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FK706

Catalog No. T15285   CAS 144055-55-0

FK706 is a slow-binding and competitive human neutrophil elastase inhibitor (IC50: 83 nM; Ki: 4.2 nM). FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase (IC50s: 22 nM and 100 nM, respectively). FK706 has an anti-inflammatory effect.

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FK706 Chemical Structure
FK706, CAS 144055-55-0
Pack Size Availability Price/USD Quantity
25 mg 8-10 weeks $ 1,530.00
50 mg 8-10 weeks $ 1,990.00
100 mg 8-10 weeks $ 3,190.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description FK706 is a slow-binding and competitive human neutrophil elastase inhibitor (IC50: 83 nM; Ki: 4.2 nM). FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase (IC50s: 22 nM and 100 nM, respectively). FK706 has an anti-inflammatory effect.
Targets&IC50 Neutrophil elastase (human):(ki)4.2 nM, Neutrophil elastase (human):83 nM, Neutrophil elastase (mouse):22 nM, Pancreatic elastase (porcine):100 nM
In vitro FK706 effectively inhibits the hydrolysis of bovine neck ligament elastin (2 mg/mL final concentration) by human neutrophil elastase (4 μg/mL final concentration) (IC50: 230 nM) [1]. FK706 blocks the release of inflammatory chemokines, suppresses the expression of IL-8 and MCP-1 mRNA, and suppresses NF-κB activation. FK706 may directly block human lung fibroblasts activation of NF-κB, preventing the expression of inflammatory chemokines during cigarette smoke-induced lung inflammation [2].
In vivo FK706 (10-100 mg/kg; subcutaneous injection; for 1-6 hours; male C57BL mice) treatment obviously inhibits human neutrophil elastase (20 μg/paw)-induced paw edema in mice. It shows a dose-dependent manner (47% inhibition at a dose of 100 mg/kg) [1].
Molecular Weight 593.556
Formula C26H33F3N4NaO7
CAS No. 144055-55-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Shinguh Y, et al. Biochemical and pharmacological characterization of FK706, a novel elastase inhibitor. Eur J Pharmacol. 1997 Oct 15;337(1):63-71. 2. Numanami H, et al. Serine protease inhibitors modulate smoke-induced chemokine release from human lung fibroblasts. Am J Respir Cell Mol Biol. 2003 Nov;29(5):613-9.

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Keywords

FK706 144055-55-0 Proteases/Proteasome Serine Protease FK 706 FK-706 inhibitor inhibit

 

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