1. Metabolic Enzyme/Protease
  2. Elastase
  3. FK706

FK706 

Cat. No.: HY-19269
Handling Instructions

FK706 is a potent, slow-binding and competitive inhibitor of human neutrophil elastase with an IC50 of 83 nM and a Ki of 4.2 nM. FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase with IC50s of 22 nM and 100 nM, respectively, and has no inhibitory activity against other serine proteinases such as human pancreatic trypsin, human pancreatic α-chymotrypsin and human leukocyte cathepsin G. FK706 has anti-inflammatory effect.

For research use only. We do not sell to patients.

FK706 Chemical Structure

FK706 Chemical Structure

CAS No. : 144055-55-0

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Description

FK706 is a potent, slow-binding and competitive inhibitor of human neutrophil elastase with an IC50 of 83 nM and a Ki of 4.2 nM. FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase with IC50s of 22 nM and 100 nM, respectively, and has no inhibitory activity against other serine proteinases such as human pancreatic trypsin, human pancreatic α-chymotrypsin and human leukocyte cathepsin G. FK706 has anti-inflammatory effect[1][2].

IC50 & Target

IC50: 83 nM (Human neutrophil elastase), 22 nM (Mouse neutrophil elastase) and 100 nM (Porcine pancreatic elastase)[1];
Ki: 4.2 nM (Human neutrophil elastase)[1]

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) with an IC50 value of 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. It seems possible that FK706 may directly blocks human lung fibroblasts activation of NF-κB, preventing 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 significantly suppresses human neutrophil elastase (20 μg/paw)-induced paw edema in mice in a dose-dependent manner (47% inhibition at a dose of 100 mg/kg)[1].

Animal Model: Male C57BL mice (6 weeks old) injected with human neutrophil elastase[1]
Dosage: 10 mg/kg, 32 mg/kg, 100 mg/kg
Administration: Subcutaneous injection; for 1 hour, 2 hours, 4 hours, 6 hours
Result: Significantly suppressed human neutrophil elastase-induced paw edema in mice in a dose-dependent manner.
Molecular Weight

592.54

Formula

C₂₆H₃₂F₃N₄NaO₇

CAS No.

144055-55-0

SMILES

O=C(NC(C(C)C)C(C(F)(F)F)=O)[[email protected]]1N(C([[email protected]](C(C)C)NC(C2=CC=C(C(NCC(O[Na])=O)=O)C=C2)=O)=O)CCC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

FK706FK 706FK-706ElastaseWater-solubleslow-bindingsynthetichumanserineproteasesporcineinflammatorydisordersInhibitorinhibitorinhibit

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FK706
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