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Tadalafil Sale

(Synonyms: 他达那非; IC-351) 目录号 : GC17074

A PDE5 inhibitor

Tadalafil Chemical Structure

Cas No.:171596-29-5

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥368.00
现货
50mg
¥588.00
现货
100mg
¥893.00
现货
500mg
¥3,392.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

实验参考方法

Cell experiment [1]:

Cell lines

human hepatocytes

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

Applications

Tadalafil (1 μM) increased CYP3A protein expression in human hepatocytes.

Animal experiment [2,3]:

Animal models

Rat model with bilateral cavernous neurotomy (BCN)-induced penile damage and hypo-oxygenation, Mice with cavernous nerve resection

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.

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.

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.

产品描述

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

Chemical Properties

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。
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。

溶解性数据

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
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