化合物 T13099
| 中文名稱 | 化合物 T13099 |
|---|---|
| 中文同義詞 | 化合物 T13099;化合物TC ASK 10;TC ASK 10,ASK1抑制劑;N-(6-(1H-咪唑-1-基)咪唑并[1,2-A]吡啶-2-基)-4-(叔丁基)苯甲酰胺二鹽酸鹽;化合物TC ASK 10,10 MM DMSO 溶液 |
| 英文名稱 | TC ASK 10 |
| 英文同義詞 | 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;N-(6-(1H-Imidazol-1-yl)imidazo[1,2-a]pyridin-2-yl)-4-(tert-butyl)benzamide dihydrochloride;TC ASK 10, 10 mM in DMSO |
| CAS號 | 1005775-56-3 |
| 分子式 | C21H22ClN5O |
| 分子量 | 395.89 |
| EINECS號 | |
| 相關類別 | |
| Mol文件 | 1005775-56-3.mol |
| 結構式 |  |
化合物 T13099 性質
| 熔點 | >270° (dec.) |
|---|---|
| 儲存條件 | Refrigerator, under inert atmosphere |
| 溶解度 | 可溶于DMSO（少許）、甲醇（少許） |
| 形態(tài) | 固體 |
| 顏色 | 白色至類白色 |
TC ASK 10 (Compound 10) 是一種有效的，選擇性的，口服活性的細胞凋亡信號調節(jié)激酶 1 (ASK1) 抑制劑，IC50 為 14 nM。TC ASK 10 對其他代表性激酶的抑制活性低于 50％，ASK2 除外 (IC50 為 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
| 海關編碼 | 2933998090 |
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| 更新日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
|---|---|---|---|---|---|
| 2026/06/05 | HY-103258 | 化合物 T13099 TC ASK 10 | 1005775-56-3 | 1 mg | 371元 |
| 2026/06/05 | HY-103258 | 化合物 T13099 TC ASK 10 | 1005775-56-3 | 5mg | 866元 |