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AHU-377 hemicalcium salt
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AHU-377 hemicalcium salt图片
CAS NO:1369773-39-6
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
AHU-377 hemicalcium salt (AHU-377 hemicalcium salt) 是一种有效的 NEP 抑制剂,IC50 为 5 nM。
Cas No.1369773-39-6
别名LCZ696中间体,AHU-377 hemicalcium salt
Canonical SMILESO=C(OCC)[C@@H](C)C[C@@H](NC(CCC([O-])=O)=O)CC1=CC=C(C2=CC=CC=C2)C=C1.[0.5Ca2+]
分子式C24H28Ca0.5NO5
分子量430.52
溶解度≥ 17.9mg/mL in DMSO
储存条件Store at 2-8℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

AHU-377 hemicalcium salt is a hemicalcium salt form of AHU-377. It is an inhibitor of neprilysin with IC50 value of 5 nM [1].

AHU-377 and the angiotensin II AT1 receptor antagonist valsartan compose LCZ696 in a 1:1 molar ratio. LCZ696 is an angiotensin receptor neprilysin inhibitor. It can reduce blood pressure and may be a novel drug for the treatment of heart failure. AHU-377 is a pro-drug, it can be converted by enzymatic cleavage of the ethyl ester into the active form LBQ657. It is reported that AHU-377(30 and 100 mg/kg, PO) can cause antihypertensive effect in a dose-dependent manner in DAHI-SS rats. But in the DOCA-salt hypertensive rats, it shows a weak reduction [2, 3].

References: [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. 1995 May 12; 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. 2013 Aug;22(8):1041-7. [3] Laxminarayan G Hegde, Cecile Yu, Cheruvu Madhavi et al. Comparative efficacy of AHU-377, a potent neprilysin inhibitor, in two rat models of volume-dependent hypertension. BMC Pharmacology 2011, 11(Suppl 1):P33.