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Related CAS#:
24365-47-7 55123-66-5
103476-89-7 24125-28-8
24365-46-6 24125-16-4
147385-61-3

55123-66-5

55123-66-5 structure
55123-66-5 structure
  • Name: Leupeptin
  • Chemical Name: leupeptin hemisulfate monohydrate
  • CAS Number: 55123-66-5
  • Molecular Formula: C40H78N12O12S
  • Molecular Weight: 951.18600
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease Cathepsin
  • Create Date: 2016-04-21 06:50:12
  • Modify Date: 2024-01-03 13:50:54
  • 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].
Name leupeptin hemisulfate monohydrate
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].
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

[1]. Fu L, et al. Mechanism of Microbial Metabolite Leupeptin in the Treatment of COVID-19 by Traditional Chinese Medicine Herbs. mBio. 2021 Oct 26;12(5):e0222021.  

[2]. Haspel J, et al. Characterization of macroautophagic flux in vivo using a leupeptin-based assay. Autophagy. 2011 Jun;7(6):629-42.  

[3]. Aoyagi T, et al. Biological activities of leupeptins. J Antibiot (Tokyo). 1969 Nov;22(11):558-68.

Molecular Formula C40H78N12O12S
Molecular Weight 951.18600
Exact Mass 950.55800
PSA 415.52000
LogP 5.18540

CHEMICAL IDENTIFICATION

RTECS NUMBER :
YV4205100
CHEMICAL NAME :
Valeramide, 2-(2-acetamido-4-methylvaleramido)-N-(1-formyl-4-guan idinobutyl)-4-methyl- (S)-
CAS REGISTRY NUMBER :
55123-66-5
LAST UPDATED :
198910
DATA ITEMS CITED :
1
MOLECULAR FORMULA :
C20-H38-N6-O4
MOLECULAR WEIGHT :
426.64
WISWESSER LINE NOTATION :
MUYZM3YVHMVY1Y1&1&MVYMV1&1Y1&1 S-

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
57600 mg/kg/69W-C
TOXIC EFFECTS :
Tumorigenic - neoplastic by RTECS criteria Lungs, Thorax, or Respiration - tumors Liver - tumors
REFERENCE :
GANNA2 Gann. Japanese Journal of Cancer Research. (Tokyo, Japan) V.1-75, 1907-84. For publisher information, see JJCREP. Volume(issue)/page/year: 71,913,1980

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