1976038-41-1
中文名称
TGFβRI-IN-2
英文名称
TGFβRI-IN-2
CAS
1976038-41-1
分子式
C20H15ClFN5O2
分子量
411.82
MOL 文件
1976038-41-1.mol
1976038-41-1 结构式
基本信息
中文别名
化合物 T13139 英文别名
TP-008TGFβRI-IN-2
TGFβRI-IN-2
TP008,TP 008
3H-Imidazo[4,5-c]pyridine-3-acetamide, 1-[2-(5-chloro-2-fluorophenyl)-5-methyl-4-pyridinyl]-1,2-dihydro-2-oxo-
物理化学性质
沸点664.2±65.0 °C(Predicted)
密度1.450±0.06 g/cm3(Predicted)
储存条件2-8°C
溶解度DMSO: 2mg/mL, clear
酸度系数(pKa)15.82±0.40(Predicted)
形态Solid
颜色White to off-white
常见问题列表
生物活性
TGFβRI-IN-2 (compound 18) 是一种有效的，选择性的和口服活性的激活素样激酶 5 (ALK 5) 抑制剂，pIC50 和 pEC50 值分别为 7.6 和 6.63。TGFβRI-IN-2 在高剂量时会在体内产生心脏毒性。靶点
IC50: ALK 5
体外研究
TGFβRI-IN-2 (compound 18) at 1 μM shows a 31% inhibition of MAP3K2 (MEKK2) with an IC 50 value of 2.2 μM.
体内研究
TGFβRI-IN-2 (oral administation; 50, 150 and 500 mg/kg; 5 days) induces cardiovascular toxicity characterized by valvular interstitial cell proliferation, neutrophil presence, hemorrhage and fibrin deposition in the heart valves.
| Animal Model: | Rats |
| Dosage: | 50, 150 and 500 mg/kg |
| Administration: | Oral administation; 50, 150 and 500 mg/kg; 5 days |
| Result: | Induced cardiovalvulopathy in both the medium and high dose animal groups. |