Leupeptin

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Leupeptin

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

55123-66-5

Leupeptin 是一种广谱的、具有细胞膜渗透性的蛋白酶抑制剂。 Leupeptin 能有效抑制丝氨酸、半胱氨酸和苏氨酸蛋白酶。 Leupeptin 能抑制M^pro(SARS-CoV-2的主要蛋白酶)，还具有抗炎活性。

生物活性

Leupeptin is a broad-spectrum, membrane-permeableprotease inhibitor. Leupeptin potently inhibitsserine,cysteineandthreonine proteases. Leupeptin inhibitsM^pro(the mainproteaseofSARS-CoV-2) and also has anti-inflammatory activity^[1]^[2]^[3].

IC₅₀& Target

Cathepsin B, Cathepsin H, Cathepsin L, Ser/Thr Protease, Mpro^[1]^[2]^[3].

体外研究
(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 M^pro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).

体内研究
(In Vivo)

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^[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.

分子量

426.55

Formula

C₂₀H₃₈N₆O₄

CAS 号

55123-66-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.