324759

Elastase Inhibitor IV

The Elastase Inhibitor IV, also referenced under CAS 127373-66-4, controls the biological activity of Elastase. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.

• Synonym(s): Elastase Inhibitor IV, N-( o-( p-Pivaloyloxybenzene)sulfonylaminobenzoyl)glycine, N-(2-(4-(2,2-Dimethylpropionyloxy)phenylsulfonylamino)benzoyl)aminoacetic acid, N-(o-(p-Pivaloyloxybenzene)sulfonylaminobenzoyl)glycine, N-(2-(4-(2,2-Dimethylpropionyloxy)phenylsulfonylamino)benzoyl)aminoacetic acid
• Empirical Formula (Hill Notation): C₂₀H₂₂N₂O₇S
• CAS Number: 127373-66-4
• Molecular Weight: 434.46
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white to off-white
• solubility: DMSO: 10 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C20H22N2O7S/c1-20(2,3)19(26)29-13-8-10-14(11-9-13)30(27,28)22-16-7-5-4-6-15(16)18(25)21-12-17(23)24/h4-11,22H,12H2,1-3H3,(H,21,25)(H,23,24)
• InChI key: BTGNGJJLZOIYID-UHFFFAOYSA-N

Description

General description

A cell-permeable sulfanilide compound that acts as a potent, substrate-competitive, and highly specific inhibitor of neutrophil elastase (IC₅₀ = 19-49 nM in rat, rabbit, hamster, human, and mouse leukocyte elastase). Displays >100-fold greater selectivity over pancreas elastase (IC₅₀ = 5.6 µM). Does not inhibit trypsin, thrombin, plasmin, kallikrein, chymotrypsin, and cathepsin G even at concentrations as high as 100 µM. Effectively suppresses human neutrophil elastase-induced lung hemorrhage and skin capillary permeability in vivo. Also reported to inhibit mast cell Stat6-protease.

A cell-permeable, potent, substrate-competitive, and highly specific inhibitor of neutrophil elastase (IC₅₀ = 19-49 nM using rat, rabbit, hamster, human, and mouse leukocyte elastase). Displays about 100-fold greater selectivity over pancreatic elastase (IC₅₀ = 5.6 µM) and is inactive against trypsin, thrombin, plasmin, kallikrein, chymotrypsin, and cathepsin G even at concentrations as high as 100 µM. Effectively suppresses human neutrophil elastase-induced lung hemorrhage and skin capillary permeability in vivo. Also reported to inhibit mast cell Stat6-protease.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
Neutrophil elastase

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 19-49 nM in rat, rabbit, hamster, human, and mouse leukocyte elastase

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Suzuki, K., et al. 2003. Biochem. Biophys. Res. Commun.309, 768.
Kawabata, K., et al. 1991. Biochem. Biophys. Res. Commun.177, 814.

Legal Information

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

Safety Information

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