PDE5 enzyme inhibition studies. Purified PDE5 enzyme is incubated with the compound and substrate (cGMP) at varying concentrations. Enzyme activity is measured by quantifying cGMP hydrolysis using radioactive or fluorescence-based detection methods. IC50 values are determined by plotting percent inhibition against compound concentration. The prodrug may require pre-incubation with esterases to assess activity of the active metabolite.
|
| Cell Assay |
Cellular assays for Lodenafil carbonate are not typically performed, as the compound is a prodrug designed for oral administration. Instead, assays focus on PDE5 inhibition in cell-free systems or use cells expressing PDE5 to assess downstream effects on cGMP levels. Smooth muscle cell relaxation assays may be used to confirm functional activity following metabolic activation.
|
| Animal Protocol |
In vivo animal models for Lodenafil carbonate would include standard erectile dysfunction models such as cavernous nerve stimulation in rats or other species. Oral administration of the prodrug is followed by assessment of intracavernosal pressure responses to nerve stimulation. These models evaluate the compound's ability to enhance erectile function through PDE5 inhibition. Detailed protocols are not extensively reported.
|
| ADME/Pharmacokinetics |
Lodenafil carbonate has a molecular weight of 1035.21 g/mol and molecular formula C47H62N12O11S2. The compound is soluble in DMSO. Storage: powder at -20°C for 3 years; in solvent at -80°C for 1 year. As a prodrug dimer, it is designed to improve oral bioavailability and pharmacokinetic properties compared to the parent compound.
|
| Toxicity/Toxicokinetics |
Lodenafil carbonate is a research compound for laboratory use only. Detailed toxicity data are not extensively reported in the available literature. As a PDE5 inhibitor, potential side effects would be expected to be similar to other drugs in this class, including headache, flushing, and hypotension. Standard preclinical toxicity assessments would be required for therapeutic development.
|
| References |
|
| Additional Infomation |
Lodinafil carbonate has been used in trials investigating its use in the treatment of coronary artery disease and erectile dysfunction.
Lodenafil carbonate has CAS number 398507-55-6. It is a dimeric prodrug that delivers Lodenafil in vivo. The compound is an orally active PDE5 inhibitor indicated for erectile dysfunction. It is also known as carbonate lodenafil and is used in research applications studying PDE5 inhibition and erectile dysfunction therapy. |
| Molecular Formula |
C47H62N12O11S2
|
|---|---|
| Molecular Weight |
1035.19898
|
| Exact Mass |
1034.41
|
| CAS # |
398507-55-6
|
| Related CAS # |
Lodenafil;139755-85-4
|
| PubChem CID |
135431100
|
| Appearance |
White to off-white solid powder
|
| Boiling Point |
1109.0±75.0 °C(Predicted)
|
| Melting Point |
229-231 °C
|
| LogP |
5.042
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
19
|
| Rotatable Bond Count |
22
|
| Heavy Atom Count |
72
|
| Complexity |
2020
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
MVYUCRDXZXLFSB-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C47H62N12O11S2/c1-7-11-35-39-41(54(5)52-35)45(60)50-43(48-39)33-29-31(13-15-37(33)67-9-3)71(63,64)58-21-17-56(18-22-58)25-27-69-47(62)70-28-26-57-19-23-59(24-20-57)72(65,66)32-14-16-38(68-10-4)34(30-32)44-49-40-36(12-8-2)53-55(6)42(40)46(61)51-44/h13-16,29-30H,7-12,17-28H2,1-6H3,(H,48,50,60)(H,49,51,61)
|
| Chemical Name |
bis[2-[4-[4-ethoxy-3-(1-methyl-7-oxo-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-5-yl)phenyl]sulfonylpiperazin-1-yl]ethyl] carbonate
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9660 mL | 4.8300 mL | 9.6600 mL | |
| 5 mM | 0.1932 mL | 0.9660 mL | 1.9320 mL | |
| 10 mM | 0.0966 mL | 0.4830 mL | 0.9660 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
