ARL67156 (FPL 67156) triethylamine is a selective ecto-ATPase inhibitor. ARL67156 triethylamine is a competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with K i s of 11, 18 and 12?μM, respectively. ARL67156 triethylamine can be used in the research of disease like calcific aortic valve disease, asthma.
ARL67156 triethylamine (1-100 μM) potentiates neurogenic contractions in a concentration-dependent manner.ARL67156 triethylamine (10 μg/mL, 24 h) increases the surface expression of CXCR3 on ATP-treated HMC-1 cells.ARL67156 triethylamine (30 μM, 5s) potentiates the norepinephrine release promoted by ATP in guinea pig heart synaptosomes.ARL67156 triethylamine (100 μM, 4h) significantly decreases HIV-1replication in macrophages. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
ARL67156 triethylamine (1.1 μg/kg/day, administered with osmotic pumps implanted subcutaneously, for 28 days) prevents the development of calcific aortic valve disease in Warfarin (HY-B0687)-treated rats.
ARL67156 triethylamine (intraperitoneal injection, 2?mg/kg) prevents the increase of serum adenosine concentration induced by Fructose 1,6-bisphosphate (FBP). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. évesque SA, et al. Specificity of the ecto-ATPase inhibitor ARL 67156 on human and mouse ectonucleotidases. Br J Pharmacol. 2007 Sep;152(1):141-50. [2]. Nancy C?té, et al. Inhibition of Ectonucleotidase With ARL67156 Prevents the Development of Calcific Aortic Valve Disease in Warfarin-Treated Rats. Eur J Pharmacol. 2012 Aug 15;689(1-3):139-46.
溶解度数据
In Vitro: Methanol : 125 mg/mL (108.30 mM; Need ultrasonic)DMSO : 100 mg/mL (86.64 mM; Need ultrasonic)配制储备液