Lopinavir (ABT-378)

製品コードS1380 バッチS138001

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) は、セル・フリー・アッセイで Ki が 1.3 pM の強力な HIV Protease 阻害剤です。
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 also suppresses HIV protease activity in the absence and presence of 50% HS with EC50 of 17 nM and 102 nM, respectively, in MT4 cells. This compound is converted to several metabolites in an NADPH-dependent manner in liver microsomes with the primary metabolites M-3 and M-4. It is a potent inhibitor of Rh123 efflux in Caco-2 monolayers with IC50 of 1.7 mM. Its exposure (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. It inhibits subtype C clone C6 with IC50 of 9.4 nM. Additionally, 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.
in vivo Lopinavir (ABT-378) (10 mg/kg, orally) results in Cmax of 0.8 μg/mL and oral bioavailability of 25% in rats.

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 by Lopinavir (ABT-378) 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

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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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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