208743

Calpain Inhibitor XI

The Calpain Inhibitor XI, also referenced under CAS 145731-49-3, controls the biological activity of Calpain. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.

• Sinonimo/i: Calpain Inhibitor XI, Z-L-Abu-CONH(CH₂)₃-morpholine
• Formula empirica (notazione di Hill): C₂₆H₄₀N₄O₆
• Numero CAS: 145731-49-3
• Peso molecolare: 504.62
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥95% (HPLC)
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; desiccated (hygroscopic)
• Colore: white to off-white
• Solubilità: DMSO: 5 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: 2-8°C

Descrizione

Descrizione generale

A cell-permeable dipeptidyl α-ketoamide that acts as a potent, highly selective, reversible, and active site inhibitor of calpain-1 and -2 (K_i = 140 nM and 41 nM, respectively). Weakly inhibits cathepsin B (K_i = 6.9 µM). Reported to have a neuroprotective role in the central nervous system following focal ischemia. Also protects against virus-induced apoptotic myocardial injury in mice.

A cell-permeable dipeptidyl a-ketoamide that acts as a potent, highly selective, reversible, active site inhibitor of calpain-1 (K_i = 140 nM) and calpain-2 (K_i = 41 nM). Weakly inhibits cathepsin B (K_i = 6.9 µM). Shown to inhibit calpain-m-mediated degradation of neurofilament protein (NFP) (IC₅₀ = 600 nM). Also shown to exhibit neuroprotective effects in the central nervous system following focal ischemia. Reported to protect against reovirus-induced myocarditis in mice.

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
calpain 1, calpain 2

Product does not compete with ATP.

Reversible: yes

Target K_i: 140 nM and 41 nM, against calpain-1 and -2, respectively

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Sequenza

Z-Leu-Abu-CONH(CH₂)₃-morpholine (Abu = α-aminobutyric acid)

Stato fisico

Supplied as a trifluoroacetate salt.

Ricostituzione

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Altre note

Blomgren, K., et al. 2001. J. Biol. Chem.276, 10191.
DeBiasi, R.L., et al. 2001. J. Virol.75, 351.
Saatman, K.E., et al. 2000. J. Cereb. Blood Flow Metab.20, 66.
Stelmasiak, Z., et al. 2000. Med. Sci. Monit.6, 426.
Blomgren, K., et al. 1999. J. Biol. Chem.274, 14046.
James, T., et al. 1998. J. Neurosci. Res.51, 218.
Li, Z., et al. 1996. J. Med. Chem.39, 4089.
Saatman, K.E, et al. 1996. Proc. Natl. Acad. Sci. USA93, 3428.
Bartus, R.T., et al. 1995. Neurol. Res.17, 249.
Bartus, R.T., et al. 1994. Stroke25, 2265.

Note legali

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 1
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable