1144477-35-9
中文名称
1144477-35-9
英文名称
TM-N1324
CAS
1144477-35-9
分子式
C18H13ClFN7O
分子量
397.79
MOL 文件
1144477-35-9.mol
![1144477-35-9 结构式](/CAS/20200611/GIF/1144477-35-9.gif)
基本信息
中文别名
化合物 T17103化合物TM-N1324
英文别名
TM-N13244-(2-Chloro-4-fluorophenyl)-1,4,5,7-tetrahydro-3-methyl-1-(9H-purin-6-yl)-6H-pyrazolo[3,4-b]pyridin-6-one
6H-Pyrazolo[3,4-b]pyridin-6-one, 4-(2-chloro-4-fluorophenyl)-1,4,5,7-tetrahydro-3-methyl-1-(9H-purin-6-yl)-
物理化学性质
沸点681.3±55.0 °C(Predicted)
密度1.74±0.1 g/cm3(Predicted)
储存条件-20°C储存
溶解度DMSO: soluble; Ethanol: soluble
酸度系数(pKa)8.07±0.10(Predicted)
形态固体
颜色White to off-white
常见问题列表
生物活性
TM-N1324 是 G 蛋白偶联受体 39 (GPR39) 的激动剂,在 Zn2+ 存在的情况下,对人和鼠 GPR39 的 EC50 值分别为 9 nM 和 5 nM,在 Zn2+ 不存在的情况下,对人和鼠 GPR39 的 EC50 值分别为 280 nM 和 180 nM。靶点
EC50: 280 nM (human GPR39 without Zn 2+ ), 9 nM (human GPR39 with Zn 2+ ), 180 nM (murine GPR39 without Zn 2+ ), 5 nM (murine GPR39 with Zn 2+ )
体外研究
TM-N1324 activates human GPR39 with high efficacy and potencies of 280 nM and 9 nM in the absence and presence of Zn 2+ , respectively. TM-N1324 has similar potencies on murine GPR39, 180 nM and 5 nM. TM-N1324 is also found to have promising in vitro ADME properties. TM-N1324 has reasonably good aqueous solubility (65 μM at pH 7.0). Measurements of somatostatin confirms that the GPR39 agonist TM-N1324 increases somatostatin release by 53%.