Clevidipine-d7
(Synonyms: 氯维地平 d7) 目录号 : GC47100
A neuropeptide with diverse biological activities
Cas No.:2747918-66-5
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
Clevidipine-d7 is intended for use as an internal standard for the quantification of clevidipine by GC- or LC-MS. Clevidipine is an inhibitor of L-type calcium channels (IC50s = 7.1 and 78.8 nM at -40 and -80 mV, respectively, in isolated guinea pig cardiomyocytes).1 It preferentially inhibits L-type calcium channels in isolated rat portal vein over rat left ventricle (IC50s = 427 and 20,417 nM, respectively).2 Clevidipine decreases mean arterial pressure in anesthetized normotensive or spontaneously hypertensive rats with ED30 values of 316 and 58 nmol/kg, respectively. Formulations containing clevidipine have been used in the treatment of hypertension.
1.Yi, X., Vivien, B., and Lynch, C., IIIClevidipine blockade of L-type Ca2+ currents: Steady-state and kinetic electrophysiological studies in guinea pig ventricular myocytesJ. Cardiovasc. Pharmacol.36(5)592-600(2000) 2.Norlander, M., SjÖquist, P.O., Ericsson, H., et al.Pharmacodynamic, pharmacokinetic and clinical effects of clevidipine, an ultrashort-acting calcium antagonist for rapid blood pressure controlCardiovasc. Drugs Ther.22(3)227-250(2004)
| Cas No. | 2747918-66-5 | SDF | |
| 别名 | 氯维地平 d7 | ||
| Canonical SMILES | O=C(C1=C(C)NC(C)=C(C1C2=C(Cl)C(Cl)=CC=C2)C(OCOC(C([2H])([2H])C([2H])([2H])C([2H])([2H])[2H])=O)=O)OC | ||
| 分子式 | C21H16Cl2D7NO6 | 分子量 | 463.4 |
| 溶解度 | DMSO: Soluble,Methanol: Soluble | 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 | 2.158 mL | 10.7898 mL | 21.5796 mL |
| 5 mM | 0.4316 mL | 2.158 mL | 4.3159 mL |
| 10 mM | 0.2158 mL | 1.079 mL | 2.158 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 samples stabilization strategy and LC-MS/MS method for simultaneous determination of clevidipine and its primary metabolite in human plasma: Application to clinical pharmacokinetic study in Chinese healthy volunteers
J Chromatogr B Analyt Technol Biomed Life Sci 2020 Dec 15;1161:122448.PMID:33246284DOI:10.1016/j.jchromb.2020.122448
A feasible LC-MS/MS method with reliable stabilizers consisted of sodium fluoride, ascorbic acid and formic acid was developed and validated for the determination of clevidipine and its primary metabolite (H152/81) in human plasma. Sodium fluoride existing in the vacutainer tubes was used to inhibit esterase activity to protect the clevidipine from hydrolysis as soon as blood was collected. Ascorbic acid and formic acid were added to the separated plasma samples to avoid the oxidation and further hydrolysis of clevidipine and H152/81. The further sample preparation was accomplished through a single step liquid-liquid extraction (LLE) by ethyl acetate. The chromatography separation was carried out on an ACE Excel 3 μm SuperC18 (2.1 × 50 mm, id, ACE, United Kingdom) column with gradient elution using 10 mM ammonium acetate water solution and methanol as the mobile phase. Detection was performed in the negative ion electrospray ionization mode using multiple reaction monitoring (clevidipine: m/z 454.1 → 234.0; Clevidipine-d7: m/z 461.1 → 240.1; H152/81: m/z 354.0 → 208.0; H152/81-13CD3: m/z 358.0 → 212.0). The method exhibited good linearity over the concentration ranges of 0.100 to 40.0 ng/mL for clevidipine and 5.00 to 400 ng/mL for H152/81. The intra- and inter-batch precision and accuracy of clevidipine and H152/81 were all within the acceptable criteria. The method was successfully applied to a pharmacokinetic study of clevidipine and H152/81 in healthy Chinese volunteers following 8 mg/h intravenous infusion of clevidipine butyrate injectable emulsion for 0.5 h. The results showed that clevidipine was rapidly eliminated with a short half-life time of 0.244 ± 0.125 h and a maximum concentration of 25.2 ± 7.09 ng/mL. H152/81 was detectable in the plasma samples up to 48.5 h with a half-life time of 10.7 ± 2.30 h and a maximum plasma concentration of 301 ± 38.1 ng/mL.