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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
规格:98%
市场价:3640元
分子量:785.06

产品介绍
ecto-ATPase inhibitor
CAS:1021868-83-6
分子式:C15H21Br2N5O12P3.3Na
分子量:785.06
纯度:98%
存储:Store at -20°C

Background:

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].


参考文献:
[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.