Name | leupeptin hemisulfate monohydrate |
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Synonyms |
l-valeramide
acetyl-Leu-Leu-Arg-al 6-O-D-Glucopyranosyl-D-glucopyranose Ac-Leu-Leu-Arg-aldehyde . sulfate 6-O-B-D-GLUCOPYRANOSYL-D-GLUCOPYRANOSE Gentibiose Ac-Leu-Leu-Arg-H N-acetyl-Leu-Leu-argininal AC-LEU-LEU-ARGINAL 1/2H2SO4 H2O |
Description | 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[1][2][3]. |
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Related Catalog | |
Target |
Cathepsin B, Cathepsin H, Cathepsin L, Ser/Thr Protease, Mpro[1][2][3]. |
In Vitro | 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[1] 。Leupeptin 抑制 Vero 细胞中 SARS-CoV-2 的 RNA 水平,EC50 值为 42.34 µM[1] 。Leupeptin 对 Mpro 有一定的抑制活性,其 IC50 值为127.2 µM[1] 。Leupeptin 对人类冠状病毒 229E 株的 IC50 值为 0.4 µg/mL (约 1 µM)[1]。 RT-PCR[1] Cell Line: Vero cells Concentration: 0.06-200 µM Incubation Time: 72 h Result: Significantly decreased copy numbers of SARS-CoV-2 viral RNA (vRNA). |
In Vivo | Leupeptin (0, 9, 18, 36 mg/kg; i.p.; single) 具有很好的动物耐受性,并在总组织提取物、溶酶体以及富含自噬体的颗粒部分以剂量依赖的方式显著诱导 LC3b-II 的增加[2]。 Animal Model: C57BL/6NCrl male mice (6-8 weeks old, 20-25 g)[1]. Dosage: 0, 9, 18, 36 mg/kg Administration: Intraperitoneal injection; single Result: Promoted the accumulation of LC3b-II in mouse liver. |
References |
[3]. Aoyagi T, et al. Biological activities of leupeptins. J Antibiot (Tokyo). 1969 Nov;22(11):558-68. |
Molecular Formula | C40H78N12O12S |
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Molecular Weight | 951.18600 |
Exact Mass | 950.55800 |
PSA | 415.52000 |
LogP | 5.18540 |
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATAACUTE TOXICITY DATA
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