货号	规格	价格	上海	北京	珠海	重庆	武汉
S83481-5mg	≥98%	￥200.00 S83481-5mg ￥200.00 现货	190 >10	-	-	-	-
S83481-10mg	≥98%	￥350.00 S83481-10mg ￥350.00 现货	95 >10	-	-	-	-
S83481-25mg	≥98%	￥550.00 S83481-25mg ￥550.00 现货	37 >10	-	-	-	-
S83481-50mg	≥98%	￥800.00 S83481-50mg ￥800.00 现货	18 >10	-	-	-	-

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产品描述：

Sacubitrilat (Desethyl Sacubitril) is an active neprilysin (NEP) inhibitor.

靶点：

Neprilysin

体外研究：

Sacubitrilat (LBQ657) is a single diastereomer with specific stereocenters. Sacubitrilat is bound to the active site of NEP by an intricate network of interactions that involves all functional groups of the compound giving rise to the high inhibitory potency of 5 nM

体内研究：

Pharmacokinetics of Sacubitril, Sacubitrilat (LBQ657), and valsartan following the administration of single oral doses of LCZ696 400 or 1200 mg under fasting condition are summarized. The mean plasma concentrations of Sacubitril increases rapidly with a median Tmax of 0.52 h for the 400 mg dose and 1.05 h for the 1200 mg dose, followed by Sacubitrilat, with the corresponding Tmax values of 2.07 and 3.05 h, respectively. The median Tmax for valsartan is 2.07 h for both the LCZ696 400 mg and 1200 mg doses. The Cmax of Sacubitrilat shows a dose proportional increase, while the Cmax of Sacubitril and Valsartan shows less than proportional increases between the doses. The arithmetic mean AUC0-24 h and AUClast for Sacubitril and Sacubitrilat increases approximately dose proportionally, but shows less than dose proportional increase for Valsartan

参考文献：

1. Schiering N, et al. Structure of neprilysin in complex with the active metabolite of sacubitril. Sci Rep. 2016 Jun 15;6:27909. 2. Langenickel TH, et al. Single therapeutic and supratherapeutic doses of sacubitril/valsartan (LCZ696) do not affect cardiac repolarization. Eur J Clin Pharmacol. 2016 Aug;72(8):917-24.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.608 ml	13.04 ml	26.08 ml
5 mM	0.522 ml	2.608 ml	5.216 ml
10 mM	0.261 ml	1.304 ml	2.608 ml
50 mM	0.052 ml	0.261 ml	0.522 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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