3-[7-(2,4-DIMETHOXYPHENYL)-2,3,6,7-TETRAHYDRO-1,4-THIAZEPIN-5-YL]-4-HYDROXY-6-METHYL-2H-PYRAN-2-ONE
3-[7-(2,4-DIMETHOXYPHENYL)-2,3,6,7-TETRAHYDRO-1,4-THIAZEPIN-5-YL]-4-HYDROXY-6-METHYL-2H-PYRAN-2-ONE Basic information
- Product Name:
- 3-[7-(2,4-DIMETHOXYPHENYL)-2,3,6,7-TETRAHYDRO-1,4-THIAZEPIN-5-YL]-4-HYDROXY-6-METHYL-2H-PYRAN-2-ONE
- Synonyms:
-
- 3-[7-(2,4-DIMETHOXYPHENYL)-2,3,6,7-TETRAHYDRO-1,4-THIAZEPIN-5-YL]-4-HYDROXY-6-METHYL-2H-PYRAN-2-ONE
- KF 38789
- 2H-Pyran-2-one, 3-[7-(2,4-dimethoxyphenyl)-2,3,6,7-tetrahydro-1,4-thiazepin-5-yl]-4-hydroxy-6-methyl-
- inhibit,Inhibitor,PSGL-1,Cell adhesion,P-selectin Inhibitor,KF-38789,KF38789,Inflammation
- CAS:
- 257292-29-8
- MF:
- C19H21NO5S
- MW:
- 375.44
- Mol File:
- 257292-29-8.mol
3-[7-(2,4-DIMETHOXYPHENYL)-2,3,6,7-TETRAHYDRO-1,4-THIAZEPIN-5-YL]-4-HYDROXY-6-METHYL-2H-PYRAN-2-ONE Chemical Properties
- storage temp.
- Desiccate at +4°C
- solubility
- <37.54mg/ml in DMSO
- form
- Solid
- color
- Light yellow to yellow
3-[7-(2,4-DIMETHOXYPHENYL)-2,3,6,7-TETRAHYDRO-1,4-THIAZEPIN-5-YL]-4-HYDROXY-6-METHYL-2H-PYRAN-2-ONE Usage And Synthesis
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-ONESupplier
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