CP-471474 是一个口服有效的、广泛的MMP抑制剂，IC50值分别为1170 nM (MMP-1)、0.7 nM (MMP-2)、16 nM (MMP-3)、13 nM (MMP-9) 和 0.9 nM (MMP-13)。
| 生物活性 | CP-471474 is an orally active and panMMPinhibitor, withIC50values 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[1][2]. |
| IC50& Target[1] | MMP-2 0.7 nM (IC50) | MMP-13 0.9 nM (IC50) | MMP-9 13 nM (IC50) | MMP-3 16 nM (IC50) | MMP-1 1170 nM (IC50) |
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体内研究
(In Vivo) | CP-471474 plasma levels following subcutaneous injection are 2,020 ng/mL (1 h postdose) to 160 ng/mL (6 h postdose)[2].
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[2].
CP-471474 significantly decreases the destructive lesions mainly at 2 months and also at 4 months[2].
| Animal Model: | Guinea pigs weighing 400 to 450 g (COPD)[2]. | | 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
