Calpeptin

Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID50 of 40 nM for Calpain I in human platelets[1]. Calpeptin is also an inhibitor of cathepsin K.

Product information

CAS Number: 117591-20-5

Molecular Weight: 362.46

Formula: C20H30N2O4

Chemical Name: benzyl N-[(1S)-3-methyl-1-{[(2S)-1-oxohexan-2-yl]carbamoyl}butyl]carbamate

Smiles: CC(C)C[C@H](NC(=O)OCC1C=CC=CC=1)C(=O)N[C@@H](CCCC)C=O

InChiKey: PGGUOGKHUUUWAF-ROUUACIJSA-N

InChi: InChI=1S/C20H30N2O4/c1-4-5-11-17(13-23)21-19(24)18(12-15(2)3)22-20(25)26-14-16-9-7-6-8-10-16/h6-10,13,15,17-18H,4-5,11-12,14H2,1-3H3,(H,21,24)(H,22,25)/t17-,18-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (275.89 mM; Need ultrasonic)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Calpeptin (0-100 nM, 24 hours) treatment suppresses the proliferation of both WI38 VA13 and IMR90 cells in a dose-dependent manner. Calpeptin (1000 pg/ml, 24 hours) inhibits IL-6-induced cell proliferation of lung fibroblasts.

In Vivo:

Calpeptin with Bleo (0.04 mg/mouse, i.p., 3 times weekly, 28 days) administration significantly inhibits the collagen deposition and increases of calpain activity in the NSC-125066 treated mouse lung tissues.

References:

1. Tsujinaka T, et al. Synthesis of a new cell penetrating calpain inhibitor (calpeptin). Biochem Biophys Res Commun. 1988 Jun 30;153(3):1201-8.
2. Catalano JG, et al. Design of small molecule ketoamide-based inhibitors of cathepsin K. Bioorg Med Chem Lett. 2004 Feb 9;14(3):719-22.
3. Tabata C, et al. The calpain inhibitor calpeptin prevents pulmonary fibrosis in mice. Clin Exp Immunol. 2010 Dec;162(3):560-7.

Products are for research use only. Not for human use.