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Tadalafil

现货
Catalog No.
A4327
PDE5抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 500.00
现货
50mg
¥ 770.00
现货
100mg
¥ 1,190.00
现货
500mg
¥ 4,690.00
现货

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Background

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

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)

H Porst. IC351 (tadalafil, Cialis): update on clinical experience. Internation Journal of Impotence Research (2002) 14, Suppl 1, S57-S64

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

StorageStore at -20°C
M.Wt389.4
Cas No.171596-29-5
FormulaC22H19N3O4
SynonymsCialis,ICOS 351,Ic351,IC 351,IC-351
Solubility≥16.6 mg/mL in DMSO, <2.81 mg/mL in EtOH, <2.09 mg/mL in H2O
Chemical Name(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
SDFDownload SDF
Canonical SMILESO=C1N(C)CC(N([C@@H]2C(C=C3)=CC4=C3OCO4)[C@]1([H])CC5=C2NC6=CC=CC=C56)=O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

人肝细胞

溶解方法

该化合物在DMSO中的溶解度大于16.6mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

1 μM

应用

Tadalafil (1 μM)提高了人肝细胞中CYP3A蛋白的表达。

动物实验 [2,3]:

动物模型

双侧海绵状神经切断术(BCN)诱导阴茎损伤和低氧合的大鼠模型,海绵体神经切除小鼠

给药剂量

2 mg/kg,每天给药,持续三周

应用

在假手术大鼠的阴茎切片中,Tadalafil (2 mg/kg)几乎完全恢复了阴茎氧合,并且消除了神经切断术诱发的增加,显著挽救了肌肉/纤维的比例。Tadalafil减少凋亡细胞的数量,并增加小鼠中2种存活相关激酶Akt和细胞外信号调节激酶1/2的磷酸化。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

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.

质量控制

化学结构

Tadalafil