| Identification | Back 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 Properties | Back 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 Information | Back 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]. | [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]. | 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).
|
| Animal Model: | C57BL/6 mice[3] | | Dosage: | 2?mg/kg | | Administration: | Intraperitoneal injection, 1 ?h before administration of FBP (100?mg/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]. 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. |
|
| Company Name: |
BOC Sciences
|
| Tel: |
|
| Website: |
https://www.bocsci.com |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
|