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Submit ReviewLopinavir is a highly potent and selective HIV-1 protease inhibitor (IC50 = 6.5 nM, HIV cultured in peripheral blood mononuclear cells; Ki = 1.3 pM). Displays >105-fold selectivity for HIV-1 protease over mammalian proteases including renin and cathepsin D and E. Inhibits HIV-1 protease in patient HIV isolates displaying mutations that confer resistance to ritonavir (Cat. No. 5856) (IC50 values in 5 - 50 nM range). Also inhibits SARS-CoV-2 replication in vitro (IC50 = 26 μM)
Lopinavir is also offered as part of the Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
分子量 | 628.8 |
公式 | C37H48N4O5 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 192725-17-0 |
PubChem ID | 92727 |
InChI Key | KJHKTHWMRKYKJE-SUGCFTRWSA-N |
Smiles | CC([C@@H](C(N[C@@H](CC1=CC=CC=C1)C[C@@H]([C@@H](NC(COC2=C(C=CC=C2C)C)=O)CC3=CC=CC=C3)O)=O)N4CCCNC4=O)C |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 62.88 | 100 | |
ethanol | 62.88 | 100 |
以下数据基于产品分子量 628.8。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.59 mL | 7.95 mL | 15.9 mL |
5 mM | 0.32 mL | 1.59 mL | 3.18 mL |
10 mM | 0.16 mL | 0.8 mL | 1.59 mL |
50 mM | 0.03 mL | 0.16 mL | 0.32 mL |
参考文献是支持产品生物活性的出版物。
Sham et al (1998) ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease. Antimicrob.Agents Chemother. 42 3218 PMID: 9835517
Carrillo et al (1998) In vitro selection and characterization of human immunodeficiency virus type 1 variants with increased resistance to ABT-378, a novel protease inhibitor. J.Virol. 72 7532 PMID: 9696850
Choy et al (2020) Remdesivir, lopinavir, emetine, and homoharringtonine inhibit SARS-CoV-2 replication in vitro. Antiviral Res. 178 PMID: 32251767
If you know of a relevant reference for Lopinavir, please let us know.
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