Darunavir-d9
(Synonyms: 九氘代地瑞拉为,TMC114-d9; UIC-94017-d9) 目录号 : GC47173
An internal standard for the quantification of darunavir
Cas No.:1133378-37-6
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
Darunavir-d9 is intended for use as an internal standard for the quantification of darunavir by GC- or LC-MS. Darunavir is an HIV-1 protease inhibitor.1 It is active against HIV-1LAI in MT-2 cells (IC50 = 3 nM) with a cytotoxic concentration (CC50) of 74.4 μM. Darunavir is also active against wild-type and multidrug-resistant clinical isolates of HIV-1 in phytohemagglutinin-activated peripheral blood mononuclear cells (PHA-PBMCs; IC50s = 3 and 3-29 nM, respectively). It inhibits cell-free diffusion and cell-to-cell spread of HIV-1 in Jurkat cell populations (IC50s = 2.5 and 2.8 nM, respectively).2 Formulations containing darunavir have been used in combination therapy for the treatment of HIV.
1.Koh, Y., Nakata, H., Maeda, K., et al.Novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI) UIC-94017 (TMC114) with potent activity against multi-PI-resistant human immunodeficiency virus in vitroAntimicrob. Agents Chemother.47(10)3123-3129(2003) 2.Titanji, B.K., Aasa-Chapman, M., Pillay, D., et al.Protease inhibitors effectively block cell-to-cell spread of HIV-1 between T cellsRetrovirology10161(2013)
| Cas No. | 1133378-37-6 | SDF | |
| 别名 | 九氘代地瑞拉为,TMC114-d9; UIC-94017-d9 | ||
| Canonical SMILES | O=C(N[C@@H](CC1=CC=CC=C1)[C@@H](CN(C([2H])([2H])C(C([2H])([2H])[2H])([2H])C([2H])([2H])[2H])S(C2=CC=C(N)C=C2)(=O)=O)O)O[C@H]3CO[C@]4([H])[C@@]3([H])CCO4 | ||
| 分子式 | C27H28D9N3O7S | 分子量 | 556.7 |
| 溶解度 | DMF: Soluble,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 | 1.7963 mL | 8.9815 mL | 17.963 mL |
| 5 mM | 0.3593 mL | 1.7963 mL | 3.5926 mL |
| 10 mM | 0.1796 mL | 0.8981 mL | 1.7963 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。
Application of a validated ultra performance liquid chromatography-tandem mass spectrometry method for the quantification of darunavir in human plasma for a bioequivalence study in Indian subjects
J Chromatogr B Analyt Technol Biomed Life Sci 2011 Aug 15;879(24):2443-53.PMID:21788160DOI:10.1016/j.jchromb.2011.07.008
A simple, precise and rapid ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method has been developed and validated for the quantification of darunavir, a protease inhibitor, using Darunavir-d9 as internal standard (IS). The method involved liquid-liquid extraction of darunavir and IS in methyl-tert-butyl ether from 50 μL human plasma. The chromatographic separation was achieved on an Acquity UPLC BEH C18 (50 mm × 2.1mm, 1.7 μm particle size) analytical column under gradient conditions, in a run time of 1.6 min. The precursor → product ion transitions for darunavir (m/z 548.1 → 392.0) and IS (m/z 557.1 → 401.0) were monitored on a triple quadrupole mass spectrometer, operating in the multiple reaction monitoring (MRM) and positive ion mode. The method was extensively validated for its selectivity, sensitivity, carryover check, linearity, precision and accuracy, reinjection reproducibility, recovery, matrix effect, ion suppression/enhancement, stability and dilution integrity. The linearity of the method was established in the concentration range of 1.0-5000 ng/mL. The mean relative recovery for darunavir (100.8%) and IS (89.8%) from spiked plasma samples was consistent and reproducible. The application of this method for routine measurement of plasma darunavir concentration was demonstrated by a bioequivalence study conducted in 40 healthy Indian subjects for a 600 mg tablet formulation along with 100mg ritonavir as booster under fast and fed conditions. To demonstrate the reproducibility in the measurement of study data, an incurred sample reanalysis was done with 400 subject samples and the % change in concentration was within ± 12%.