ARL67156 (trisodium)

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].

Product Specifications

CAS Number

[1021868-83-6]

Product Name Alternative

FPL 67156 (trisodium)

UNSPSC

12352005

Target

NTPDase

Type

Reference compound

Related Pathways

Immunology/Inflammation

Field of Research

Inflammation/Immunology; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/arl67156-trisodium.html

Purity

99.94

Solubility

H2O : 2.5 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O[C@H]1[C@@H](O[C@H](COP(OP(C(Br)(Br)P(O)(O[Na])=O)(O[Na])=O)(O[Na])=O)[C@H]1O)N2C3=NC=NC(N(CC)CC)=C3N=C2

Molecular Formula

C15H21Br2N5Na3O12P3

Molecular Weight

785.05

References & Citations

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