貨號	規(guī)格	價格	上海	北京	武漢	南京
S83483-5mg	99.5%	￥425.00 S83483-5mg ￥425.00 現(xiàn)貨	1536 >10	-	-	-
S83483-10mg	99.5%	￥637.50 S83483-10mg ￥637.50 現(xiàn)貨	773 >10	-	-	-
S83483-25mg	99.5%	￥880.00 S83483-25mg ￥880.00 現(xiàn)貨	312 >10	-	-	-
S83483-50mg	99.5%	￥1490.00 S83483-50mg ￥1490.00 現(xiàn)貨	162 >10	-	-	-
S83483-250mg	99.5%	￥5100.00 S83483-250mg ￥5100.00 現(xiàn)貨	34 >10	-	-	-

產(chǎn)品介紹

Sacubitril (AHU-377) is a potent and orally active NEP (neprilysin) inhibitor with an IC50 of 5 nM. Sacubitril is a component of the heart failure medicine LCZ696. Sacubitril can be used for the research of heart failure, hypertension and COVID-19

產(chǎn)品描述：

靶點(diǎn)：

IC50: 5 nM (NEP);Neprilysin

體外研究：

Sacubitril (AHU-377) is a single molecule that is comprised of molecular moieties of valsartan, an ARB, and Sacubitril (AHU-377), a neprilysin inhibitor (1:1 ratio). Sacubitril (AHU-377) is converted by enzymatic cleavage of the ethyl ester into the active neprilysin inhibiting metabolite LBQ657. The inactive NEPi precursor, Sacubitril (AHU-377), does not inhibit collagen accumulation in fibroblasts nor cardiac myocyte hypertrophy. In cardiac fibroblasts, the active NEPi LBQ657 had no discernible effects. In contrast, LBQ657 modestly inhibits cardiac myocyte hypertrophy

體內(nèi)研究：

In vehicle-treated dogs, ANF increases urinary sodium excretion from 17.3±3.6 to 199.5±18.4 pequivkglmin. This effect is potentiated significantly in animals which receive Sacubitril (AHU-377). Urinary volume is also potentiated in animals which receive an iv administration of Sacubitril (AHU-377). In normotensive rats, pretreatment with Sacubitril (3, 10 and 30 mg/kg, PO.) augments ANP-evoked plasma cGMP levels by 2.4, 3.3 and 4.0 fold, respectively (4h AUC compared to vehicle). Sacubitril (30 and 100 mg/kg, PO) produces a dose-dependent antihypertensive effect in Dahl-SS rats

參考文獻(xiàn)：

1. Ksander GM, et al. Dicarboxylic acid dipeptide neutral endopeptidase inhibitors. J Med Chem. 1995 May 12;38(10):1689-700. 2. Voors AA, et al. The potential role of valsartan + AHU377 ( LCZ696 ) in the treatment of heart failure. Expert Opin Investig Drugs. 2013 Aug;22(8):1041-7. 3. von Lueder TG, et al. Angiotensin receptor neprilysin inhibitor LCZ696 attenuates cardiac remodeling and dysfunction after myocardial infarction by reducing cardiac fibrosis and hypertrophy. Circ Heart Fail. 2015 Jan;8(1):71-8. 4. Hegde, L.G., et al. Comparative efficacy of AHU-377, a potent neprilysin inhibitor, in two rat models of volume-dependent hypertension. BMC Pharmacol 11, P33 (2011).

溶解性：

Soluble in DMSO、H2O

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.43 ml	12.151 ml	24.302 ml
5 mM	0.486 ml	2.43 ml	4.86 ml
10 mM	0.243 ml	1.215 ml	2.43 ml
50 mM	0.049 ml	0.243 ml	0.486 ml

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻(xiàn)

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