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ChemicalBook--->CAS DataBase List--->1021868-83-6

1021868-83-6

1021868-83-6 Structure

1021868-83-6 Structure
IdentificationBack Directory
[Name]

ARL 67156
[CAS]

1021868-83-6
[Synonyms]

ARL67156 trisodium salt,ARL-67156 trisodium salt
[Molecular Formula]

C15H21Br2N5O12P3.3Na
[MDL Number]

MFCD08544552
[MOL File]

1021868-83-6.mol
[Molecular Weight]

743.11
Chemical PropertiesBack Directory
[storage temp. ]

Desiccate at -20°C
[solubility ]

<15.78mg/ml in H2O
[form ]

solid
[color ]

White
[Water Solubility ]

Soluble to 20 mM in water
Hazard InformationBack Directory
[Uses]

ARL 67156 Trisodium Salt acts as an ecto-ATPase inhibitor used to aid in distinguishing the function of ATP and its hydrolysis product adenosine in vivo.
[Biological Activity]

arl 67156 trisodium salt is a selective inhibitor of ecto-atpase. also, fpl 67156 is a weak agonist of p2u-purinoceptors and weak antagonist of p2t- and p2x-purinoceptors [1].ecto-atpase is an integral membrane protein that catalyzes the hydrolysis of extracellular atp to adp and inorganic phosphate.arl 67156 trisodium salt is a selective ecto-atpase inhibitor. in the human blood cell assay, arl 67156 inhibited atp degradation with pic50 value of 4.62. in the rabbit ear artery, arl 67156 30 μm-1 mm) increased the contractile effects of atp and inhibited ecto-atpase with pki value of 5.2 [1]. in the guinea-pig vas deferens, arl 67156 (5-100 μm) significantly increased neurogenic contract response to nerve stimulation in a concentration-dependent way, which was due to potentiation of the action of atp [2]. in hek 293t or cos-7 cells transfected with human npp1, npp3, ntpdase1, 2, 3 or 8, arl 67156 (50-100 μm) competitively inhibited human npp1, ntpdase1 and ntpdase3 with ki values of 12, 11 and 18 μm, respectively [3].in warfarin-induced mineralization rat model, arl67156 inhibited mineralization of the aortic valve/aorta and prevented aortic stenosis by the inhibition of apoptosis. also, arl67156 normalized the level of pakt, which was involved in the survival pathway [4].
[storage]

Store at -20°C
[References]

[1]. crack be, pollard ce, beukers mw, et al. pharmacological and biochemical analysis of fpl 67156, a novel, selective inhibitor of ecto-atpase. br j pharmacol, 1995, 114(2): 475-481.
[2]. westfall td, kennedy c, sneddon p. enhancement of sympathetic purinergic neurotransmission in the guinea-pig isolated vas deferens by the novel ecto-atpase inhibitor arl 67156. br j pharmacol, 1996, 117(5): 867-872.
[3]. lévesque sa, lavoie eg, lecka j, et al. specificity of the ecto-atpase inhibitor arl 67156 on human and mouse ectonucleotidases. br j pharmacol, 2007, 152(1): 141-150.
[4]. c?té n, el husseini d, pépin a, et al. inhibition of ectonucleotidase with arl67156 prevents the development of calcific aortic valve disease in warfarin-treated rats. eur j pharmacol, 2012, 689(1-3): 139-146.
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