CAS NO: | 1369773-39-6 |
包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
Cas No. | 1369773-39-6 |
别名 | LCZ696中间体,AHU-377 hemicalcium salt |
Canonical SMILES | O=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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation 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. |