Sacubitril Hemicalcium
沙库比曲半钙盐 | Sacubitril Hemicalcium | 1369773-39-6 | Yn-hûs |
沙库比曲钠盐 | 149690-05-1 | Yn-hûs | |
LCZ-4 | 1426129-50-1 | Yn-hûs | |
LCZ-7 | 1012341-48-8 | Yn-hûs | |
LCZ-8 | 1012341-50-2 | Yn-hûs | |
LCZ-9 | 149690-12-0 | Yn-hûs |
Eftergrûn
AHU-377 hemicalcium sâlt is in hemicalcium sâlt foarm fan AHU-377.It is in ynhibitor fan neprilysin mei IC50 wearde fan 5 nM [1].
AHU-377 en de angiotensin II AT1 receptor antagonist valsartan komponearje LCZ696 yn in 1: 1 molêre ferhâlding.LCZ696 is in angiotensin receptor neprilysin inhibitor.It kin bloeddruk ferminderje en kin in nij medisyn wêze foar de behanneling fan hertfalen.AHU-377 is in pro-drug, it kin wurde omboud troch enzymatyske spjalting fan 'e ethylester yn' e aktive foarm LBQ657.It wurdt rapportearre dat AHU-377 (30 en 100 mg / kg, PO) antihypertensive effekt kin feroarsaakje op in dose-ôfhinklike manier yn DAHI-SS-ratten.Mar yn 'e DOCA-sâlt hypertensive ratten toant it in swakke reduksje [2, 3].
Referinsjes:
[1] Ksander GM, Ghai RD, deJesus R, Diefenbacher CG, Yuan A, Berry C, Sakane Y, Trapani A. Dicarboxylic acid dipeptide neutral endopeptidase inhibitors.J Med Chem.12 mei 1995;38(10):1689-700.
[2] Voors AA, Dorhout B, van der Meer P. The potential role of valsartan + AHU377 (LCZ696) in the treatment of heart failure.Expert Opin Investig Drugs.Aug 2013;22(8):1041-7.
[3] Laxminarayan G Hegde, Cecile Yu, Cheruvu Madhavi et al.Fergelykjende effektiviteit fan AHU-377, in krêftige neprilysin-ynhibitor, yn twa ratmodellen fan folume-ôfhinklike hypertensie.BMC Pharmacology 2011, 11 (Suppl 1): P33.
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