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.

• 동의어(들): Calpain Inhibitor XI, Z-L-Abu-CONH(CH₂)₃-morpholine
• 실험식(Hill 표기법): C₂₆H₄₀N₄O₆
• CAS Number: 145731-49-3
• Molecular Weight: 504.62
• UNSPSC 코드: 12352200

속성

• Quality Level: 100
• 분석: ≥95% (HPLC)
• 형태: solid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; desiccated (hygroscopic)
• 색상: white to off-white
• solubility: DMSO: 5 mg/mL
• 배송 상태: ambient
• 저장 온도: 2-8°C

설명

일반 설명

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.

생화학적/생리학적 작용

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

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

서열

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

물리적 형태

Supplied as a trifluoroacetate salt.

재구성

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

기타 정보

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.

법적 정보

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

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable