ARL67156 trisodium hydrate  (Synonyms: FPL 67156 trisodium hydrate)

ARL67156 (FPL 67156) trisodium hydrate is a selective small is a selective samll molecular inhibitor, targeting to ecto-ATPase, CD39, and CD73. ARL67156 trisodium hydrate is also a competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with K_is of 11, 18 and 12?μM, respectively. ARL67156 trisodium hydrate can be used in the research of disease like calcific aortic valve disease, asthma^[1][2].

Ki: 11 μM (NTPDase1), 18 μM (NTPDase3), 12 μM (NPP1)^[1]; 0.97 μM (CD39), 0.45 μM (CD73)^[8]

ARL67156 trisodium hydrate (1-100 μM) potentiates neurogenic contractions in a concentration-dependent manner^[4].
ARL67156 trisodium hydrate (10 μg/mL, 24 h) increases the surface expression of CXCR3 on ATP-treated HMC-1 cells^[5].
ARL67156 trisodium hydrate (30 μM, 5s) potentiates the norepinephrine release promoted by ATP in guinea pig heart synaptosomes^[6].
ARL67156 trisodium hydrate (100 μM, 4h) significantly decreases HIV-1replication in macrophages^[7].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

ARL67156 trisodium hydrate (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^[2].
ARL67156 trisodium hydrate (intraperitoneal injection, 2 mg/kg) prevents the increase of serum adenosine concentration induced by Fructose 1,6-bisphosphate (FBP)^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

834.61

C₁₅H₂₃Br₂N₅Na₃O₁₃P₃

固体

White to off-white

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

• [1]. Lévesque 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.  [Content Brief]

  [2]. Nancy Côté, 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.  [Content Brief]

  [3]. Flávio P Veras, et al. Fructose 1,6-bisphosphate, a high-energy intermediate of glycolysis, attenuates experimental arthritis by activating anti-inflammatory adenosinergic pathway. Sci Rep. 2015 Oct 19;5:15171.  [Content Brief]

  [4]. C Kennedy, et al. ATP as a co-transmitter with noradrenaline in sympathetic nerves--function and fate. Ciba Found Symp. 1996;198:223-35; discussion 235-8.  [Content Brief]

  [5]. Ya-Dong Gao, et al. Th2 cytokine-primed airway smooth muscle cells induce mast cell chemotaxis via secretion of ATP. J Asthma. 2014 Dec;51(10):997-1003.  [Content Brief]

  [6]. Casilde Sesti, et al. EctoNucleotidase in cardiac sympathetic nerve endings modulates ATP-mediated feedback of norepinephrine release. J Pharmacol Exp Ther. 2002 Feb;300(2):605-11.  [Content Brief]

  [7]. Julieta Schachter, et al. Inhibition of ecto-ATPase activities impairs HIV-1 infection of macrophages. Immunobiology. 2015 May;220(5):589-96.  [Content Brief]

  [8]. Schäkel L, et al. Nucleotide Analog ARL67156 as a Lead Structure for the Development of CD39 and Dual CD39/CD73 Ectonucleotidase Inhibitors. Front Pharmacol. 2020 Sep 8;11:1294.  [Content Brief]