化合物 T13099
| 中文名称 | 化合物 T13099 |
|---|---|
| 中文同义词 | 化合物 T13099;化合物TC ASK 10;TC ASK 10,ASK1抑制剂 |
| 英文名称 | TC ASK 10 |
| 英文同义词 | TC ASK 10;ASK1 Inhibitor 10;4-tert-butyl-N-(6-imidazol-1-ylimidazo[1,2-a]pyridin-2-yl)benzamide:hydrochloride;4-(1,1-Dimethylethyl)-N-[6-(1H-imidazol-1-yl)imidazo[1,2-a]pyridin-2-yl]benzamide dihydrochloride;Apoptosis,ASK1,oral,MAP3K,bioavailability,TC ASK-10,TC ASK10,Inhibitor,pharmacokinetic,JNK,TC ASK 10,p38,inhibit,selective,MAP kinase kinase kinase, MEKK, MAPKKK,Phosphorylation |
| CAS号 | 1005775-56-3 |
| 分子式 | C21H22ClN5O |
| 分子量 | 395.89 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1005775-56-3.mol |
| 结构式 |  |
化合物 T13099 性质
| 熔点 | >270° (dec.) |
|---|---|
| 储存条件 | Refrigerator, under inert atmosphere |
| 溶解度 | 可溶于DMSO（少许）、甲醇（少许） |
| 形态 | 固体 |
| 颜色 | 白色至类白色 |
TC ASK 10 (Compound 10) 是一种有效的，选择性的，口服活性的细胞凋亡信号调节激酶 1 (ASK1) 抑制剂，IC50 为 14 nM。TC ASK 10 对其他代表性激酶的抑制活性低于 50％，ASK2 除外 (IC50 为 0.51 μM)。
|
ASK1 14 nM (IC 50 ) |
TC ASK 10 (Compound 10; 0-10 μM; 1 hour; INS-1 cells) treatment inhibits streptozotocin (STZ)-induced JNK in INS-1 pancreatic β cells from 0.3 μM. Phosphorylation of p38 is also inhibited in a dosedependent manner.
Western Blot Analysis
| Cell Line: | INS-1 cells |
| Concentration: | 0 μM, 0.3 μM, 1 μM, 3 μM, 10 μM |
| Incubation Time: | 1 hour |
| Result: | Was found to inhibit streptozotocin (STZ)-induced JNK in INS-1 pancreatic β cells from 0.3 μM. Phosphorylation of p38 was also inhibited in a dosedependent manner. |
Pharmacokinetic profiles in rats are tested. TC ASK 10 (Compound 10•HCl; rat cassette doing at 0.1 mg/kg, iv and 1 mg/kg, po.) has a good oral bioavailability. The C max , T max and AUC po,0-8h are 285.1 ng/mL, 1.67 h and 275.4 ng.h/mL, respectively for TC ASK 10.
安全信息
| 海关编码 | 2933998090 |
|---|
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-103258 | TC ASK 10 | 1 mg | 1333元 | |
| 2024/01/25 | HY-103258 | 化合物 T13099 TC ASK 10 | 1005775-56-3 | 5mg | 3850元 |