Lopinavir-d8
目录号 : GC47573
An internal standard for the quantification of lopinavir
Cas No.:1322625-54-6
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Lopinavir-d8 is intended for use as an internal standard for the quantification of lopinavir by GC- or LC-MS. Lopinavir is a potent HIV-1 protease inhibitor (Ki = 1.3 pM for wild-type enzyme).1 It inhibits the replication of clinical isolates of HIV-1 (EC50s = 5-52 nM). Lopinavir reduces the infectious virus yield and viral RNA copy numbers in the culture supernatant of Vero E6 cells infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2; EC50s = 26.63 and 26.10 µM, respectively).2 It reduces lung and kidney viral load, bronchointerstitial pneumonia, and pulmonary inflammatory cell infiltration in a marmoset model of Middle East respiratory syndrome coronavirus (MERS-CoV) infection when administered in combination with ritonavir .3
1.Sham, H.L., Kempf, D.J., Molla, A., et al.ABT-378, a highly potent inhibitor of the human immunodeficiency virus proteaseAntimicrob. Agents Chemother.42(12)3218-3224(1998) 2.Choy, K.-T., Wong, A.-Y., Kaewpreedee, P., et al.Remdesivir, lopinavir, emetine, and homoharringtonine inhibit SARS-CoV-2 replication in vitroAntiviral Res.178104786(2020) 3.Chan, J.-F., Yao, Y., Yeung, M.-L., et al.Treatment with lopinavir/ritonavir or interferon-β1b improves outcome of MERS-CoV infection in a nonhuman primate model of common marmosetJ. Infect. Dis.212(12)1904-1913(2015)
| Cas No. | 1322625-54-6 | SDF | |
| Canonical SMILES | O=C1NCCCN1C(C(C([2H])([2H])[2H])([2H])C([2H])([2H])[2H])([2H])C(N[C@@H](CC2=CC=CC=C2)C[C@H](O)[C@H](CC3=CC=CC=C3)NC(COC4=C(C)C=CC=C4C)=O)=O | ||
| 分子式 | C37H40D8N4O5 | 分子量 | 636.9 |
| 溶解度 | Chloroform: Slightly Soluble,Methanol: Slightly 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.5701 mL | 7.8505 mL | 15.7011 mL |
| 5 mM | 0.314 mL | 1.5701 mL | 3.1402 mL |
| 10 mM | 0.157 mL | 0.7851 mL | 1.5701 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 an electrospray ionization LC-MS/MS method for quantitative analysis of raltegravir, etravirine, and 9 other antiretroviral agents in human plasma samples
Ther Drug Monit 2009 Dec;31(6):695-702.PMID:19865000DOI:10.1097/FTD.0b013e3181c05adf
Background: Raltegravir is the first human immunodeficiency virus-1 (HIV-1) integrase inhibitor used in treatment-experienced patients who have evidence of viral replication and HIV-1 strains resistance to multiple antiretroviral regimens. Etravirine is a novel NNRTI, active against HIV-1 strains harboring multiple NNRTI mutations. A liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed for the quantification of raltegravir, etravirine, and 9 other antiretroviral agents (amprenavir, atazanavir, darunavir, efavirenz, indinavir, lopinavir, ritonavir, saquinavir, and tipranavir) in plasma at the concentrations associated with therapy. Materials and methods: The ritonavir analog, methyl indinavir, and Lopinavir-d8 were used as internal standards, added to 100 microL of plasma sample prior to a protein precipitation using methanol. Chromatographic separation was achieved on a C18 HPLC column (Waters Sunfire 100 x 2.1 mm, 3.5 microm) with a mobile phase gradient at a flow rate of 0.3 mL/min. Five microL of sample were injected into the LC-MS/MS system (Waters Quattro Premier XE) to determine concentrations of raltegravir, etravirine, and other antiretroviral agents. Results and discussion: This method showed an excellent linearity for all calibration curves (r2 > 0.998). The lower limit of quantification was established at 5 ng/mL for raltegravir and 40 ng/mL for etravirine, with precision and accuracy within +/-20% and 80% to 120% for all analytes. Intraassay and interassay precision and inaccuracy ranged from -9.2% to 6.9% for raltegravir and from -14.3% to 12.3% for etravirine and were less than 15% for all other compounds. No matrix effect was observed for any of the antiretrovirals studied. Conclusion: A rapid, specific, and sensitive LC-MS/MS method for quantification of raltegravir, etravirine, and 9 other antiretrovirals in human plasma was developed and was successfully applied for routine therapeutic drug monitoring.