Description
Nortadalafil is a inhibitor of PDE5.
Product Overview
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. 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.
Synonyms
Demethyl Tadalafil
IC50
N/A for Nortadalafil; 5 nM for Tadalafil
Molecular Formula
C21H17N3O4
Chemical Name
(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
Solubility
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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.
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).
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