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Sample solution is provided at 25 µL, 10mM.
Publications citing ApexBio Products.
2017 Jan 19;541(7637):417-420.
2018 Mar 29;555(7698):673-677.
2016 Apr 21;532(7599):398-401.
2016 Aug 5;353(6299)594-8.
2018 Feb 22;172(5):1007-1021.e17.
2017 Nov 30;171(6):1284-1300.e21.
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2017 Nov 20. pii: S1934-5909(17)30375-2.
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2016 Jan 19;44(1):88-102.
2017 Dec 13;9(420). pii: eaal3765.
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Cell Host Microbe.
2017 Oct 11;22(4):561-573.e4.
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2017 Oct 5;68(1):210-223.e6.
Quality Control.
Quality Control & MSDS.
Purity = 98.00% COA (Certificate Of Analysis) MSDS (Material Safety Data Sheet) Datasheet.
Chemical structure.
Biological Activity.
Nortadalafil Dilution Calculator.
Nortadalafil Molarity Calculator.
Chemical Properties.
All other available size: ship with RT , or blue ice upon request.
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.