受注:045-509-1970 |
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Synonyms | ABT-378 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C37H48N4O5 |
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分子量 | 628.8 | CAS No. | 192725-17-0 | |
Solubility (25°C)* | 体外 | DMSO | 126 mg/mL (200.38 mM) | |
Ethanol | 126 mg/mL (200.38 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Lopinavir (ABT-378) is a potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay. |
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in vitro | Lopinavir binds to mutant HIV protease (V82A, V82F and V82T) with Ki of 4.9 pM, 3.7 pM and 3.6 pM, respectively. Lopinavir inhibits 93% of wild-type HIV protease activity at 0.5 nM. Lopinavir inhibits HIV protease activity in the absence and presence of 50% HS with EC50 of 17 nM and 102 nM, respectively, in MT4 cells. [1] Lopinavir is converted to several metabolites in an NADPH-dependent manner in liver microsomes with the primary metabolites M-3 and M-4. [2] Lopinavir is a potent inhibitor of Rh123 efflux in Caco-2 monolayers with IC50 of 1.7 mM. Lopinavir exposure (72 hours) in LS 180V cells reduces the content of intracellular Rh123. Lopinavir induces P-glycoprotein immunoreactive protein and messenger RNA levels in LS 180V cells. [3] Lopinavir inhibits subtype C clone C6 with IC50 of 9.4 nM. [4] Lopinavir inhibits CYP3A with IC50 of 7.3 mM in human liver microsomes, while produces negligible or weak inhibition of human CYP1A2, 2B6, 2C9, 2C19 and 2D6. [5] |
in vivo | Lopinavir (10 mg/kg, orally) results in Cmax of 0.8 μg/mL and oral bioavailability of 25% in rats. [1] |
キナーゼアッセイ | HIV protease inhibition | |
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Inhibition of the activity of recombinant wild-type and mutant HIV type 1 (HIV-1) proteases is measured by a continuous fluorometric assay with the internally quenched fluorogenic substrate DABCYL-GABA-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-EDANS. The apparent Ki is estimated by nonlinear regression by the equation for tightly binding inhibitors. | ||
動物実験 | 動物モデル | Sprague-Dawley-derived rats or cynomolgus monkeys |
投薬量 | 10 mg/kg | |
投与方法 | Orally |
Data from [Data independently produced by Antimicrob Agents Chemother, 2014, 58(8), 4875-84]
Data from [Data independently produced by , , Biochim Biophys Acta, 2017, 1864(3):475-486]
Reactivated endogenous retroviruses promote protein aggregate spreading [ Nat Commun, 2023, 14(1):5034] | PubMed: 37596282 |
Reactivated endogenous retroviruses promote protein aggregate spreading [ Nat Commun, 2023, 14(1):5034] | PubMed: 37596282 |
Stabilization of the Dimeric State of SARS-CoV-2 Main Protease by GC376 and Nirmatrelvir [ Int J Mol Sci, 2023, 24(7)6062] | PubMed: 37047038 |
Garbage in, garbage out: how reliable training data improved a virtual screening approach against SARS-CoV-2 MPro [ Front Pharmacol, 2023, 14:1193282] | PubMed: 37426813 |
The Interleukin-11/IL-11 Receptor Promotes Glioblastoma Survival and Invasion under Glucose-Starved Conditions through Enhanced Glutaminolysis [ Int J Mol Sci, 2023, 24(4)3356] | PubMed: 36834778 |
Stabilization of the Dimeric State of SARS-CoV-2 Main Protease by GC376 and Nirmatrelvir [ Int. J. Mol. Sci, 2023, 10.3390/ijms24076062] | PubMed: None |
Biological and Structural Analyses of New Potent Allosteric Inhibitors of HIV-1 Integrase [ Antimicrob Agents Chemother, 2023, 67(7):e0046223] | PubMed: 37310224 |
The IDentif.AI-x pandemic readiness platform: Rapid prioritization of optimized COVID-19 combination therapy regimens [ NPJ Digit Med, 2022, 5(1):83] | PubMed: 35773329 |
Cell-to-cell transmission of HIV-1 from provirus-activated cells to resting naïve and memory human primary CD4 T cells is highly efficient and requires CD4 and F-actin but not chemokine receptors [ J Med Virol, 2022, 10.1002/jmv.28005] | PubMed: 35840493 |
Significant role of host sialylated glycans in the infection and spread of severe acute respiratory syndrome coronavirus 2 [ PLoS Pathog, 2022, 18(6):e1010590] | PubMed: 35700214 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。