1021868-83-6
中文名稱
ARL 67156
英文名稱
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 結(jié)構(gòu)式
物理化學(xué)性質(zhì)
儲(chǔ)存條件Desiccate at -20°C
溶解度<15.78mg/ml in H2O
形態(tài)固體
顏色白色
水溶解性Soluble to 20 mM in water
常見問題列表
生物活性
ARL67156 trisodium salt 是一種 ecto-ATPase 抑制劑。ARL67156 trisodium salt 是弱的競(jìng)爭(zhēng)性 NTPDase1 (CD39)，NTPDase3 和 NPP1 抑制劑，Ki 分別為 11，18 和 12 μM。ARL67156 trisodium salt 可預(yù)防體內(nèi)主動(dòng)脈瓣鈣化。靶點(diǎn)
Ki: 11 μM (NTPDase1), 18 μM (NTPDase3), 12 μM (NPP1)
體外研究
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.
體內(nèi)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. |