1021868-83-6
中文名称
ARL 67156
英文名称
ARL 67156
CAS
1021868-83-6
分子式
C15H21Br2N5O12P3.3Na
分子量
743.11
MOL 文件
1021868-83-6.mol
1021868-83-6 结构式
常见问题列表
生物活性
ARL67156 trisodium salt 是一种 ecto-ATPase 抑制剂。ARL67156 trisodium salt 是弱的竞争性 NTPDase1 (CD39)，NTPDase3 和 NPP1 抑制剂，Ki 分别为 11，18 和 12 μM。ARL67156 trisodium salt 可预防体内主动脉瓣钙化。靶点
Ki: 11 μM (NTPDase1), 18 μM (NTPDase3), 12 μM (NPP1)
体外研究
ARL67156 trisodium salt is also an effective inhibitor of UTP breakdown by superior cervical ganglion cells and to potentiate contractions elicited by this nucleotide in isolated tail artery of rat. ARL67156 is not an effective inhibitor of NTPDase2, NTPDase8, NPP3 and ecto-5′-nucleotidase (CD73), although it also reduces the activity of these enzymes.
体内研究
Pre-treatment of mice with ARL67156 (2 mg/kg, i.p.), a selective inhibitor of CD39 (CD39i), completely prevents the increase of serum adenosine concentration induced by Fructose 1,6-bisphosphate (FBP; 100 mg/kg).
| Animal Model: | C57BL/6 mice |
| Dosage: | 2 mg/kg |
| Administration: | Pre-treated (i.p.) 1 h before administration of FBP (100 mg/kg) |
| Result: | Completely prevented the increase of serum adenosine concentration induced by FBP. |