LCZ696杂质
中文名称 | LCZ696杂质 |
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中文同义词 | (2R,4S)-5-([1,1'-联苯]-4-基)-4-(3-羧酰氨基)-2-甲基戊酸;LCZ-696杂质1;LCZ696杂质900-04;CU屈二酸;沙库比曲杂质4;沙库必曲起始物料杂质3;脱乙基沙库巴曲;SACUBITRIL METABOLITE LBQ 657 |
英文名称 | Sacubitril Impurity 7 |
英文同义词 | LBQ657;Sacubitrilat;(2R,4S)-4-(3-carboxypropanoylamino)-2-methyl-5-(4-phenylphenyl)pentanoic acid;LCZ696-4;Diacid of Sacubitril;LCZ-696 Impurity 1;Sacubitrilat (LBQ-657);Sacubitril Desethyl Impurity |
CAS号 | 149709-44-4 |
分子式 | C22H25NO5 |
分子量 | 383.44 |
EINECS号 | |
相关类别 | 杂质对照品 |
Mol文件 | 149709-44-4.mol |
结构式 | ![]() |
LCZ696杂质 性质
沸点 | 705.4±60.0 °C(Predicted) |
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密度 | 1?+-.0.06 g/cm3(Predicted) |
储存条件 | Sealed in dry,Room Temperature |
溶解度 | DMF:30.0(最大浓度 mg/mL);78.24(最大浓度 mM) DMSO:77.0(最大浓度 mg/mL);200.81(最大浓度 mM) 乙醇:77.0(最大浓度 mg/mL);200.81(最大浓度 mM) 乙醇:PBS (pH 7.2) (1:1):0.5(最大浓度 mg/mL);1.3(最大浓度 mM) |
形态 | 结晶固体 |
酸度系数(pKa) | 4.59±0.23(Predicted) |
颜色 | 白色至米白色 |
Target | Value |
NEP
() |
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.
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 T max of 0.52 h for the 400 mg dose and 1.05 h for the 1200 mg dose, followed by Sacubitrilat, with the corresponding T max values of 2.07 and 3.05 h, respectively. The median T max for valsartan is 2.07 h for both the LCZ696 400 mg and 1200 mg doses. The C max of Sacubitrilat shows a dose proportional increase, while the C max of Sacubitril and Valsartan shows less than proportional increases between the doses. The arithmetic mean AUC 0-24 h and AUC last for Sacubitril and Sacubitrilat increases approximately dose proportionally, but shows less than dose proportional increase for Valsartan.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/04/30 | HY-17620 | Sacubitrilat | 1 mg | 545元 | |
2024/04/30 | HY-17620 | LCZ696杂质 Sacubitrilat | 149709-44-4 | 10mM * 1mLin DMSO | 1320元 |