Name: Nortadalafil
Price: 326.00 USD

- Overview
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    Background
    
    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].
    
    [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.
- Properties
  - Alternative Name
    
    Demethyl Tadalafil; (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
    
    CAS Number
    
    171596-36-4
    
    Molecular Formula
    
    C21H17N3O4
    
    Molecular Weight
    
    375.38
    
    Purity
    
    98.00%
    
    Solubility
    
    Soluble in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Nortadalafil

Nortadalafil

Background

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