FK706

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].

Product Specifications

CAS Number

[144055-55-0]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Elastase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/fk706.html

Purity

99.16

Solubility

DMSO : 115 mg/mL (ultrasonic) |H2O : ≥ 100 mg/mL

Smiles

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

Molecular Formula

C26H32F3N4NaO7

Molecular Weight

592.54

Precautions

H302, H315, H319, H335

References & Citations

[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.