| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
Carbodenafil targets phosphodiesterase type 5 (PDE5), the same enzyme targeted by Sildenafil and other PDE5 inhibitors. PDE5 is the primary phosphodiesterase responsible for the hydrolysis of cGMP in the corpus cavernosum of the penis. Inhibition of PDE5 increases cGMP levels, leading to smooth muscle relaxation and increased blood flow. Sildenafil is a potent PDE5 inhibitor with an IC50 of 5.22 nM. Carbodenafil is a structural analog of Sildenafil.
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| ln Vitro |
In vitro studies have demonstrated that Carbodenafil is a PDE5 inhibitor structurally related to Sildenafil. As a Sildenafil-related compound found in health foods, it likely exhibits similar PDE5 inhibitory activity. Sildenafil is a potent PDE5 inhibitor with an IC50 of 5.22 nM. Carbodenafil has been studied for its pharmacological profile and structural similarities to clinically approved PDE5 inhibitors. Further detailed in vitro characterization data are limited.
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| ln Vivo |
In vivo studies of Carbodenafil are limited. As a PDE5 inhibitor structurally related to Sildenafil, it is expected to have similar pharmacological effects including vasodilation and increased blood flow. Sildenafil and other PDE5 inhibitors are used for the treatment of erectile dysfunction. Carbodenafil has been found in health foods, suggesting it may be used as an adulterant in dietary supplements. Detailed in vivo pharmacokinetic and efficacy studies are limited.
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| Enzyme Assay |
In vitro enzyme/receptor binding (non-cell) assays for Carbodenafil typically involve PDE5 inhibition studies using recombinant human PDE5. The enzyme is incubated with increasing concentrations of Carbodenafil (0.01 nM - 10 μM) and a substrate (e.g., ³H-cGMP or a fluorogenic cGMP analog) in assay buffer at 37°C for 30-60 minutes. The hydrolysis of cGMP is measured by scintillation counting or fluorescence. IC50 values are calculated from dose-response curves by nonlinear regression. Selectivity for PDE5 over other PDE isoforms (PDE1-4, PDE6-11) can be assessed using similar assays. Sildenafil is used as a positive control.
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| Cell Assay |
For in vitro cell-based assays, cells expressing PDE5 (e.g., vascular smooth muscle cells) are cultured in appropriate media. Cells are treated with Carbodenafil at concentrations ranging from 0.01-10 μM for 1-24 hours. PDE5 inhibition is assessed by measuring cGMP levels in cells using ELISA or radioimmunoassay. Cells are typically stimulated with nitric oxide donors (e.g., sodium nitroprusside) to increase cGMP production. Cell viability is assessed by MTT or CCK-8 assays. The compound's effects on smooth muscle relaxation can be assessed using isolated tissue preparations.
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| Animal Protocol |
In vivo animal studies with Carbodenafil are limited. As a PDE5 inhibitor, it could be administered orally to animal models to study its effects on erectile function, pulmonary hypertension, or other PDE5-mediated processes. Hemodynamic parameters including blood pressure and heart rate would be measured. However, specific published protocols are limited. The compound is primarily known as a Sildenafil-related compound found in health foods.
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| ADME/Pharmacokinetics |
Carbodenafil has a molecular weight of 452.54 g/mol and molecular formula C24H32N6O3. Chemical name: 5-[2-ethoxy-5-[(4-ethyl-1-piperazinyl)carbonyl]phenyl]-1,6-dihydro-1-methyl-3-propyl-7H-pyrazolo[4,3-d]pyrimidin-7-one. The compound is also known as Fondenafil. Pharmacokinetic properties are expected to be similar to other PDE5 inhibitors. The compound is found in health foods as an adulterant. It is not approved as a therapeutic drug.
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| Toxicity/Toxicokinetics |
As a PDE5 inhibitor structurally related to Sildenafil, Carbodenafil is expected to have a similar side effect profile, including headache, flushing, dyspepsia, and hypotension. The compound is found in health foods as an adulterant, raising concerns about unregulated use. The compound is not approved as a therapeutic drug and should not be used without medical supervision.
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| References | |
| Additional Infomation |
Carbodenafil (also known as Fondenafil) is a phosphodiesterase type 5 (PDE5) inhibitor that is structurally related to Sildenafil. It has a molecular weight of 452.54 g/mol and molecular formula C24H32N6O3. The compound is found in health foods as a Sildenafil-related compound. It has been studied for its pharmacological profile and structural similarities to clinically approved PDE5 inhibitors, originally developed for the treatment of erectile dysfunction. Carbodenafil is not FDA-approved and is not intended for therapeutic use.
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| Molecular Formula |
C24H32N6O3
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|---|---|
| Molecular Weight |
452.54928
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| Exact Mass |
452.254
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| CAS # |
944241-52-5
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| PubChem CID |
135564767
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| Appearance |
White to off-white solid powder
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| LogP |
2.328
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
33
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| Complexity |
738
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
BNQTXDVBJLRWNB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H32N6O3/c1-5-8-18-20-21(28(4)27-18)23(31)26-22(25-20)17-15-16(9-10-19(17)33-7-3)24(32)30-13-11-29(6-2)12-14-30/h9-10,15H,5-8,11-14H2,1-4H3,(H,25,26,31)
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| Chemical Name |
5-[2-ethoxy-5-(4-ethylpiperazine-1-carbonyl)phenyl]-1-methyl-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-7-one
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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) |
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
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| 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 | 2.2097 mL | 11.0485 mL | 22.0970 mL | |
| 5 mM | 0.4419 mL | 2.2097 mL | 4.4194 mL | |
| 10 mM | 0.2210 mL | 1.1049 mL | 2.2097 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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