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Vardenafil
🥰Excellent
Catalog No. T0096Cas No. 224785-90-4
Alias Vivanza, Levitra
Vardenafil (Vivanza) is an oral therapy for the treatment of erectile dysfunction. It is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). Penile erection is a hemodynamic process initiated by the relaxation of smooth muscle in the corpus cavernosum and its associated arterioles. During sexual stimulation, nitric oxide is released from nerve endings and endothelial cells in the corpus cavernosum. Nitric oxide activates the enzyme guanylate cyclase resulting in increased synthesis of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. The cGMP in turn triggers smooth muscle relaxation, allowing increased blood flow into the penis, resulting in erection. The tissue concentration of cGMP is regulated by both the rates of synthesis and degradation via phosphodiesterases (PDEs). The most abundant PDE in the human corpus cavernosum is the cGMPspecific phosphodiesterase type 5 (PDE5); therefore, the inhibition of PDE5 enhances erectile function by increasing the amount of cGMP.
Vardenafil
🥰Excellent
Purity: 99.88%
Catalog No. T0096Alias Vivanza, LevitraCas No. 224785-90-4
Vardenafil (Vivanza) is an oral therapy for the treatment of erectile dysfunction. It is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). Penile erection is a hemodynamic process initiated by the relaxation of smooth muscle in the corpus cavernosum and its associated arterioles. During sexual stimulation, nitric oxide is released from nerve endings and endothelial cells in the corpus cavernosum. Nitric oxide activates the enzyme guanylate cyclase resulting in increased synthesis of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. The cGMP in turn triggers smooth muscle relaxation, allowing increased blood flow into the penis, resulting in erection. The tissue concentration of cGMP is regulated by both the rates of synthesis and degradation via phosphodiesterases (PDEs). The most abundant PDE in the human corpus cavernosum is the cGMPspecific phosphodiesterase type 5 (PDE5); therefore, the inhibition of PDE5 enhances erectile function by increasing the amount of cGMP.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 25 mg | 29 € | In Stock | |
| 50 mg | 45 € | In Stock | |
| 100 mg | 64 € | In Stock | |
| 500 mg | 153 € | In Stock | |
| 1 g | 226 € | In Stock | |
| 1 mL x 10 mM (in DMSO) | 37 € | In Stock |
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CitedSelect Batch
Purity:99.88%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | Vardenafil (Vivanza) is an oral therapy for the treatment of erectile dysfunction. It is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). Penile erection is a hemodynamic process initiated by the relaxation of smooth muscle in the corpus cavernosum and its associated arterioles. During sexual stimulation, nitric oxide is released from nerve endings and endothelial cells in the corpus cavernosum. Nitric oxide activates the enzyme guanylate cyclase resulting in increased synthesis of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. The cGMP in turn triggers smooth muscle relaxation, allowing increased blood flow into the penis, resulting in erection. The tissue concentration of cGMP is regulated by both the rates of synthesis and degradation via phosphodiesterases (PDEs). The most abundant PDE in the human corpus cavernosum is the cGMPspecific phosphodiesterase type 5 (PDE5); therefore, the inhibition of PDE5 enhances erectile function by increasing the amount of cGMP. |
| Targets&IC50 | PDE5:0.7 nM |
| In vitro | Vardenafil, through the mechanism of mitochondrial K(ATP) channel opening, protects against myocardial ischemia due to reperfusion injury. Oral administration of 3 mg/kg Vardenafil alters object recognition capability in rats. A dose of 30 mg/L orally also upregulates iNOS and proliferating cell nuclear antigen expression (replication of SM cells), leading to the normalization of the rate of dynamic corporal tissue fusion decline and the SM/collagen ratio. Furthermore, Vardenafil induces robust preconditioning-like cardioprotective effects against ischemia/reperfusion injury in rabbits by opening mitochondrial K(ATP) channels. Additionally, it dose-dependently induces an erectile response in rabbits when administered intravenously with Nitroprusside sodium. |
| In vivo | Vardenafil significantly induces relaxation of trabecular smooth muscle elicited by both acetylcholine and electrical stimulation. It competitively inhibits phosphodiesterase type 5 (PDE5), thus enhancing the accumulation and relaxation effect of cyclic guanosine monophosphate (cGMP) in vascular smooth muscle. Its IC50 for specifically inhibiting PDE5-mediated cGMP hydrolysis is 0.7 nM (6.6 nM). At 3 nM (10 nM), Vardenafil notably potentiates the relaxation of human trabecular smooth muscle induced by SNP. At 100 mM, Vardenafil significantly increases cGMP levels in rat hippocampus. |
| Alias | Vivanza, Levitra |
| Molecular Weight | 488.6 |
| Formula | C23H32N6O4S |
| Cas No. | 224785-90-4 |
| Smiles | C(CC)C=1N2C(C(=O)N=C(N2)C3=C(OCC)C=CC(S(=O)(=O)N4CCN(CC)CC4)=C3)=C(C)N1 |
| Relative Density. | 1.212. Temperature:20. |
Storage & Solubility Information
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 45 mg/mL (92.1 mM), Sonication is recommended.  | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
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