Vardenafil NEW
| Price | $31 | $48 | $68 |
| Package | 25mg | 50mg | 100mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-02 |
Product Details
| Product Name: Vardenafil | CAS No.: 224785-90-4 |
| Purity: 99.88% | Supply Ability: 10g |
| Release date: 2024/11/02 |
Product Introduction
Bioactivity
| 名稱 | Vardenafil |
| 描述 | 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. |
| 體外活性 | 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. |
| 體內(nèi)活性 | 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. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 45 mg/mL (92.1 mM) |
| 關(guān)鍵字 | erectile dysfunction | stimulation | Zucker diabetic fatty (ZDF) rats | hepatitis | muscle | inhibit | impotence | Inhibitor | pharmacokinetics | Vardenafil | Endogenous Metabolite | dysfunction | cGMP | selective | Vardenafil Hydrochloride | erectile | smooth | diabetes | Phosphodiesterase (PDE) |
| 相關(guān)產(chǎn)品 | Theophylline monohydrate | Roflumilast | Theobromine | Apremilast | Isoprenaline hydrochloride | Indomethacin | Icariin | Theophylline | Vardenafil hydrochloride | Doxofylline |
| 相關(guān)庫 | FDA上市及藥典收錄分子庫 | 經(jīng)典已知活性庫 | 上市藥物庫 | ReFRAME 相關(guān)化合物庫 | EMA 上市藥物庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | FDA 上市藥物庫 | 已知活性化合物庫 | 人代謝物化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
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