Empagliflozin-d4
(Synonyms: BI 10773-d4) 目录号 : GC47289
A neuropeptide with diverse biological activities
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Empagliflozin-d4 contains four deuterium atoms and is intended for use as an internal standard for the quantification of empagliflozin by GC- or LC-MS. Empagliflozin is a potent SGLT2 inhibitor (IC50 = 3.1 nM) that demonstrates a high degree of selectivity (>2,500-fold) over SGLT1, 4, 5, and 6.1 In clinical trials of patients with type 2 diabetes, formulations containing empagliflozin lowered fasting and postprandial glucose levels by increasing total glucose excretion, improving β-cell function, and shifting substrate utilization from glucose to lipids.2
1.Grempler, R., Thomas, L., Eckhardt, M., et al.Empagliflozin, a novel selective sodium glucose contransporter-2 (SGLT-2) inhibitor: Characterisation and comparison with other SGLT-2 inhibitorsDiabetes Obes. Metab.14(1)83-90(2012) 2.Ndefo, U.A., Anidiobi, N.O., Basheer, E., et al.Empagliflozin (Jardiance): A novel SGLT2 inhibitor for the treatment of type-2 diabetesP.T.40(6)364-368(2015)
| Cas No. | N/A | SDF | |
| 别名 | BI 10773-d4 | ||
| Canonical SMILES | ClC(C=CC([C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1)=C2)=C2CC3=C([2H])C([2H])=C(O[C@@H]4COCC4)C([2H])=C3[2H] | ||
| 分子式 | C23H23D4ClO7 | 分子量 | 454.9 |
| 溶解度 | DMSO: Solube | 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 | 2.1983 mL | 10.9914 mL | 21.9829 mL |
| 5 mM | 0.4397 mL | 2.1983 mL | 4.3966 mL |
| 10 mM | 0.2198 mL | 1.0991 mL | 2.1983 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。
Validation of a novel UPLC-MS/MS method for estimation of metformin and empagliflozin simultaneously in human plasma using freezing lipid precipitation approach and its application to pharmacokinetic study
J Pharm Biomed Anal 2021 Jun 5;200:114078.PMID:33901756DOI:10.1016/j.jpba.2021.114078
A fast, sensitive one step UPLC ESI-MS/MS method was successfully applied for the simultaneous estimation of two concurrently administrated antidiabetic drugs, Metformin (MET) and Empagliflozin (EMPA) in human plasma. Metformin-d6 (MET-d6) and Empagliflozin-d4 (EMPA-d4) were utilized as internal standards. Extraction of the analytes from the human plasma was performed through acetonitrile precipitation technique followed by freezing the precipitated plasma proteins and lipids to minimize the matrix effect. Chromatographic analysis was developed on Acquity UPLC BEH C18 column (1.7 μm, 2.1 × 50 mm) using isocratic elution mode. A mobile phase of formic acid (0.01 %): acetonitrile (70:30 v/v) with a flow rate of 0.3 mL/min achieved optimum separation. Multiple reaction monitoring (MRM) in positive ion mode, with transitions at (m/z) 130.14 →71.08 for (MET), 451.72 →71.29 for (EMPA), 136.03 →77.02 for (MET-d6), and 455.43 → 75.05 for (EMPA-d4) was used for quantification. The obtained linearity covered the concentration ranges of 10-1500 ng/mL and 2.0-250.0 ng/mL for MET and EMPA, respectively. The run time of the proposed Method didn't exceed 3.0 min allowing faster analysis and determination of larger number of samples per day without affecting accuracy and sensitivity. The presented chromatographic method could be successfully applied in pharmacokinetics studies and therapeutic monitoring of MET and EMPA in patients' plasma administrating fixed dose combination of both drug with high reproducibility and ruggedness.