Tadalafil
(Synonyms: 他达那非; IC-351) 目录号 : GC17074
A PDE5 inhibitor
Cas No.:171596-29-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
human hepatocytes |
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Preparation method |
The solubility of this compound in DMSO is >16.6mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
1 μM |
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Applications |
Tadalafil (1 μM) increased CYP3A protein expression in human hepatocytes. |
| Animal experiment [2,3]: | |
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Animal models |
Rat model with bilateral cavernous neurotomy (BCN)-induced penile damage and hypo-oxygenation, Mice with cavernous nerve resection |
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Dosage form |
2 mg/kg, daily for 3 months |
|
Application |
Tadalafil (2 mg/kg) almost completely restored penile oxygenation and abolished neurotomy induced increase and substantially rescued muscle/fiber ratio in penile sectionsin sham-operated rats. Tadalafil decreased the number of apoptotic cells and increased the phosphorylation of the 2 survival associated kinases Akt and extracellular signal-regulated kinase 1/2 in mice. |
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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]. Ring B J, Patterson B E, Mitchell M I, et al. Effect of tadalafil on cytochrome P450 3A4–mediated clearance: studies in vitro and in vivo[J]. Clinical Pharmacology & Therapeutics, 2005, 77(1): 63-75. [2]. Morelli A, Vignozzi V, Filippi S, et al. Effect of Chronic Tadalafil Administration on Penile Hypoxia Induced by Cavernous Neurotomy in the Rat[J]. The Journal of Sexual Medicine, 2006, 3: 46. [3]. Lysiak J J, Yang S K, Klausner A P, et al. Tadalafil increases Akt and extracellular signal-regulated kinase 1/2 activation, and prevents apoptotic cell death in the penis following denervation[J]. The Journal of urology, 2008, 179(2): 779-785. |
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Tadalafil, also known as IC351 or Cialis, is a potent, reversible and competitive small-molecule inhibitor of phosphodiesterase 5 (PDE5), a predomiant PDE in the pulmonary vasculature that hydrolyzes cyclic guanosine monophosphate (cGMP) and is involved in the pathobiology of pulmonary arterial hypertension (PAH). The inhibitory effect of tadalafil is PDE5 specific with the selectivity of 10000 times greater than that of PDE1, PDE4, PDE7, PDE8, PDE9 and PDE10 and of 780 times greater than that of PDE6. Although it is used for the treatment of erectile dysfunction through oral administration, tadalafil also improves the vasoconstrictive-predominate condition of PAH through elevating cGMP levels in pulmonary vessels resulted from PDE5 inhibition.
Reference
[1].Fusae Sawamura, Masami Kato, Kazushisa Fujita, Takahiro Nakazawa and Anthony Bearsworth. Tadalafil, a long-acting inhibitor of PDE5, improves pulmonary hemodynamics and survival rate of monocrotaline-induced pulmonary artery hypertension in rats. J Pharmacol Sci 111, 235-243 (2009)
[2].H Porst. IC351 (tadalafil, Cialis): update on clinical experience. Internation Journal of Impotence Research (2002) 14, Suppl 1, S57-S64
[3].S. Thomas Forgue, Beverley E. Patterson, Alun W. Bedding, Christopher D. Payne, Diane L. Phillips, Rebecca E. Wrishko and Malcolm I. Mitchell. Tadalafil pharmacokinetics in healthy subjects. Br J Clin Pharmacol (2005); 61(3): 280-288
| Cas No. | 171596-29-5 | SDF | |
| 别名 | 他达那非; IC-351 | ||
| 化学名 | (6R,12aR)-6-(benzo[d][1,3]dioxol-5-yl)-2-methyl-2,3,12,12a-tetrahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4(6H,7H)-dione | ||
| Canonical SMILES | O=C1N(C)CC(N([C@@H]2C(C=C3)=CC4=C3OCO4)[C@]1([H])CC5=C2NC6=CC=CC=C56)=O | ||
| 分子式 | C22H19N3O4 | 分子量 | 389.4 |
| 溶解度 | ≥ 16.6 mg/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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5681 mL | 12.8403 mL | 25.6805 mL |
| 5 mM | 0.5136 mL | 2.5681 mL | 5.1361 mL |
| 10 mM | 0.2568 mL | 1.284 mL | 2.5681 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。