Nortadalafil Struktur

Nortadalafil

Bezeichnung:Nortadalafil

CAS-Nr171596-36-4

Englisch Name:Nortadalafil

CBNumberCB92549609

SummenformelC21H17N3O4

Molgewicht375.38

MOL-Datei171596-36-4.mol

Nortadalafil physikalisch-chemischer Eigenschaften

Schmelzpunkt	285-290℃ (methanol )
Siedepunkt	718.6±60.0 °C(Predicted)
Dichte	1.55±0.1 g/cm3(Predicted)
storage temp.	Inert atmosphere,Room Temperature
Löslichkeit	DMSO (Slightly), Methanol (Slightly, Sonicated)
Aggregatzustand	Solid
pka	13.53±0.40(Predicted)
Farbe	White to Pale Yellow

Gefahreninformationscode (GHS)

Nortadalafil Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
A N-desmethyl analogue of the human PDE5 inhibitor Tadalafil (T004500). A potential antiplasmodial drug.
Biologische Aktivität
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].
target
PDE5
IC 50
n/a for nortadalafil; 5 nm for tadalafil
Einzelnachweise
[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.

Nortadalafil Upstream-Materialien And Downstream Produkte

Nortadalafil Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

171596-36-4, Nortadalafil Verwandte Suche:

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