UK 356618
| 中文名称 | UK 356618 |
|---|---|
| 中文同义词 | 化合物 T17201 |
| 英文名称 | N1-[(1S)-2,2-Dimethyl-1-[[[(1R)-1-phenylethyl]amino]carbonyl]propyl]-N4-hydroxy-2-[3-(2-methyl[1,1'-biphenyl]-4-yl)propyl]-butanediamine |
| 英文同义词 | N1-[(1S)-2,2-Dimethyl-1-[[[(1R)-1-phenylethyl]amino]carbonyl]propyl]-N4-hydroxy-2-[3-(2-methyl[1,1'-biphenyl]-4-yl)propyl]-butanediamine;(2R)-N1-[(1S)-2,2-DiMethyl-1-[[[(1R)-1-phenylethyl]aMino]carbonyl]propyl]-N4-hydroxy-2-[3-(2-Methyl[1,1'-biphenyl]-4-yl)propyl]butanediaMide;PF-03890101;(2R)-N1-[(1S)-2,2-Dimethyl-1-({[(1R)-1-phenylethyl]amino}carbonyl)propyl]-2-{3-[(3-methyl-4-phenyl)-phenyl]propyl}-(N4-hydroxy)butanediamide;UK 356618 - PF 03890101;UK 356618;Butanediamide, N1-[(1S)-2,2-dimethyl-1-[[[(1R)-1-phenylethyl]amino]carbonyl]propyl]-N4-hydroxy-2-[3-(2-methyl[1,1'-biphenyl]-4-yl)propyl]-, (2R)- |
| CAS号 | 230961-08-7 |
| 分子式 | C34H43N3O4 |
| 分子量 | 557.72 |
| EINECS号 | |
| 相关类别 | Aromatics;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pfizer Compounds;Pharmaceuticals |
| Mol文件 | 230961-08-7.mol |
| 结构式 |  |
UK 356618 性质
| 熔点 | 93-102oC |
|---|---|
| 密度 | 1.124±0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 二甲基亚砜：≥25mg/mL |
| 形态 | 粉末 |
| 酸度系数(pKa) | 9.16±0.20(Predicted) |
| 颜色 | 白色至棕褐色 |
| 旋光性 (optical activity) | [α]/D >+25.0°, c = 0.5 in methanol |
|
MMP-3 5.9 nM (IC 50 ) |
MMP-13 73 nM (IC 50 ) |
MMP-9 0.84 μM (IC 50 ) |
MMP-2 1.79 μM (IC 50 ) |
MMP-14 1.9 μM (IC 50 ) |
MMP-1 51 μM (IC 50 ) |
Inhibition of MMP-3 and selectivity over MMP-2 was remarkably sensitive to the size of the substituent and is clearly optimal for a methyl group (UK 356618, compound 4j). UK 356618 is more widely profiled against other MMPs.
MMP-13 is closely involved in IL-6 or TNF-α increasing tumor metastasis. MMP-13 deficiency abrogate TNF-α effect on lung cancer cell migration. UK 356618 treatment efficiently abolished the effect of TNF-α on cell migration in NCI-H446 cells.
UK 356618 (15 mg/kg; intravenous injection; for 24 h or 7 days; male Wistar rats) treatment at reperfusion significantly reduces MMP3 activity in the brain.
| Animal Model: | Hyperglycemic male Wistar rats injected with middle cerebral artery occlusion (MCAO) |
| Dosage: | 15 mg/kg |
| Administration: | Intravenous injection; for 24 h or 7 days |
| Result: | Significantly reduced MMP3 activity in the brain. |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-107394 | UK 356618 UK 356618 | 230961-08-7 | 1mg | 1700元 |
| 2024/04/30 | HY-107394 | UK 356618 | 10 mM * 1 mLin DMSO | 5610元 |