ARL67156 trisodium salt hydrate is an inhibitor of ecto-ATPase. ARL67156 trisodium salt hydrate is a weak competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with Kis of 11, 18 and 12 μM, respectively. ARL67156 trisodium salt hydrate prevents in vivo the development of calcific aortic valve disease.
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.
运输条件
Room temperature in continental US; may vary elsewhere.