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.
別名:
Calpain Inhibitor XI, Z-L-Abu-CONH(CH2)3-morpholine
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この商品について
実験式（ヒル表記法）:
C26H40N4O6
CAS番号:
分子量:
504.62
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
solid
Storage condition:
OK to freeze, desiccated (hygroscopic)
Quality Segment
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated (hygroscopic)
color
white to off-white
solubility
DMSO: 5 mg/mL
shipped in
ambient
storage temp.
2-8°C
SMILES string
N2(CCOCC2)CCCNC(=O)C(=O)C(NC(=O)C(NC(=O)OCc1ccccc1)CC(C)C)CC
InChI
1S/C26H40N4O6/c1-4-21(23(31)25(33)27-11-8-12-30-13-15-35-16-14-30)28-24(32)22(17-19(2)3)29-26(34)36-18-20-9-6-5-7-10-20/h5-7,9-10,19,21-22H,4,8,11-18H2,1-3H3,(H,27,33)(H,28,32)(H,29,34)
InChI key
TZVQRMYLYQNBOA-UHFFFAOYSA-N
General description
A cell-permeable dipeptidyl α-ketoamide that acts as a potent, highly selective, reversible, and active site inhibitor of calpain-1 and -2 (Ki = 140 nM and 41 nM, respectively). Weakly inhibits cathepsin B (Ki = 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 (Ki = 140 nM) and calpain-2 (Ki = 41 nM). Weakly inhibits cathepsin B (Ki = 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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
calpain 1, calpain 2
calpain 1, calpain 2
Product does not compete with ATP.
Reversible: yes
Target Ki: 140 nM and 41 nM, against calpain-1 and -2, respectively
Packaging
Packaged under inert gas
Physical form
Supplied as a trifluoroacetate salt.
Preparation Note
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
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.
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.
Z-Leu-Abu-CONH(CH₂)₃-morpholine (Abu = α-aminobutyric acid)
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
保管分類
11 - Combustible Solids
一体何が起きているの？
WGK 1
引火点 (F)
Not applicable
引火点（°C）
Not applicable