2-[[[4-(4-氟苯氧基)苯基]磺酰基]氨基] -N-羟基-2-甲基丙酰胺
| 中文名称 | 2-[[[4-(4-氟苯氧基)苯基]磺酰基]氨基] -N-羟基-2-甲基丙酰胺 |
|---|---|
| 中文同义词 | 2-[[[4-(4-氟苯氧基)苯基]磺酰基]氨基] -N-羟基-2-甲基丙酰胺;化合物 T22685;化合物 CP-471474 |
| 英文名称 | CP 471,474 |
| 英文同义词 | PF-1626077;CP 471,474;2-[[[4-(4-Fluorophenoxy)phenyl]sulfonyl]amino]-N-hydroxy-2-methylpropanamide;2-(4-(4-Fluorophenoxy)phenylsulfonamido)-N-hydroxy-2-methylpropanamide;Propanamide, 2-[[[4-(4-fluorophenoxy)phenyl]sulfonyl]amino]-N-hydroxy-2-methyl- |
| CAS号 | 210755-45-6 |
| 分子式 | C16H17FN2O5S |
| 分子量 | 368.38 |
| EINECS号 | |
| 相关类别 | Amines;Aromatics;Inhibitors;Intermediates & Fine Chemicals;Pfizer Compounds;Pharmaceuticals;Sulfur & Selenium Compounds;Heterocycles |
| Mol文件 | 210755-45-6.mol |
| 结构式 | ![2-[[[4-(4-氟苯氧基)苯基]磺酰基]氨基] -N-羟基-2-甲基丙酰胺 结构式](CAS/GIF/210755-45-6.gif) |
2-[[[4-(4-氟苯氧基)苯基]磺酰基]氨基] -N-羟基-2-甲基丙酰胺 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 | 白色至类白色 |
| InChI | 1S/C16H17FN2O5S/c1-16(2,15(20)18-21)19-25(22,23)14-9-7-13(8-10-14)24-12-5-3-11(17)4-6-12/h3-10,19,21H,1-2H3,(H,18,20) |
| InChIKey | QCOQJYRPDUMCNP-UHFFFAOYSA-N |
| SMILES | CC(C)(NS(=O)(=O)c1ccc(Oc2ccc(F)cc2)cc1)C(=O)NO |
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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. |