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Lopinavir

现货
Catalog No.
A8204
HIV蛋白酶抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
现货
50mg
¥ 500.00
现货
100mg
¥ 800.00
现货
250mg
¥ 1,600.00
现货

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Background

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

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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt628.81
Cas No.192725-17-0
FormulaC37H48N4O5
SynonymsLopinavir
Solubility≥31.45mg/mL in DMSO, ≥48.3 mg/mL in EtOH, <2.21 mg/mL in H2O
Chemical Name(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
SDFDownload SDF
Canonical SMILESCC1=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
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

MT4细胞

制备方法

在DMSO中的溶解度大于31.5 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

4 ~ 52 nM

实验结果

相对于Ritonavir,具有多重突变的HIV对Lopinavir的耐受性显著降低。相对于对照组菌株,尽管Lopinavir对多重突变菌株的活性显著下降,但其下降程度明显低于Ritonavir。此外,Lopinavir对多重突变HIV的EC50值比Ritonavir低10倍。

动物实验 [1]:

动物模型

大鼠

给药剂量

10 mg/kg;口服

实验结果

Lopinavir在大鼠中的Cmax和口服生物利用度分别为0.8 μg/mL和25%。在第6小时,Lopinavir血浆水平下降到定量限以下 (0.01 μg/mL)。然而,联合使用Lopinavir与Ritonavir (10 mg/kg) 使Lopinavir浓度维持在3 μg/mL以上,而且浓度波动不大。此外,联合使用Ritonavir使Lopinavir在0 ~ 8小时的血浆浓度-时间曲线下面积增加14倍。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

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.

生物活性

描述 Lopinavir是一种强效的HIV蛋白酶抑制剂,Ki值为1.3 pM。
靶点 HIV protease          
IC50 1.3 pM (Ki)          

质量控制

化学结构

Lopinavir