Vardenafil HCl Trihydrate
(Synonyms: 盐酸瓦地那非三水合物) 目录号 : GC10588
An inhibitor of PDE5 and PDE6
Cas No.:330808-88-3
Sample solution is provided at 25 µL, 10mM.
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Vardenafil is a potent and selective inhibitor of phosphodiesterase type5 (PDE5) with the IC50 value of 0.7 nM in enzymatic assay in vitro [1]. Vardenafil HCl Trihydrate is a salt form of vardenafil. [1]
Vardenafil has shown a greater selective inhibition towards PDE5 than PDEs from bovine, with the IC50 values of 180nM,>10000nM, 2500nM, 4000nM and 11nM for PDE1, PDE2, PDE3, PDE4 and PDE6, respectively. Besides, Vardenafil has been reported to significantly enhance the SNP-induced, ACh-induced and transmural electrical stimulation-induced relaxation of human trabecular smooth muscle. Vardenafil has been revealed to increase the amount of cGMP in human corpus cavernosum. Apart from these, Vardenafil has also enhanced the length of penile in the conscious rabbit [1].
Reference:
[1] Saenz de Tejada I1, Angulo J, Cuevas P, Fernández A, Moncada I, Allona A, Lledó E, Körschen HG, Niewöhner U, Haning H, Pages E, Bischoff E.The phosphodiesterase inhibitory selectivity and the in vitro and in vivo potency of the new PDE5 inhibitor vardenafil. Int J Impot Res. 2001 Oct;13(5):282-90.
| Kinase experiment [1]: | |
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Enzyme inhibition assays |
PDE5 and 3H-cGMP were added in DMSO (final concentration of DMSO 0.1%). Incubation period was 15 min at 30 ℃. All tests were done in duplicate and were repeated at least three times. The IC50 value for the PDE5 inhibition were determined from sigmoidal curves, fitted to plots of enzyme activity vs log compound concentration using a GraphPad curve fitting program. |
| Cell experiment [1]: | |
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Cell lines |
Human trabecular smooth muscle cells |
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Preparation method |
This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 °C for several months. |
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Reaction Conditions |
3, 10 or 30 nM |
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Applications |
In human trabecular smooth muscle strips, Vardenafil HCl Trihydrate significantly enhanced SNP-induced relaxation. |
| Animal experiment [1]: | |
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Animal models |
A conscious rabbit model |
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Dosage form |
0.1, 0.3, 1 or 3 mg/kg; p.o. |
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Applications |
In a conscious rabbit model, Vardenafil HCl Trihydrate dose-dependently potentiated erectile responses induced by SNP. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Saenz de Tejada I1, Angulo J, Cuevas P, Fernández A, Moncada I, Allona A, Lledó E, K?rschen HG, Niew?hner U, Haning H, Pages E, Bischoff E.The phosphodiesterase inhibitory selectivity and the in vitro and in vivo potency of the new PDE5 inhibitor vardenafil. Int J Impot Res. 2001 Oct;13(5):282-90. | |
| Cas No. | 330808-88-3 | SDF | |
| 别名 | 盐酸瓦地那非三水合物 | ||
| 化学名 | 2-[2-ethoxy-5-(4-ethylpiperazin-1-yl)sulfonylphenyl]-5-methyl-7-propyl-1H-imidazo[5,1-f][1,2,4]triazin-4-one | ||
| Canonical SMILES | CCCC1=NC(=C2N1NC(=NC2=O)C3=C(C=CC(=C3)S(=O)(=O)N4CCN(CC4)CC)OCC)C | ||
| 分子式 | C23H32N6O4S.HCl.3H2O | 分子量 | 579.11 |
| 溶解度 | ≥ 13.3 mg/mL in DMSO, ≥ 3.42 mg/mL in EtOH with ultrasonic and warming, ≥ 95 mg/mL in Water | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.7268 mL | 8.6339 mL | 17.2679 mL |
| 5 mM | 0.3454 mL | 1.7268 mL | 3.4536 mL |
| 10 mM | 0.1727 mL | 0.8634 mL | 1.7268 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet