氟舒胺
氟舒胺 性质
| 熔点 | 156 °C(Solv: ethanol (64-17-5)) |
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| 沸点 | 446.9±55.0 °C(Predicted) |
| 密度 | 1.506±0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 6.95±0.20(Predicted) |
氟舒胺 用途与合成方法
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COX-2
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Flosulide (1 nM-100 μM) causes a concentration-dependent and finally complete inhibition of PGE2 production in the OSC-2 cell line, but with no effect on PG formation in the OSC-1 cells. Flosulide completely suppresses mitotic activity of OSC-2 cells, whereas mitotic activity of OSC-1 cells remain unchanged.
In normovolemic rats, flosulide increases renal plasma flow (RPF) and and glomerular filtration rate (GFR). In hypovolemic rats, flosulide (5-25 mg/kg) reduces RPF and GFR. Flosulide at 5 mg/kg reduces 6-keto-PGF1alpha whereas at 25 mg/kg and after indomethacin at 10 mg/kg a fall in 6-keto-PGF1alpha and TXB2 appeares. Flosulide (0.75 mg/day) significantly reduces proteinuria as compared to aspirin treatment. Plasma protein and albumin levels are significantly lower in the aspirin-treated group than in flosulide-treated rats.
