Lopinavir (ABT-378)

製品コードS1380 バッチS138003

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 126 mg/mL (200.38 mM)
Ethanol 126 mg/mL (200.38 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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 (ABT-378) binds to mutant HIV protease (V82A, V82F and V82T) with Ki of 4.9 pM, 3.7 pM and 3.6 pM, respectively. It inhibits 93% of wild-type HIV protease activity at 0.5 nM, and 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] This compound is converted to several metabolites in an NADPH-dependent manner in liver microsomes with the primary metabolites M-3 and M-4. [2] It is a potent inhibitor of Rh123 efflux in Caco-2 monolayers with IC50 of 1.7 mM. Exposure to it (72 hours) in LS 180V cells reduces the content of intracellular Rh123, and it induces P-glycoprotein immunoreactive protein and messenger RNA levels in LS 180V cells. [3] It inhibits subtype C clone C6 with IC50 of 9.4 nM. [4] It inhibits CYP3A with IC50 of 7.3 mM in human liver microsomes, while producing negligible or weak inhibition of human CYP1A2, 2B6, 2C9, 2C19 and 2D6. [5]
in vivo In rats, Lopinavir (ABT-378) (10 mg/kg, orally) results in a Cmax of 0.8 μg/mL and oral bioavailability of 25%. [1]

プロトコル(参考用のみ)

キナーゼアッセイ HIV protease inhibition
Lopinavir (ABT-378) inhibits the activity of recombinant wild-type and mutant HIV type 1 (HIV-1) proteases, as 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 of this compound is estimated by nonlinear regression using 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

参考

  • https://pubmed.ncbi.nlm.nih.gov/9835517/
  • https://pubmed.ncbi.nlm.nih.gov/9884314/
  • https://pubmed.ncbi.nlm.nih.gov/12700464/
  • https://pubmed.ncbi.nlm.nih.gov/12936979/
  • https://pubmed.ncbi.nlm.nih.gov/12724045/

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]

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Reactivated endogenous retroviruses promote protein aggregate spreading [ Nat Commun, 2023, 14(1):5034] PubMed: 37596282
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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

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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