[CAS NO. 144055-55-0] FK706
PRODUCTS SPECIFICATIONS [144055-55-0]
DESCRIPTION [144055-55-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 592.54 |
| Molecular Formula | C26H32F3N4NaO7 |
| 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 |
Summary
FK706 is a potent, slow-binding and competitive inhibitor of human neutrophil elastase with an IC 50 of 83 nM and a K i of 4.2 nM. FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase with IC 50 s 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
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 115 mg/mL ( 194.08 mM ; Need ultrasonic)
H 2 O : ≥ 100 mg/mL ( 168.76 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.6876 mL | 8.4382 mL | 16.8765 mL |
| 5 mM | 0.3375 mL | 1.6876 mL | 3.3753 mL |
| 10 mM | 0.1688 mL | 0.8438 mL | 1.6876 mL |