Sildenafil Citrate
(Synonyms: 西地那非柠檬酸盐; UK-92480 citrate) 目录号 : GC17685
A PDE5 inhibitor
Cas No.:171599-83-0
Sample solution is provided at 25 µL, 10mM.
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Sildenafil Citrate is a potent inhibitor of cGMP-specific phosphodiesterase including PDE5 with IC50 values of 3.6 nM.[1]
PDE5 (cGMP-specific phosphodiesterase type 5) is an enzyme from the phosphodiesterase class. The function of PDE5 is to accept cGMP and breaks it down. cGMP (cyclic guanosine monophosphate) is one of second messenger which is the production of guanylate cyclase. cGMP is a regulator of cellular apoptosis glycogenolysis, conductance , and ion channel. It can relaxe smooth muscle tissues. In blood vessels, It also can relaxe vascular smooth muscles, then lead to increased blood flow and vasodilation. The inhibitors of PDE5 can inhibit the degradation of cGMP, then leads to increase bloodflow to the penis. Sildenafil Citrate is used treatment of erectile dysfunction.
Sildenafil is a potent cGMP-specific phosphodiesterase. It is highly selective for PDE5. It inhibits the activity of PDE5 with an IC50 value of 3 nM in human corpus cavernosum (3.6nM in isolated rabbit platelets). At the same condition, It inhibits the activity of PDE1 and PDE3 activities with IC50s = 0.26 and 65 μM, respectively.[1] Sildenafil potently relaxed anococcygeus muscle strip swith maximum response of 100 ± 2% and a pEC50 value of 6.44 ± 0.03 in rat. Sildenafil also increased by approximately 55% the duration of nitrergic relaxations.[1, 2] Compared to the base salt, the citrate salt has pharmacokinetics and superior water solubility.[3]
References:
[1]. Teixeira CE, Priviero FB, Claudino MA, Baracat JS, De Nucci G, Webb RC, Antunes E: Stimulation of soluble guanylyl cyclase by BAY 41-2272 relaxes anococcygeus muscle: interaction with nitric oxide. Eur J Pharmacol 2006, 530(1-2):157-165.
[2]. Richalet JP, Gratadour P, Robach P, Pham I, Dechaux M, Joncquiert-Latarjet A, Mollard P, Brugniaux J, Cornolo J: Sildenafil inhibits altitude-induced hypoxemia and pulmonary hypertension. Am J Respir Crit Care Med 2005, 171(3):275-281.
[3]. Jung SY, Seo YG, Kim GK, Woo JS, Yong CS, Choi HG: Comparison of the solubility and pharmacokinetics of sildenafil salts. Arch Pharm Res 2011, 34(3):451-454.
| Cell experiment [1]: | |
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Cell lines |
PASMCs |
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Preparation method |
The solubility of this compound in DMSO is > 25.4 mg/mL. 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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Reacting condition |
1 μM |
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Applications |
In PASMCs, pretreatment with 1 μM Sildenafil Citrate increased the phosphorylation of ERK1/ERK2, the percentage of cells in S phase, as well as cell proliferation, compared with serotonin stimulation alone. Furthermore, pretreatment with 10 μM U0126 for 30 mins prevented Sildenafil Citrate-induced increases in the phosphorylation of ERK1/ERK2, and abolished Sildenafil Citrate-induced cell cycle progression and PASMC proliferation. |
| Animal experiment [2]: | |
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Animal models |
Hypercholesterolemic MetS rabbits |
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Dosage form |
5 mg/kg/day; p.o. |
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Applications |
In hypercholesterolemic MetS rabbits, Sildenafil Citrate inhibited the development of endothelial dysfunction and Erectile dysfunction (ED). Moreover, Sildenafil Citrate significantly improved relaxation responses of cavernosal tissues. In addition, compared with the control group, Sildenafil Citrate maintained the in vitro erectile responses of the corporal tissue strips in MetS rabbits. |
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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]. Li BB, Jiang Z, Sheng JY, Yao K. Sildenafil potentiates the proliferative effect of porcine pulmonary artery smooth muscle cells induced by serotonin in vitro. Chin Med J (Engl). 2011 Sep;124(17):2733-40. [2]. Erden Y, Korgal E, Dundar G, Ayan S, Gokce G, Yildirim S, Gultekin EY. In-vitro effects of PDE5 inhibitor and statin treatment on the contractile responses of experimental MetS rabbit's cavernous smooth muscle Arch Ital Urol Androl. 2014 Mar 28;86(1):33-8. | |
| Cas No. | 171599-83-0 | SDF | |
| 别名 | 西地那非柠檬酸盐; UK-92480 citrate | ||
| 化学名 | 5-[2-ethoxy-5-(4-methylpiperazin-1-yl)sulfonylphenyl]-1-methyl-3-propyl-4H-pyrazolo[4,3-d]pyrimidin-7-one;2-hydroxypropane-1,2,3-tricarboxylic acid | ||
| Canonical SMILES | CCCC1=NN(C2=C1NC(=NC2=O)C3=C(C=CC(=C3)S(=O)(=O)N4CCN(CC4)C)OCC)C.C(C(=O)O)C(CC(=O)O)(C(=O)O)O | ||
| 分子式 | C22H30N6O4S.C6H8O7 | 分子量 | 666.7 |
| 溶解度 | ≥ 25.35 mg/mL in DMSO, ≥ 2.97 mg/mL in Water with ultrasonic and warming | 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 | 1.4999 mL | 7.4996 mL | 14.9993 mL |
| 5 mM | 0.3 mL | 1.4999 mL | 2.9999 mL |
| 10 mM | 0.15 mL | 0.75 mL | 1.4999 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet