Sildenafil mesylate
(Synonyms: 甲磺酸西地那非) 目录号 : GC15037
A PDE5 inhibitor
Cas No.:1308285-21-3
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
IC50: 3.5 nM
Sildenafil mesylate is an inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5).
PDE5 is the predominant phosphodiesterase in the corpus cavernosum. The catalytic site of PDE5 degrades cGMP, and PDE5 inhibitors can potentiate endogenous increases in cGMP.
In vitro: Sildenafil mesylate had been identified as a potent PDE5 reversible and selective inhibitor. Sildenafil enhanced sodium nitroprusside- or transmural electrical stimulation-induced relaxation of precontracted corpus cavernosum muscle strips in organ baths. Sildenafil also increased intracellular cGMP concentrations in cultured smooth muscle cells treated with sodium nitroprusside [1].
In vivo: In anesthetized dogs, sildenafil could enhance the erectile function following pelvic nerve stimulation as measured by increased intracavernosal pressure [1].
Clinical trial: Ten previous randomised controlled trials had been conducted. Dose optimisation resulted in >60% of attempts at sexual intercourse, which was successful in 49% of men. Sildenafil treatment related adverse events occurred in 30% of men compared with 11% on placebo. Dose optimisation of sildenafil showed efficacy equivalent to the highest fixed doses, and adverse events equivalent to the lowest fixed doses [2].
References:
[1] Nehra A,Colreavy F,Khandheria BK,Chandrasekaran K. Sildenafil citrate, a selective phosphodiesterase type 5 inhibitor: urologic and cardiovascular implications. World J Urol.2001 Feb;19(1):40-5.
[2] Moore RA,Edwards JE,McQuay HJ. Sildenafil (Viagra) for male erectile dysfunction: a meta-analysis of clinical trial reports. BMC Urol.2002 May 22;2:6.
| Cas No. | 1308285-21-3 | SDF | |
| 别名 | 甲磺酸西地那非 | ||
| 化学名 | 5-(2-ethoxy-5-((4-methylpiperazin-1-yl)sulfonyl)phenyl)-1-methyl-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one methanesulfonate | ||
| Canonical SMILES | CCCC(C(N=C(N1)C2=C(OCC)C=CC(S(N3CCN(CC3)C)(=O)=O)=C2)=C4C1=O)=NN4C.CS(O)(=O)=O | ||
| 分子式 | C23H34N6O7S2 | 分子量 | 570.68 |
| 溶解度 | ≥ 57.1mg/mL in DMSO | 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 | 1.7523 mL | 8.7615 mL | 17.523 mL |
| 5 mM | 0.3505 mL | 1.7523 mL | 3.5046 mL |
| 10 mM | 0.1752 mL | 0.8761 mL | 1.7523 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。