CALPEPTIN

Bezeichnung:CALPEPTIN

CAS-Nr117591-20-5

Englisch Name:CALPEPTIN

CBNumberCB4713515

SummenformelC20H30N2O4

Molgewicht362.46

MOL-Datei117591-20-5.mol

CALPEPTIN physikalisch-chemischer Eigenschaften

Schmelzpunkt	60-75 °C
Siedepunkt	494.07°C (rough estimate)
Dichte	1.1667 (rough estimate)
Brechungsindex	1.6800 (estimate)
storage temp.	-20°C
Löslichkeit	Soluble in DMSO at 15mg/ml
Aggregatzustand	White to off-white solid
pka	11.14±0.46(Predicted)
Farbe	white to beige
InChIKey	PGGUOGKHUUUWAF-ROUUACIJSA-N
CAS Datenbank	117591-20-5(CAS DataBase Reference)

Sicherheit

S-Sätze:	24/25
WGK Germany	3
HS Code	29242990

Gefahreninformationscode (GHS)

CALPEPTIN Chemische Eigenschaften,Einsatz,Produktion Methoden

S-Sätze Betriebsanweisung:
S24/25:Berührung mit den Augen und der Haut vermeiden.
Chemische Eigenschaften
white to off-white powder
Verwenden
Calpeptin is used to to inhibit the activities of cathepsin L and calpain-1. Calpeptin blocked the expression of aspartyl protease cathepsin D, amyloid precursor protein, and calparin. It acts as an inhibitor of the Ca2+-dependent protease, calpain. Prevents collagen- and thrombin-induced platelet aggregation, probably by blocking calpain induced phospholipase C and thromboxane synthase activation. Potent cathepsin L inhibitor. It is shown to preferentially inhibit a subset of protein-tyrosine phosphatases.
Definition
ChEBI: Calpeptin is an amino acid amide.
Allgemeine Beschreibung
Calpeptin (Z-Leu-nLeu-H) is a cell permeable, peptide aldehyde inhibitor. It is more sensitive to calpain I compared to other inhibitors, such as Z-Leu-Met-H and leupeptin. Calpeptin stimulates neurite elongation in differentiating pheochromocytoma (PC12) cells. Calpeptin decreases microgliosis, astrogliosis, axonal damage and neuron and oligodendrocyte death in experimental autoimmune encephalomyelitis (EAE) spinal cord. Therefore, it can be considered as a potent therapeutic for treating EAE and multiple sclerosis (MS).
Biologische Aktivität
Potent, cell-permeable inhibitor of the Ca 2+ -dependent protease, calpain. Prevents collagen- and thrombin-induced platelet aggregation, probably by blocking calpain induced phospholipase C and thromboxane synthase activation. Potent cathepsin L inhibitor. Recently shown to preferentially inhibit a subset of protein-tyrosine phosphatases.
Biochem/physiol Actions
Calpeptin is a rho kinase activator and an inhibitor of calpains, a family of calcium-dependent cysteine proteases involved in apoptosis, long-term potentiation in neurons, and cell cycle progression.
in vitro
calpeptin reduced production of tgf-b1, il-6, angiopoietin-1 and collagen synthesis from lung fibroblasts. calpeptin also reduced both angiopoietin-1-dependent migration and il-6-dependent proliferation of the cells, which could be the underlying mechanism of the preventive effect of calpeptin on pulmonary fibrosis [1].
in vivo
the preventive effect of calpeptin has been examined on bleomycin-induced pulmonary fibrosis in mice. histological examinations and quantitative measurements of related proteins in bleomycin-treated mouse lung tissues with or without calpeptin were performed. calpeptin histologically ameliorated bleomycininduced pulmonary fibrosis in mice. results showed that calpeptin decreased the expression of il-6, tgf-b1, angiopoietin-1 and collagen type ia1 mrna in mouse lung tissues [1].
IC 50
5 nm for human calpain 1
Lager
Desiccate at +4°C
Einzelnachweise
[1] tabata c,tabata r,nakano t. the calpain inhibitor calpeptin prevents bleomycin-induced pulmonary fibrosis in mice. clin exp immunol.2010 dec;162(3):560-7.

CALPEPTIN Upstream-Materialien And Downstream Produkte

CALPEPTIN Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

117591-20-5, CALPEPTIN Verwandte Suche:

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