1005775-56-3
中文名稱
化合物 T13099
英文名稱
TC ASK 10
CAS
1005775-56-3
分子式
C21H21N5O.2HCl
更新日期
2024/11/19 11:42:47
分子量
395.89
MOL 文件
1005775-56-3.mol
1005775-56-3 結(jié)構(gòu)式
基本信息
中文別名
化合物 T13099化合物TC ASK 10
英文別名
TC ASK 10ASK1 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
物理化學(xué)性質(zhì)
熔點(diǎn)>270° (dec.)
儲(chǔ)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
顏色白色至灰白色
常見(jiàn)問(wèn)題列表
生物活性
TC ASK 10 (Compound 10) 是一種有效的，選擇性的，口服活性的細(xì)胞凋亡信號(hào)調(diào)節(jié)激酶 1 (ASK1) 抑制劑，IC50 為 14 nM。TC ASK 10 對(duì)其他代表性激酶的抑制活性低于 50％，ASK2 除外 (IC50 為 0.51 μM)。靶點(diǎn)
|
ASK1 14 nM (IC 50 ) |
體外研究
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. |
體內(nèi)研究
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.