Lopinavir
(Synonyms: 洛匹那韦; ABT-378) 目录号 : GC13716
A potent HIV-1 protease inhibitor
Cas No.:192725-17-0
Sample solution is provided at 25 µL, 10mM.
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Lopinavir (also known as ABT-378) is a highly potent inhibitor of human immunodeficiency virus (HIV) protease that potently inhibits wild-type and mutant HIV protease with inhibition constant Ki values ranging from 1.3 to 3.6 pM. Lopinavir, a ritonavir analog designed to have a diminished interaction with Val82 in HIV protease, maintains a high potency inhibiting Val82 mutant HIV selected by ritonavir with 50% effective concentration EC50 value lower than 0.06 μM. Although the antiviral activity of ritonavir is considerably attenuated by human serum, lopinavir is less affected by human serum proteins and is 10-fold greater in potency than ritonavir in the presence of human serum.
Reference
[1].Sham HL, Kempf DJ, Molla A, Marsh KC, Kumar GN, Chen CM, Kati W, Stewart K, Lal R, Hsu A, Betebenner D, Korneyeva M, Vasavanonda S, McDonald E, Saldivar A, Wideburg N, Chen X, Niu P, Park C, Jayanti V, Grabowski B, Granneman GR, Sun E, Japour AJ, Leonard JM, Plattner JJ, Norbeck DW. ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease. Antimicrob Agents Chemother. 1998 Dec;42(12):3218-24.
| Cell experiment [1]: | |
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Cell lines |
MT4 cells |
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Preparation method |
The solubility of this compound in DMSO is > 31.5 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
|
Reacting condition |
4 ~ 52 nM |
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Applications |
HIV with multiple mutations was markedly less resistant to Lopinavir than to Ritonavir. Although the activity of Lopinavir declined significantly against the multiply mutated strains compared with its activity against the baseline strains, the extent of the decline was substantially less than that of Ritonavir. Furthermore, the EC50 value of Lopinavir against HIV with multiple mutations was 10-fold lower than that of Ritonavir. |
| Animal experiment [1]: | |
|
Animal models |
Rats |
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Dosage form |
10 mg/kg; p.o. |
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Applications |
The Cmax and oral bioavailability of Lopinavir in rats were 0.8 μg/mL and 25%, respectively. At 6th hr, the plasma level of Lopinavir declined below the level of quantitation (0.01 μg/mL). However, co-administration of Lopinavir with Ritonavir (10 mg/kg) maintained the concentrations of Lopinavir in excess of 3 μg/mL with low variability. In addition, the area under the plasma concentration-time curve from 0 ~ 8 hrs for Lopinavir increased 14-fold due to Ritonavir co-administration. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1]. Sham HL, Kempf DJ, Molla A, Marsh KC, Kumar GN, Chen CM, Kati W, Stewart K, Lal R, Hsu A, Betebenner D, Korneyeva M, Vasavanonda S, McDonald E, Saldivar A, Wideburg N, Chen X, Niu P, Park C, Jayanti V, Grabowski B, Granneman GR, Sun E, Japour AJ, Leonard JM, Plattner JJ, Norbeck DW. ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease. Antimicrob Agents Chemother. 1998 Dec;42(12):3218-24. |
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| Cas No. | 192725-17-0 | SDF | |
| 别名 | 洛匹那韦; ABT-378 | ||
| 化学名 | (2S)-N-[(2S,4S,5S)-5-[[2-(2,6-dimethylphenoxy)acetyl]amino]-4-hydroxy-1,6-diphenylhexan-2-yl]-3-methyl-2-(2-oxo-1,3-diazinan-1-yl)butanamide | ||
| Canonical SMILES | CC1=C(C(=CC=C1)C)OCC(=O)NC(CC2=CC=CC=C2)C(CC(CC3=CC=CC=C3)NC(=O)C(C(C)C)N4CCCNC4=O)O | ||
| 分子式 | C37H48N4O5 | 分子量 | 628.81 |
| 溶解度 | ≥ 31.45mg/mL in DMSO, ≥ 48.3 mg/mL in EtOH | 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 | 1.5903 mL | 7.9515 mL | 15.9031 mL |
| 5 mM | 0.3181 mL | 1.5903 mL | 3.1806 mL |
| 10 mM | 0.159 mL | 0.7952 mL | 1.5903 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。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet