| Chemical Properties | Back Directory | [storage temp. ]
4°C, protect from light | [solubility ]
DMSO: 115 mg/mL (194.08 mM) | [form ]
Solid | [color ]
White to off-white | [Cosmetics Ingredients Functions]
SKIN CONDITIONING |
| Hazard Information | Back Directory | [Uses]
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]. | [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.
|
| [References]
[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. DOI:10.1016/s0014-2999(97)01284-3
[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. DOI:10.1165/rcmb.2003-0113OC |
|
| Company Name: |
MedChemExpress
|
| Tel: |
021-58955995 |
| Website: |
www.medchemexpress.com |
|