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编 号:F270559
分子式:C16H17FN2O5S
分子量:368.38
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生物活性:
CP-471474 is an orally active and pan MMP inhibitor, with IC50 values of 1170 nM (MMP-1), 0.7 nM (MMP-2), 16 nM (MMP-3), 13 nM (MMP-9) and 0.9 nM (MMP-13), respectively.

体内研究:
CP-471474 plasma levels following subcutaneous injection are 2,020 ng/mL (1 h postdose) to 160 ng/mL (6 h postdose).CP-471,474 significantly reduces both the extent and severity of inflammation at 2 months. At 4 months, a spontaneous reduction of the inflammatory response is observed in both treated and untreated animals, and consequently no difference is observed between both.CP-471474 significantly decreases the destructive lesions mainly at 2 months and also at 4 months.Animal Model:Guinea pigs weighing 400 to 450 g (COPD).
Dosage:20 mg/kg (also supplemented daily by the diet (200 mg/200 g powdered chow)).
Administration:Subcutaneously (in 20% ethanol/80% polyethylene glycol), once a day during the entire course.
Result:Lungs derived from smoking animals treated with the compound demonstrated a statistically significant reduction in the destructive lesions.Showed an increase of both pro–MMP-9 and its active form (lanes 5 to 8) as compared with control animals.
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