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| | ARL 67156 Basic information |
| Product Name: | ARL 67156 | | Synonyms: | ARL67156 trisodium salt,ARL-67156 trisodium salt;[dibromo-[[[(2R,3S,4S,5R)-5-[6-(diethylamino)purin-9-yl]-3,4-dihydroxyoxolan-2-yl]methoxy-oxidophosphoryl]oxy-oxidophosphoryl]methyl]-hydroxyphosphinate | | CAS: | 1021868-83-6 | | MF: | C15H25Br2N5NaO12P3 | | MW: | 743.11 | | EINECS: | | | Product Categories: | | | Mol File: | 1021868-83-6.mol |  |
| | ARL 67156 Chemical Properties |
| storage temp. | Desiccate at -20°C | | solubility | <15.78mg/ml in H2O | | form | solid | | color | White | | Water Solubility | Soluble to 20 mM in water |
| | ARL 67156 Usage And Synthesis |
| 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]. | | 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, 2mg/kg) prevents the increase of serum adenosine concentration induced by Fructose 1,6-bisphosphate (FBP)[3]. | Animal Model: | Warfarin-induced mineralization rat model[2] | | Dosage: | 1.1 μg/kg/day | | Administration: | Administered with osmotic pumps implanted subcutaneously, for 28 days | | Result: | Prevented the development of aortic stenosis by lowering the level of apoptosis and mineralization of the aortic valve/aorta.
Normalized the level of pAkt (an important kinase involved in the survival pathway).
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| Animal Model: | C57BL/6 mice[3] | | Dosage: | 2mg/kg | | Administration: | Intraperitoneal injection, 1 h before administration of FBP (100mg/kg) | | Result: | Completely abolished the anti-inflammatory effects of FBP (observed by the neutrophil infiltration, hyperalgesia and oedema of the joint). |
| | 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]. côté 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. |
| | ARL 67156 Preparation Products And Raw materials |
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