Vardenafil hydrochloride
(Synonyms: 盐酸伐地那非) 目录号 : GC37888
An inhibitor of PDE5 and PDE6
Cas No.:224785-91-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Vardenafil is a potent inhibitor of phosphodiesterase 5 (PDE5; IC50s = 0.2-1.2 nM) and PDE6 (IC50 = 2 nM).1,2,3 It is selective for PDE5 and PDE6 over PDE1 and PDE11 (IC50s = 230 and 130 nM, respectively). Vardenafil (4 mg/kg per day for three weeks) improves erectile function in a rat model of acute arteriogenic erectile dysfunction by increasing intracavernous pressure and mean arterial pressure, and this effect persists for at least two weeks following the end of treatment.4 Chronic vardenafil administration at a dose of 2 mg/kg for five weeks in subordinate mice reduces the latency to mount and increases the frequency of mounting behavior.5 Formulations containing vardenafil have been used in the treatment of erectile dysfunction.
1.Card, G.L., England, B.P., Suzuki, Y., et al.Structural basis for the activity of drugs that inhibit phosphodiesterasesStructure12(12)2233-2247(2004) 2.Boyle, C.D., Xu, R., Asberom, T., et al.Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male EDBioorg. Med. Chem. Lett.15(9)2365-2369(2005) 3.Smith, W.B., II, McCaslin, I.R., Gokce, A., et al.PDE5 inhibitors: Considerations for preference and long-term adherenceInt. J. Clin. Pract.67(8)768-780(2013) 4.Hotta, Y., Ohno, R., Kataoka, T., et al.Effects of chronic vardenafil treatment persist after end of treatment in rats with acute arteriogenic erectile dysfunctionJ. Sex Med.9(7)1782-1788(2012) 5.Dadomo, H., Parmigiani, S., Nicolini, Y., et al.Repeated and chronic administration of Vardenafil or Sildenafil differentially affects emotional and socio-sexual behavior in miceBehav. Brain Res.253103-112(2013)
| Cas No. | 224785-91-5 | SDF | |
| 别名 | 盐酸伐地那非 | ||
| Canonical SMILES | CCCC1=NC(C)=C2N1N=C(C(C=C(S(=O)(N3CCN(CC)CC3)=O)C=C4)=C4OCC)NC2=O.Cl | ||
| 分子式 | C23H33ClN6O4S | 分子量 | 525.06 |
| 溶解度 | DMSO: 100 mg/mL (190.45 mM); Water: ≥ 100 mg/mL (190.45 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9045 mL | 9.5227 mL | 19.0454 mL |
| 5 mM | 0.3809 mL | 1.9045 mL | 3.8091 mL |
| 10 mM | 0.1905 mL | 0.9523 mL | 1.9045 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Vardenafil
Expert Opin Investig Drugs 2002 Oct;11(10):1487-96.PMID:12387708DOI:10.1517/13543784.11.10.1487.
Vardenafil hydrochloride is a potent and highly selective inhibitor of phosphodiesterase Type 5 that increases blood flow to the penis during sexual stimulation and helps restore the ability to achieve and sustain an erection in men with erectile dysfunction. Vardenafil was developed specifically to be an effective and safe oral medication for the treatment of erectile dysfunction, with potential advances over existing therapies. This review summarises key findings during the rapid and aggressive development of this compound, from in vitro assays to Phase III trials with both broad and special populations. Emphasis is placed on the presentation of data that demonstrates the clinical effectiveness and safety of this agent which is anticipated to be available in 2003.
Utilization of a micellar matrix for simultaneous spectrofluorimetric estimation of alfuzosin hydrochloride and Vardenafil hydrochloride
Spectrochim Acta A Mol Biomol Spectrosc 2022 Feb 5;266:120420.PMID:34619505DOI:10.1016/j.saa.2021.120420.
A sensitive and direct spectrofluorimetric method was developed for simultaneous quantitation of two co-administered drugs, namely, alfuzosin hydrochloride (AFH) and Vardenafil hydrochloride (VRH). Both drugs exhibited native fluorescence properties that could be exploited to assay them in biological fluids with high sensitivity. Spectrofluorimetric analysis of AFH and VRH is based on excitation of both drugs at 265 nm where emission spectra were recorded separately for AFH and VRH at 380 and 485 nm, respectively. Micellar trends in analytical chemistry were adopted to minimize both environmental and occupational hazards, using distilled water and sodium dodecyl sulphate (serves as a micellar medium that enhanced the sensitivity of AFH and VRH) for analysis of both drugs in their raw materials, tablets, and human biological fluids (plasma and urine). Linearity ranges were 1.0-16.0 and 10.0-700.0 ng mL-1 for AFH and VRH, respectively. The proposed method was successfully assessed for analysis of AFH and VRH in spiked human plasma and urine samples over the following concentrations: 1.0-12.0 ng mL-1 and 4.0-400.0 ng mL-1 for both drugs, simultaneously with mean recoveries of 101.08 % and 102.06 % in plasma and 96.75 % and 92.8 % in urine. Statistical analysis of the practical results has proved quite good agreement and revealed there were no significant differences in the accuracy and precision with those obtained by the comparison methods. The proposed method was applied successfully to Prostetrol® and Powerecta® commercial tablets without interference with tablet additives.
Borneol-mediated Vardenafil hydrochloride patch for pediatric pulmonary arterial hypertension: Preparation, characterization and in vivo study
Int J Pharm 2020 Dec 15;591:119864.PMID:32991961DOI:10.1016/j.ijpharm.2020.119864.
Background: Pediatric pulmonary arterial hypertension (PPAH) is a malignant progressive rare disease characterized by restricted pulmonary artery blood flow and progressively increasing blood pressure, which has shorter survival time of only about 10 months as compared to adults. Previous studies have shown that low-dose Vardenafil hydrochloride (Var) could significantly improve the symptoms of PPAH. However, Var is currently available only in tablet form in the market for erectile dysfunction, and no special preparation is available for PPAH. Methods: In this study, borneol-mediated Vardenafil hydrochloride patch (BO-VarP) with sodium polyacrylate as the skeleton material was prepared by coating method, which was characterized by temperature resistance, formability, adhesive force, skin irritation and in vitro permeation. Blood concentration of optimized BO-VarP was measured by LC-MS/MS using intragastric administration (i.g.) as a control, and pharmacodynamic studies were conducted using a rat model of pulmonary arterial hypertension induced by monocrotaline. Results and discussion: Optimized BO-VarP showed good appearance, with optimal temperature resistance and formability, appropriate adhesive force and low skin irritation, and its cumulative permeation flux was 14.9 times higher than patch without penetration enhancer. The blood concentration within therapeutic window of BO-VarP lasted longer than i.g., and BO-VarP could improve symptoms of PPAH by reducing pulmonary arterial pressure and right heart hypertrophy index. Conclusion: BO-VarP had good therapeutic effect in PPAH rats and suitable compliance in children, which provided a potential industrial transdermal delivery system for the treatment of PPAH.
Dual-purpose Vardenafil hydrochloride/dapoxetine hydrochloride orodispersible tablets: in vitro formulation/evaluation, stability study and in vivo comparative pharmacokinetic study in healthy human subjects
Drug Dev Ind Pharm 2018 Jun;44(6):988-1000.PMID:29325456DOI:10.1080/03639045.2018.1427761.
Erectile dysfunction (ED) is the most important disorder after premature ejaculation for sexual activity in men. Vardenafil hydrochloride (VH) is an oral therapy for the treatment of erectile dysfunction. VH oral disintegrating tablets (ODTs) have been prepared by freeze drying technique to improve its dissolution profile and the overall clinical performance. Dapoxetine hydrochloride (DH) was added to the best three formulae of the prepared VH ODTs to treat premature ejaculation. All the ODTs formulae were evaluated for weight variation, friability, drug content, in vitro disintegration time, wetting time, and the dissolution study. Gelatin as a matrix former with N-methylpyrrolidone as a solubilizer in VH/DH ODTs improved the dissolution rate and extent of release of VH and DH with 100% of drug being dissolved after 15 min. In vivo study results from six healthy male volunteers showed shorter Tmax of VH from VH/DH ODT of 0.583 ± 0.129 h and shorter Tmax of DH from VH/DH ODT of 0.625 ± 0.137 h and showed AUC0-12 of VH from VH/DH ODT of 39.234 ± 10.932 ng/mlh1 and AUC0-12 of DH from VH/DH ODT of 531.681 ± 129.544 ng/mlh1, with relative bioavailability values of 100.9 and 85%, respectively, compared to (Levitra®) and (Priligy®).
Prednisone and Vardenafil hydrochloride for refractory levamisole-induced vasculitis
Cutis 2016 Aug;98(2):E15-9.PMID:27622263doi
Levamisole is an immunomodulatory drug that was previously used to treat various medical conditions, including parasitic infections, nephrotic syndrome, and colorectal cancer. Over the last few years, increasing amounts of levamisole have been used as an adulterant in cocaine. Levamisole-cut cocaine has become a concern because it is known to cause a necrotizing purpuric rash, autoantibody production, and life-threatening leukopenia. Mixed histologic findings of vasculitis and thrombosis are characteristic of levamisole-induced purpura. The recommended management of levamisole-induced vasculitis currently involves withdrawal of the culprit along with supportive treatment. We describe a patient with levamisole-induced vasculitis who continued to develop skin lesions despite self-reported cocaine cessation. Complete resolution of cutaneous disease occurred with the addition of oral prednisone and Vardenafil hydrochloride, suggesting the possibility of a new treatment option in patients with refractory disease. In addition, we review the clinical presentation, disease course, diagnostic approach, laboratory findings, histology, and management of levamisole-induced vasculitis. The harmful effects of levamisole-cut cocaine are serious enough that public alerts have been issued to increase awareness. Clinicians should consider the possibility of levamisole exposure in cocaine users presenting with any combination of fever, neutropenia, and necrotic skin lesions, especially in acral areas including the ears.