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编 号:F387549
分子式:C20H38N6O4
分子量:426.55
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生物活性:
Leupeptin is a broad-spectrum, membrane-permeable protease inhibitor. Leupeptin potently inhibits serine, cysteine and threonine proteases. Leupeptin inhibits Mpro (the main protease of SARS-CoV-2) and also has anti-inflammatory activity.

体内研究:
Leupeptin (0, 9, 18, 36 mg/kg; i.p.; single) is well tolerated by the animals and produces a strong, dose-dependent increase in LC3b-II in both the total tissue extracts and the lysosome and autophagosome-enriched pellet fraction.Animal Model:C57BL/6NCrl male mice (6-8 weeks old, 20-25 g).
Dosage:0, 9, 18, 36 mg/kg
Administration:Intraperitoneal injection; single
Result:Promoted the accumulation of LC3b-II in mouse liver.

体外研究:
Leupeptin (0.06-200 μM; 72 h) 显著抑制 Vero 细胞中 SARS-CoV-2 病毒 RNA (vRNA) 的拷贝数。Leupeptin 抑制 Vero 细胞中 SARS-CoV-2 的 RNA 水平,EC50 值为 42.34 μM。Leupeptin 对 Mpro 有一定的抑制活性,其 IC50 值为127.2 μM。Leupeptin 对人类冠状病毒 229E 株的 IC50 值为 0.4 μg/mL (约 1 μM)。
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