(ALPHAS)-ALPHA-[(2,6-二氯苯甲酰)氨基]-2',6'-二甲氧基联苯-4-丙酸
| 中文名称 | (ALPHAS)-ALPHA-[(2,6-二氯苯甲酰)氨基]-2',6'-二甲氧基联苯-4-丙酸 |
|---|---|
| 中文同义词 | (ALPHAS)-ALPHA-[(2,6-二氯苯甲酰)氨基]-2',6'-二甲氧基联苯-4-丙酸;(S)-2-(2,6-二氯苯酰胺)-3-(2,6-二甲氧基-[1,1-联苯]-4-基)丙酸;化合物TR14035;TR 14035,整联蛋白Α4Β7和Α4Β1(VLA-4)拮抗剂 |
| 英文名称 | N-(2,6-Dichlorobenzoyl)-4-(2,6-diMethoxyphenyl)-L-phenylalanine |
| 英文同义词 | TR 14035;(S)-2-(2,6-DichlorobenzaMido)-3-(2',6'-diMethoxy-[1,1'-biphenyl]-4-yl)propanoic acid;N-(2,6-Dichlorobenzoyl)-4-(2,6-diMethoxyphenyl)-L-phenylalanine;(alphaS)-alpha-[(2,6-Dichlorobenzoyl)amino]-2',6'-dimethoxy-[1,1'-biphenyl]-4-propanoic acid;MDK1191;MDK-1191;TR 14035;TR14035;MDK-1191;MDK1191;TR-14035;TR 14035;TR14035 |
| CAS号 | 232271-19-1 |
| 分子式 | C24H21Cl2NO5 |
| 分子量 | 474.33 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 232271-19-1.mol |
| 结构式 | ![(ALPHAS)-ALPHA-[(2,6-二氯苯甲酰)氨基]-2',6'-二甲氧基联苯-4-丙酸 结构式](CAS/GIF/232271-19-1.gif) |
(ALPHAS)-ALPHA-[(2,6-二氯苯甲酰)氨基]-2',6'-二甲氧基联苯-4-丙酸 性质
| 沸点 | 604.0±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.333 |
| 储存条件 | 2-8°C |
| 溶解度 | 二甲基亚砜：≥ 41 mg/mL（86.44 mM） |
| 形态 | 粉末 |
| 酸度系数(pKa) | 3.53±0.10(Predicted) |
| 颜色 | 白色至米白色 |
TR-14035 (SB 683698, MDK-1191) 是一种 alpha4beta (α4β) integrin 双效拮抗剂，对 alpha4beta7 (α4β7) 和 alpha4beta1 (α4β1) 的IC50值分别为7 nM和87 nM。
| Target | Value |
|
α4β7
(Cell-free assay) | 7 nM |
|
α4β1
(Cell-free assay) | 87 nM |
TR14035 blocks adhesion of RPMI-8866 cells to MAdCAM-Ig by 100% at 1μM, with an approximate IC
50
of 0.01μM.
TR-14035 (3 mg/kg; i.g.) produces a significant decrease of the airways hyper-responsiveness to 5-hydroxytryptamine (5-HT) in an experimental model of allergic asthma in Brown Norway rats.
TR-14035 exhibits plasma decreased with half-lives of 0.28 h (3 mg/kg for i.v.) and 0.39 h (10 mg/kg for i.g.), and the oral bioavailability (F) is 17%.
| Animal Model: | Male Brown Norway rats (250-300 g) |
| Dosage: | 3 mg/kg |
| Administration: | Oral gavage, 1 h before and 3 h after antigen challenge |
| Result: | Suppressed antigen-induced airway hyper-responsiveness and inflammation. |
| Animal Model: | Male Sprague-Dawley rats (250-320 g) |
| Dosage: | 3 mg/ kg for i.v.; 10 mg/kg for i.g. |
| Administration: | Intravenous injection and oral gavage |
| Result: | T 1/2 (1.88 h for i.v.; 3.42 h for i.g.), F (17%). |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/08/19 | HY-15770 | TR-14035 | 1 mg | 838元 | |
| 2024/08/19 | HY-15770 | (ALPHAS)-ALPHA-[(2,6-二氯苯甲酰)氨基]-2',6'-二甲氧基联苯-4-丙酸 TR-14035 | 232271-19-1 | 5mg | 1900元 |