Uses
KF 38789 inhibits the binding of U937 cells to immobilized P-selectin IgG chimeric protein (P-selectin-Ig) with an IC50 value of 1.97 μM.
Definition
ChEBI: 3-[7-(2,4-dimethoxyphenyl)-1,4-thiazepan-5-ylidene]-6-methylpyran-2,4-dione is a dimethoxybenzene.
Biological Activity
Selective inhibitor of P-selectin-mediated cell adhesion (IC 50 = 1.97 μ M) that displays no effects on L-selectin- and E-selectin-mediated adhesion. Blocks P-selectin-mediated binding in vitro and leukocyte accumulation in vivo .
in vivo
KF38789 can block P-selectin-mediated binding in vitro and leukocyte accumulation in vivo[1].
Intraperitoneal injection of the P-selectin inhibitor KF38789 (daily intraperitoneal injection of 10mg/kg for 12 days) significantly reduces mechanical allodynia in the facial carrageenan-injected mice[3].
| Animal Model: | BALB/c mice[1] |
| Dosage: | 1 mg/kg |
| Administration: | Intravenously administrated |
| Result: | Significantly reduced leukocyte accumulation.
|
| Animal Model: | Twenty-four adult male C57BL/6J (B6) mice, about 6-8 weeks of age and weighing approximately 20-30 g[3] |
| Dosage: | 10 mg/kg, 1 mg/kg, 0.1 mg/kg, 0.01 mg/kg or 0.001 mg/kg |
| Administration: | Intraperitoneal injection daily for 12 days |
| Result: | Significantly reduced mechanical allodynia in the facial carrageenan-injected mice.
|
storage
Desiccate at +4°C
![3-[7-(2,4-Dimethoxyphenyl)-2,3,6,7-tetrahydro-1,4-thiazepin-5-yl]-4-hydroxy-6-methyl-2H-pyran-2-one Structure](https://www.chemicalbook.com/CAS/GIF/257292-29-8.gif)
