(R)-3-((S)-1-((S)-2-methoxy-1-phenylethylamino)-3,3-dimethyl-1-oxobutan-2-ylcarbamoyl)-6-(2-methylbiphenyl-4-yl)hexanoic acid
(R)-3-((S)-1-((S)-2-methoxy-1-phenylethylamino)-3,3-dimethyl-1-oxobutan-2-ylcarbamoyl)-6-(2-methylbiphenyl-4-yl)hexanoic acid
(R)-3-((S)-1-((S)-2-methoxy-1-phenylethylamino)-3,3-dimethyl-1-oxobutan-2-ylcarbamoyl)-6-(2-methylbiphenyl-4-yl)hexanoic acid 性质
| 熔点 | 178-180 °C |
|---|---|
| 沸点 | 802.7±65.0 °C(Predicted) |
| 密度 | 1.122±0.06 g/cm3(Predicted) |
| 储存条件 | Store at +4°C |
| 溶解度 | <57.27mg/ml，溶于 DMSO； <14.32mg/ml，乙醇中 |
| 形态 | 固体 |
| 酸度系数(pKa) | 4.68±0.10(Predicted) |
| 颜色 | 白色 |
(R)-3-((S)-1-((S)-2-methoxy-1-phenylethylamino)-3,3-dimethyl-1-oxobutan-2-ylcarbamoyl)-6-(2-methylbiphenyl-4-yl)hexanoic acid 用途与合成方法
|
MMP-3 23 nM (IC 50 ) |
MMP-12 42 nM (IC 50 ) |
MMP-8 1.75 μM (IC 50 ) |
MMP-13 2.3 μM (IC 50 ) |
MMP-7 5.8 μM (IC 50 ) |
MMP-9 30.4 μM (IC 50 ) |
MMP-2 34.2 μM (IC 50 ) |
MMP-14 66.9 μM (IC 50 ) |
The potency of UK-370106 (compound 7) for the inhibition of MMP-13 is 2.3 µM, some 100-fold less potent than its inhibition of MMP-3. UK-370106 is found to be inactive (IC
50
> 100 µM) vs zinc metalloproteases PCP and TACE and possesses the following inhibitory potencies vs MMP-2 (IC
50
of 34.2 µM), MMP-7 (IC
50
of 5.8 µM), MMP-8 (IC
50
of 1.75 µM), MMP-9 (IC
50
of 30.4 µM) and MMP-14 (IC
50
of 66.9 µM).
UK-370106 potently inhibits cleavage of [
3
H]-fibronectin by MMP-3 (IC
50
of 320 nM) but does not inhibit cleavage of [
3
H]-gelatin by either MMP-2 or -9 up to the highest concentration tested (100 µM).
UK-370106 is not cytotoxic to, nor affected proliferation of, fibroblasts, keratinocytes, or endothelial cells at 50-100 µM in vitro.
Following iv (rat; 2 mg/kg) or topical administration to dermal wounds (rabbit), UK-370106 (compound 7) is cleared rapidly (t 1/2 = 23 min) from plasma, but slowly (t 1/2 approximately 3 days) from dermal tissue. In a model of chronic dermal ulcers, topical administration of UK-370106 for 6 days substantially inhibits MMP-3 ex vivo.
(R)-3-((S)-1-((S)-2-methoxy-1-phenylethylamino)-3,3-dimethyl-1-oxobutan-2-ylcarbamoyl)-6-(2-methylbiphenyl-4-yl)hexanoic acid 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-08-19 | HY-107639 | (R)-3-((S)-1-((S)-2-methoxy-1-phenylethylamino)-3,3-dimethyl-1-oxobutan-2-ylcarbamoyl)-6-(2-methylbiphenyl-4-yl)hexanoic acid | 230961-21-4 | 1mg | 1950 |
| 2024-08-19 | HY-107639 | (R)-3-((S)-1-((S)-2-methoxy-1-phenylethylamino)-3,3-dimethyl-1-oxobutan-2-ylcarbamoyl)-6-(2-methylbiphenyl-4-yl)hexanoic acid | 230961-21-4 | 5mg | 5800 |
