化合物 T13099

生物活性靶点体外研究体内研究化合物 T13099 试剂级价格

化合物 T13099

CAS号:1005775-56-3
英文名:TC ASK 10
中文名:化合物 T13099
CBNumber:CB13037545
分子式:C21H22ClN5O
分子量:395.89
MOL File:1005775-56-3.mol

化合物 T13099化学性质

熔点 :>270° (dec.)
储存条件 :Refrigerator, under inert atmosphere
溶解度 :DMSO (Slightly), Methanol (Slightly)
形态 :Solid
颜色 :White to Off-White

安全信息

海关编码 :2933998090

化合物 T13099性质、用途与生产工艺

生物活性 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)。
靶点

ASK1

14 nM (IC ₅₀ )

体外研究

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.

体内研究

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.