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
• 実験式（ヒル表記法）: C₂₆H₄₀N₄O₆
• CAS番号: 145731-49-3
• 分子量: 504.62
• MDL番号: MFCD24369059
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• フォーム: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; desiccated (hygroscopic)
• 色: white to off-white
• 溶解性: DMSO: 5 mg/mL
• 輸送温度: ambient
• 保管温度: 2-8°C
• SMILES記法: 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

詳細

詳細

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.

生物化学的／生理学的作用

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

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

シーケンス

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

物理的形状

Supplied as a trifluoroacetate salt.

再構成

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

その他情報

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.

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 1
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable