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ARL 67156 trisodium salt

胞外ATP酶抑制剂,ARL67156 trisodium salt 是一种 ecto-ATPase 抑制剂。ARL 67156 是弱的竞争性 NTPDase1 (CD39)，NTPDase3 和 NPP1 抑制剂，Ki 分别为 11，18 和 12 μM。

目录号: PC12187 纯度: ≥98%

CAS No. :1021868-83-6

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中文名称	ARL 67156 trisodium salt
中文别名	ARL 67156 trisodium salt
英文名称	ARL 67156 trisodium salt
英文别名	ARL 67156 trisodium salt;ARL67156 trisodium salt
Cas No.	1021868-83-6
分子式	C₁₅N₅O₁₂P₃Br₂H₂₁
分子量	716.08
包装储存	-20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

ARL67156 (FPL 67156) trisodium is a selective ecto-ATPase inhibitor. ARL67156 trisodium is a competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with K_is of 11, 18 and 12?μM, respectively. ARL67156 trisodium can be used in the research of calcific aortic valve disease, asthma.

性状

Solid

IC50 & Target[1][2]

Ki: 11 μM (NTPDase1), 18 μM (NTPDase3), 12 μM (NPP1)

体外研究(In Vitro)

ARL67156 trisodium (1-100 μM) potentiates neurogenic contractions in a concentration-dependent manner.
ARL67156 trisodium (10 μg/mL, 24 h) increases the surface expression of CXCR3 on ATP-treated HMC-1 cells.
ARL67156 trisodium (30 μM, 5s) potentiates the norepinephrine release promoted by ATP in guinea pig heart synaptosomes.
ARL67156 trisodium (100 μM, 4h) significantly decreases HIV-1replication in macrophages.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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.
ARL67156 trisodium (intraperitoneal injection, 2?mg/kg) prevents the increase of serum adenosine concentration induced by Fructose 1,6-bisphosphate (FBP).

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Warfarin-induced mineralization rat model
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
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).

运输条件

Room temperature or refrigerated transportation.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献

[1]. Lévesque SA, et al. Specificity of the ecto-ATPase inhibitor ARL 67156 on human and mouse ectonucleotidases. Br J Pharmacol. 2007 Sep;152(1):141-50. [Information]

[2]. Nancy C?té, et al. Inhibition of Ectonucleotidase With ARL67156 Prevents the Development of Calcific Aortic Valve Disease in Warfarin-Treated Rats. Eur J Pharmacol. 2012 Aug 15;689(1-3):139-46. [Information]

[3]. Flávio P Veras, et al. Fructose 1,6-bisphosphate, a high-energy intermediate of glycolysis, attenuates experimental arthritis by activating anti-inflammatory adenosinergic pathway. Sci Rep. 2015 Oct 19;5:15171. [Information]

[4]. C Kennedy, et al. ATP as a co-transmitter with noradrenaline in sympathetic nerves--function and fate. Ciba Found Symp. 1996;198:223-35; discussion 235-8. [Information]

[5]. Ya-Dong Gao, et al. Th2 cytokine-primed airway smooth muscle cells induce mast cell chemotaxis via secretion of ATP. J Asthma. 2014 Dec;51(10):997-1003. [Information]

[6]. Casilde Sesti, et al. EctoNucleotidase in cardiac sympathetic nerve endings modulates ATP-mediated feedback of norepinephrine release. J Pharmacol Exp Ther. 2002 Feb;300(2):605-11. [Information]

[7]. Julieta Schachter, et al. Inhibition of ecto-ATPase activities impairs HIV-1 infection of macrophages. Immunobiology. 2015 May;220(5):589-96. [Information]

溶解度数据

体外研究:

H₂O : 25 mg/mL (31.85 mM; Need ultrasonic)

DMSO : 1 mg/mL (1.27 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.2738 mL	6.3690 mL	12.7380 mL
5 mM	0.2548 mL	1.2738 mL	2.5476 mL
10 mM	0.1274 mL	0.6369 mL	1.2738 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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