Calpain Inhibitor VI,5MG,208745-5MGCN,Sigma

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订货号 0BW0943
品牌型号 Sigma 208745-5MGCN
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最小订货量 1件
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产品介绍 Product Description

General description

A cell-permeable peptide aldehyde that acts as a potent and reversible inhibitor of calpain (IC50 = 7.5 nM for µ-calpain and 78 nM for m-calpain). Also potently inhibits cathepsin B (IC50 = 15 nM) and cathepsin L (IC50 = 1.6 nM). Reduces βFGF-induced angiogenesis in rat cornea and prevents selenite cataract formation in rats. Reduces A23187-induced nuclear opacity and proteolysis of crystallins and α-spectrin in cultured rat lenses.
A potent, cell-permeable, reversible inhibitor of calpain (IC50 = 7.5 nM for µ-calpain and 78 nM for m-calpain). Also potently inhibits cathepsin B (IC50 = 15 nM) and L (IC50 = 1.6 nM). Reduces bFGF-induced angiogenesis in rat cornea and prevents selenite cataract formation. Reduces A23187-induced nuclear opacity and proteolysis of crystallins and α-spectrin in cultured lenses.


Biochem/physiol Actions

Cell permeable: yes
Primary Target
µ-calpain
Product does not compete with ATP.
Reversible: yes
Target IC50: 7.5 nM for µ-calpain and 78 nM for m-calpain; 15 nM and 1.6 nM against cathepsin B and L, respectively


Packaging

Packaged under inert gas


Preparation Note

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


Other Notes

4-Fluorophenylsulfonyl-Val-Leu-CHO
Inoue, J., et al. 2003. J. Med. Chem.46, 868.
Tamada, Y., et al. 2001. Curr. Eye Res.22, 280.
Mathur, P., et al. 2000. Curr. Eye Res.21, 926.
Nath, R., et al. 2000. Biochem. Biophys. Res. Commun.274, 16.
Tamada, Y., et al. 2000. J. Ocul. Pharmacol. Ther.16, 271.
Fukiage, C., et al. 1998. Curr. Eye Res.17, 623.
Fukiage, C., et al. 1997. Biochim. Biophys. Acta 1361, 304.


Legal Information

Sold under license of U.S. Patent 6,551,999
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany


Disclaimer

Toxicity: Standard Handling (A)


技术参数 Specifications
Quality Level100
assay≥97% (HPLC)
formlyophilized solid
manufacturer/tradenameCalbiochem®
storage conditionOK to freeze,protect from light
color white
solubilityDMSO: 5 mg/mL
shipped inambient
storage temp.−20°C
SMILES stringFc1ccc(cc1)[S](=O)(=O)NC(C(C)C)C(=O)NC(CC(C)C)C=O
InChI1S/C17H25FN2O4S/c1-11(2)9-14(10-21)19-17(22)16(12(3)4)20-25(23,24)15-7-5-13(18)6-8-15/h5-8,10-12,14,16,20H,9H2,1-4H3,(H,19,22)
InChI keyWSJWUIDLGZAXID-UHFFFAOYSA-N
长度(mm)
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高度(mm)
重量(kg)
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