calpeptin

Cas No.:	117591-20-5
Chemical Name:	Carbamic acid,N-[(1S)-1-[[[(1S)-1-formylpentyl]amino]carbonyl]-3-methylbutyl]-, phenylmethylester
Synonyms:	Carbamic acid,N-[(1S)-1-[[[(1S)-1-formylpentyl]amino]carbonyl]-3-methylbutyl]-, phenylmethylester;CALPEPTIN;Calpeptin,N-Benzyloxycarbonyl-L-leucylnorleucinal;Carbamic acid,N-[(1S)-1-[[[(1S)-1-formylpentyl]amino]carbonyl]-3-methylbutyl]-, phenylmethyles...;BENZYLOXYCARBONYLDIPEPTIDYL ALDEHYDE;BENZYLOXYCARBONYLLEUCYL-NORLEUCINAL;CalpeptinN-Benzyloxycarbonyl-L-leucyl-norleucinal;N-benzyloxycarbonyl-L-leucyl-L-norleucinal;N-Benzyloxycarbonyl-L-leucylnorieucinal Z-Leu-Nle-CHO;N-BENZYLOXYCARBONYL-L-LEUCYLNORLEUCINAL;N-CBZ-L-LEUCYL-NORLEUCINAL;Z-LEU-NLE-CHO;Z-Leu-Nle-H;Z-LEU-NLE-OH;Z-LEU-NORLEUCINAL;N-Benzyloxycarbonyl-L-leucylnorieucinal;N-[N-[(Phenylmethoxy)carbonyl]-L-leucyl]-L-norleucinal;Calpeptin,95%
SMILES:	O=C(OCC1=CC=CC=C1)N[C@H](C(N[C@H](C=O)CCCC)=O)CC(C)C
Formula:	C20H30N2O4
M.Wt:	362.46300
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	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[2].
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 bleomycintreatedmouse lung tissues[3]. Animal Model: C57BL/6 female mice (Eight-week-old)[3]. Dosage: 0.04 mg/mouse. Administration: Intraperitoneally three times weekly for 28 days (together with Bleo). Result: Inhibited the collagen deposition and increase of calpain activity in the bleomycintreatedmouse lung tissues.
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[3]. Cell Proliferation Assay[3] Cell Line: WI38 VA13 and IMR90 cells Concentration: 0-100 nM Incubation Time: 24 hours Result: Suppressed the proliferation in a dose-dependent manner.
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.