الصفحة الرئيسية>>Signaling Pathways>> Others>> Guanylate Cyclase >>Nelociguat (BAY60-4552)

Nelociguat (BAY60-4552) (Synonyms: BAY 60-4552, Desmethyl Riociguat)

رقم الكتالوجGC32493

Nelociguat (BAY60-4552) (BAY60-4552) هو محفز لانزيم محلقة الجوانيلات القابل للذوبان حساس لأكسيد النيتريك.

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Nelociguat (BAY60-4552) التركيب الكيميائي

Cas No.: 625115-52-8

الحجم السعر المخزون الكميّة
10mM (in 1mL DMSO)
111٫00
متوفر
5mg
101٫00
متوفر
10mg
157٫00
متوفر
50mg
469٫00
متوفر
100mg
653٫00
متوفر
200mg
915٫00
متوفر
500mg
1747٫00
متوفر
1g
2436٫00
متوفر

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مراجعات العميل

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Sample solution is provided at 25 µL, 10mM.

Description Protocol Chemical Properties Product Documents Related Products

Nelociguat (BAY60-4552) is a nitric oxide sensitive soluble guanylate cyclase stimulator.

Soluble guanylate cyclase (sGC) is a key enzyme in the nitric oxide (NO) signalling pathway[1]. Riociguat is metabolized to BAY60-4552 not only via cytochrome P450 isoenzymes 3A4 (CYP3A4), CYP2C8, and CYP2J2, but also via CYP1A1, located in the liver and lungs[2].

GSK2181236A and BAY 60-4552 provide partial benefit against hypertension-induced end-organ damage. In spontaneously hypertensive stroke-prone rats, a low dose of BAY 60-4552 decreases urine output and improved survival. A high dose also reduces urine output, and in addition reduces microalbuminuria and attenuates the increase in mean arterial pressure. Both the 0.3 and 3 mg/kg/day doses of BAY 60-4552 improves survival of 46 and 69%. Seven weeks of treatment with BAY 60-4552 (0.3 and 3.0 mg/kg/day) dose-dependently decreases urine output to 79±11 and 56±10 mL/day[1]. BAY 60-4552, and vardenafil provides synergistic beneficial effects and might therefore salvage patients who experience treatment failures with PDE5 inhibitors after radical prostatectomy[3].

[1]. Costell MH, et al. Comparison of soluble guanylate cyclase stimulators and activators in models of cardiovascular disease associated with oxidative stress. Front Pharmacol. 2012 Jul 5;3:128. [2]. Zhao X, et al. Pharmacokinetics of the Soluble Guanylate Cyclase Stimulator Riociguat in Healthy Young Chinese Male Non-Smokers and Smokers: Results of a Randomized, Double-Blind, Placebo-Controlled Study. Clin Pharmacokinet. 2016 May;55(5):615-24. [3]. Oudot A, et al. Combination of BAY 60-4552 and vardenafil exerts proerectile facilitator effects in rats with cavernous nerve injury: a proof of concept study for the treatment of phosphodiesterase type 5 inhibitor failure. Eur Urol. 2011 Nov;60(5):1020-6.

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