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MedChemExpress - Model ARL67156 trisodium - 1021868-83-6

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

ARL67156 trisodium

MCE China：ARL67156 trisodium

Brand：MedChemExpress (MCE)

Cat. No.HY-103265

CAS：1021868-83-6

Synonyms：FPL 67156 trisodium

Purity：99.94%

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

Shipping：Room temperature in continental US; may vary elsewhere.

Description：ARL67156 (FPL 67156) trisodium is a selective small molecular inhibitor, targeting to ecto-ATPase, CD39, and CD73. ARL67156 trisodium is also a competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with Kis of 11, 18 and 12?μM, respectively. ARL67156 trisodium can be used in the research of calcific aortic valve disease, asthma.

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

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

IC50 & Target：Ki: 11 μM (NTPDase1), 18 μM (NTPDase3), 12 μM (NPP1)[1]; 0.97 μM (CD39), 0.45 μM (CD73)[8] In Vitro ARL67156 trisodium (1-100 μM) potentiates neurogenic contractions in a concentration-dependent manner[4].?ARL67156 trisodium (10 μg/mL, 24 h) increases the surface expression of CXCR3 on ATP-treated HMC-1 cells[5].?ARL67156 trisodium (30 μM, 5s) potentiates the norepinephrine release promoted by ATP in guinea pig heart synaptosomes[6].?ARL67156 trisodium (100 μM, 4h) significantly decreases HIV-1replication in macrophages[7]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> ARL67156 trisodium Related Antibodies

References：

[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]

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