210755-45-6
基本信息
PF-1626077
2-(4-(4-Fluorophenoxy)phenylsulfonamido)-N-hydroxy-2-methylpropanamide
2-[[[4-(4-Fluorophenoxy)phenyl]sulfonyl]amino]-N-hydroxy-2-methylpropanamide
Propanamide, 2-[[[4-(4-fluorophenoxy)phenyl]sulfonyl]amino]-N-hydroxy-2-methyl-
物理化学性质
| 熔点 | 135-137°C (dec.) |
| 密度 | 1.375±0.06 g/cm3(Predicted) |
| 储存条件 | room temp |
| 溶解度 | 二甲基亚砜：≥20mg/mL |
| 酸度系数(pKa) | 9.33±0.50(Predicted) |
| 形态 | 粉末 |
| 颜色 | 白色至灰白色 |
常见问题列表
|
MMP-2 0.7 nM (IC 50 ) |
MMP-13 0.9 nM (IC 50 ) |
MMP-9 13 nM (IC 50 ) |
MMP-3 16 nM (IC 50 ) |
MMP-1 1170 nM (IC 50 ) |
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. |