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Nortadalafil
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Nortadalafil图片
CAS NO:171596-36-4
包装与价格：
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
诺他达拉非是去甲基他达拉非，它是一种 PDE5 抑制剂，目前以药丸形式销售，用于治疗勃起功能障碍 (ED)，名称为 Cialis；并以 Adcirca 的名义用于治疗肺动脉高压。
Cas No.171596-36-4
别名去甲基他达那非; Demethyl Tadalafil
化学名(6R,12aR)-6-(benzo[d][1,3]dioxol-5-yl)-2,3,12,12a-tetrahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4(6H,7H)-dione
Canonical SMILESO=C1N([H])C([H])([H])C(N2[C@@](C(C([H])=C3[H])=C([H])C4=C3OC([H])([H])O4)([H])C(N([H])C5=C([H])C([H])=C([H])C([H])=C65)=C6C([H])([H])[C@@]21[H])=O
分子式C21H17N3O4
分子量375.38
溶解度Soluble in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: N/A for Nortadalafil; 5 nM for Tadalafil

The cGMP-specific PDE5 is the major PDE isozyme in the corpus cavernosum, and controls penile erection. The PDE5 inhibitors used in the clinic amplify the NO-cCMP pathway and enhance the normal process leading to penile erection.

Nortadalafil is demethyl Tadalafil, which is a PDE5 inhibitor currently marketed in pill form for treating erectile dysfunction under the name Cialis and for the treatment of pulmonary arterial hypertension under the name Adcirca.

In vitro: Tadalafil has been identified as a highly potent PDE5 inhibitor (IC50 = 5 nM) with high selectivity for PDE5 vs PDE1-4 and PDE6. It displays 85-fold greater selectivity vs PDE6 than sildenafil [1].

In vivo: Tadalafil showed profound and long-lasting blood pressure lowering activity (30 mmHg/>7 h) in the spontaneously hypertensive rat model after oral administration (5 mg/kg) [1].

Clinical trial: Tadalafil once-daily provides efficacy comparable to on-demand dosing regimens with PDE-5 inhibitors, is well tolerated and allows patients and their partners to disconnect the administration of medication from sexual activity, thereby enabling them to return to the sex-life they had before the onset of erectile dysfunction [2].

References:
[1] Daugan A, Grondin P, Ruault C, Le Monnier de Gouville AC, Coste H, Linget JM, Kirilovsky J, Hyafil F, Labaudinière R.  The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues. J Med Chem. 2003;46(21):4533-42.
[2] Porst H, Hell-Momeni K, Büttner H.   Chronic PDE-5 inhibition in patients with erectile dysfunction - a treatment approach using tadalafil once-daily. Expert Opin Pharmacother. 2012 Jul;13(10):1481-94. doi: 10.1517/14656566.2012.693162.