2R,4R-Sacubitril
(Synonyms: LCZ696杂质B) 目录号 : GC32645
2R,4R-Sacubitril是Sacubitri的杂质。美国食品和药物管理局批准Sacubitril与缬沙坦联合用于治疗患有心力衰竭的患者。
Cas No.:766480-48-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
2R,4R-Sacubitril is the impurity of Sacubitril. Sacubitril is approved by the Food and Drug Administration for use in combination with valsartan for the treatment of patients with heart failure.
[1]. Shi J, et al. Sacubitril Is Selectively Activated by Carboxylesterase 1 (CES1) in the Liver and the Activation Is Affected by CES1 Genetic Variation. Drug Metab Dispos. 2016 Apr;44(4):554-9.
| Cas No. | 766480-48-2 | SDF | |
| 别名 | LCZ696杂质B | ||
| Canonical SMILES | [H]N(C(CCC(O)=O)=O)[C@@H](CC(C=C1)=CC=C1C2=CC=CC=C2)C[C@H](C(OCC)=O)C | ||
| 分子式 | C24H29NO5 | 分子量 | 411.49 |
| 溶解度 | DMSO : 100 mg/mL (243.02 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4302 mL | 12.151 mL | 24.3019 mL |
| 5 mM | 0.486 mL | 2.4302 mL | 4.8604 mL |
| 10 mM | 0.243 mL | 1.2151 mL | 2.4302 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Development and validation of a novel stability-indicating reverse phase HPLC method for the determination of sacubitril-valsartan premix stereoisomers: Cellulose tris(4-methyl benzoate) stationary phase
J Sep Sci 2022 Oct;45(19):3714-3724.PMID:35907257DOI:10.1002/jssc.202200363
A new stability indicating reverse phase HPLC method has been developed and validated as per International Conference on Harmonization guidelines for the determination of sacubitril-valsartan premix stereoisomers, namely, (2R)-valsartan, (2S,4S)-sacubitril, (2R,4S)-sacubitril, and (2R,4R)-Sacubitril. Primarily, stability indicating separation study was done on reverse phase LC conditions; it was described by peak homogeneity of sacubitril-valsartan and its stereoisomers. Cellulose tris(4-methylbenzoate) packing column Chiralcel OJ-RH(150 mm × 4.6 mm), 5 μm provided better resolution than those of amylose based stationary phase's. Resolution between two arbitrary adjacent analyte was found to be more than 2.0 with 0.1% trifluoroacetic acid in water as mobile phase-A and mobile phase-B consisting of acetonitrile, methanol, and trifluoroacetic acid (90:10:0.1, v/v/v). Gradient elution was performed at a flow rate of 1.0 ml/min, column temperature 20°C, injection volume 10 μl, UV detection at 254 nm and run time was 52 min. The detector response linearity of stereoisomers found to be linear (R2 ≿0.9998), limit of detection (0.290 μg/ml, 0.122 μg/ml, 0.123 μg/ml, and 0.124 μg/ml), and limit of quantification (0.878 μg/ml, 0.370 μg/ml, 0.373 μg/ml, and 0.375 μg/ml), respectively. Percentage recovery was found to be 98-105. Finally, the proposed method is user friendly and can be used in bulk drugs analysis.