Sacubitrilat-LBQ-657-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESacubitrilatCat. No.: HY-17620CAS No.: 149709-44-4Synonyms: LBQ-657分式: CHNO分量: 383.44作靶点: Neprilysin作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (

2、260.80 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.6080 mL 13.0399 mL 26.0797 mL5 mM 0.5216 mL 2.6080 mL 5.2159 mL10 mM 0.2608 mL 1.3040 mL 2.6080 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结

3、果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.52 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.52 mM); Clear solution1/2 Master of Small Molecules

4、 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.52 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Sacubitrilat种活性的脑啡肽酶 (NEP) 抑制剂。IC50 & Target Neprilysin 1体外研究 Sacubitrilat (LBQ657) is a single diastereomer with specific stereocenters. Sacubitrilat is bound to the activesi

5、te of NEP by an intricate network of interactions that involves all functional groups of the compound givingrise to the high inhibitory potency of 5nM 1.体内研究 Pharmacokinetics of Sacubitril, Sacubitrilat (LBQ657), and valsartan following the administration of singleoral doses of LCZ696 400 or 1200 mg

6、 under fasting condition are summarized. The mean plasmaconcentrations of Sacubitril increases rapidly with a median Tmax of 0.52 h for the 400 mg dose and 1.05 hfor the 1200 mg dose, followed by Sacubitrilat, with the corresponding Tmax values of 2.07 and 3.05 h,respectively. The median Tmax for va

7、lsartan is 2.07 h for both the LCZ696 400 mg and 1200 mg doses. TheCmax of Sacubitrilat shows a dose proportional increase, while the Cmax of Sacubitril and Valsartan showsless than proportional increases between the doses. The arithmetic mean AUC0-24 h and AUClast forSacubitril and Sacubitrilat inc

8、reases approximately dose proportionally, but shows less than doseproportional increase for Valsartan 2.REFERENCES1. 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 cardiacrepolarization. Eur J Clin Pharmacol. 2016 Aug;72(8):917-24.McePdfHeightCaution: Product has not been fully validated for medical appli