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ARL 67156 trisodium salt
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
ARL 67156 trisodium salt图片
CAS NO:1021868-83-6
包装:10mg
市场价:4013元

产品介绍
ARL67156 (FPL 67156) trisodium 是一种选择性 ecto-ATPase 抑制剂。
Cas No.1021868-83-6
别名FPL 67156 trisodium
Canonical SMILESCCN(C1=C(N=CN2[C@@]3([H])[C@@](O)([H])[C@@](O)([H])[C@@](O3)([H])COP(O)(OP(C(Br)(P([O-])([O-])=O)Br)([O-])=O)=O)C2=NC=N1)CC.[Na+].[Na+].[Na+]
分子式C15H21Br2N5O12P3.3Na
分子量785.06
溶解度<15.78mg/ml in Water
储存条件Desiccate at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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].

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].  Coté 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.