Lopinavir (ABT-378)

製品コードS1380 バッチS138004

印刷

化学情報

Chemical Structure Synonyms ABT-378 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C37H48N4O5
分子量 628.8 CAS No. 192725-17-0
Solubility (25°C)* 体外 DMSO 100 mg/mL (159.03 mM)
Ethanol 100 mg/mL (159.03 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
30%PEG400 0.5%Tween80 5%propylene glycol
30.0mg/ml Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O to adjust the volume. to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Lopinavir (ABT-378) is a potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay.
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]

プロトコル(参考用のみ)

キナーゼアッセイ HIV protease inhibition
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

カスタマーフィードバック

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]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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。

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