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Tadalafil

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Chemical Structure| 171596-29-5 同义名 : 他达那非;西力士 ;IC-351
CAS号 : 171596-29-5
货号 : A147960
分子式 : C22H19N3O4
纯度 : 98%
分子量 : 389.404
MDL号 : MFCD07771966
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(128.4 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+30% PEG300+water 3.2 mg/mL clear

PO 0.5% CMC-Na 50 mg/mL suspension

生物活性
靶点

  • PDE5

    PDE5, IC50:1.8 nM
描述 Phosphodiesterase-5 (PDE5) is a homodimer that belongs to mammalian PDE family. The catalytic domain of PDE5 catalyzes the breakdown of cGMP to 5’-GMP. Tadalafil is a PDE5 inhibitor with an IC50 value of 1.8  0.4nM. The stoichiometry of [3H]Tadalafil binding to PDE5 was 0.68  0.10 mol/subunit. The KD (isotherm), KD (dissociation rate), and KD (1/2 EC50) values of tadalafil against PDE5 were 2.4  0.60, 1.9  0.37, and 2.7  0.25nM, respectively[5]. Tadalafil also inhibits human cytochrome P450 (CYPs) with Ki values of 41  5, 66  6, 73  8, and 14  1μM against CYP3A-, CYP2C9-, CYP2C19-, and CYP1A2-mediated metabolism, respectively. Tadalafil at the dose of 1μM or greater induced the protein level of CYP3A in hepatocytes. The CYP3A activity was increased by 1μM tadalafil, but this induction was suppressed after the exposure to 10μM tadalafil. Also in hepatocyte cultures, the exposure to 0.1 – 1μM tadalafil slightly inhibited CYP3A-mediated midazolam 1’-hydroxylase activity. With the treatment of 10μM tadalafil, 1’-OH-midazolam formation was significantly inhibited in a time-dependent manner[6]. In mice subjected to cavernous nerve resection, treatment with tadalafil (1.3 gm per day) via oral gavage for 20 days decreased the number of apoptotic cells and increased the phosphorylation of the 2 survival associated kinases, Akt and extracellular signal-regulated kinase 1/2[7].
作用机制 Tadalafil inhibits PDE5 by specifically binding to the catalytic site of PDE5[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.57mL

0.51mL

0.26mL

12.84mL

2.57mL

1.28mL

25.68mL

5.14mL

2.57mL
参考文献

[1]CIALIS

[2]Washington SL 3rd, Shindel AW, et al. A once-daily dose of tadalafil for erectile dysfunction: compliance and efficacy. Drug Des Devel Ther. 2010 Sep 7;4:159-71.

[3]66(1):144-52.

[4]77(1):63-75.

[5]Blount MA, Beasley A, Zoraghi R, Sekhar KR, Bessay EP, Francis SH, Corbin JD. Binding of tritiated sildenafil, tadalafil, or vardenafil to the phosphodiesterase-5 catalytic site displays potency, specificity, heterogeneity, and cGMP stimulation. Mol Pharmacol. 2004 Jul;66(1):144-52.