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Nortadalafil

Catalog No.
A3665
PDE5 inhibitor
Grouped product items
SizePriceStock Qty
2mg
$149.00
Ship with 10-15 days
5mg
$203.00
Ship with 10-15 days
10mg
$315.00
Ship with 10-15 days
50mg
$945.00
Ship with 10-15 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

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].

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.

Chemical Properties

StorageStore at -20°C
M.Wt375.38
Cas No.171596-36-4
FormulaC21H17N3O4
SynonymsDemethyl Tadalafil
SolubilitySoluble in DMSO
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
SDFDownload SDF
Canonical SMILESO=C1N([H])C([H])([H])C(N2[[email protected]@](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])[[email protected]@]21[H])=O
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Biological Activity

Description Nortadalafil is a inhibitor of PDE5.
Targets PDE5          
IC50            

Quality Control

Quality Control & MSDS

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Chemical structure

Nortadalafil