ARL 67156 trisodium salt是一种选择性的细胞外ATP酶抑制剂。
Cas No.:1021868-83-6
Sample solution is provided at 25 µL, 10mM.
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ARL 67156 trisodium salt is a selective inhibitor of ecto-ATPases[1]. The Ki values of ARL 67156 trisodium salt against human NTPDase1(CD39), NTPDase3, and NPP1 were 11±3, 18±4, and 12±3μM, respectively[1].
In vitro, treatment with 10μg/ml ARL 67156 trisodium salt for 24 hours increased the surface expression of CXCR3 on ATP-treated HMC-1 cells[2]. Treatment with 100μM ARL 67156 trisodium salt for 4 hours reduced HIV-1 replication in macrophages[3]. Treatment with 30μM ARL 67156 trisodium salt for 5 seconds enhanced ATP-promoted norepinephrine release in the synaptosome of guinea pig hearts[4].
In vivo, administration of ARL 67156 trisodium salt(2mg/kg; i.p.) for 24 hours completely prevented the FBP-induced increase in serum adenosine concentration in mice[5].
References:
[1] Lévesque SA, Lavoie EG, Lecka J, Bigonnesse F, Sévigny J. Specificity of the ecto-ATPase inhibitor ARL 67156 on human and mouse ectonucleotidases. Br J Pharmacol. 2007;152(1):141-150.
[2] Gao YD, Cao J, Li P, Huang G, Yang J. Th2 cytokine-primed airway smooth muscle cells induce mast cell chemotaxis via secretion of ATP. J Asthma. 2014;51(10):997-1003.
[3] Schachter J, Delgado KV, Barreto-de-Souza V, Bou-Habib DC, Persechini PM, Meyer-Fernandes JR. Inhibition of ecto-ATPase activities impairs HIV-1 infection of macrophages. Immunobiology. 2015;220(5):589-596.
[4] Sesti C, Broekman MJ, Drosopoulos JH, Islam N, Marcus AJ, Levi R. EctoNucleotidase in cardiac sympathetic nerve endings modulates ATP-mediated feedback of norepinephrine release. J Pharmacol Exp Ther. 2002;300(2):605-611.
[5]Veras FP, Peres RS, Saraiva AL, et al. Fructose 1,6-bisphosphate, a high-energy intermediate of glycolysis, attenuates experimental arthritis by activating anti-inflammatory adenosinergic pathway. Sci Rep. 2015;5:15171.
ARL 67156 trisodium salt是一种选择性的细胞外ATP酶抑制剂[1]。ARL 67156 trisodium salt对人NTPDase1（CD39）、NTPDase3和NPP1的Ki值分别为11±3μM、18±4μM和12±3μM[1]。
体外实验中，10μg/ml ARL 67156 trisodium salt处理24小时可增加ATP处理的HMC-1细胞表面CXCR3的表达水平[2]。100μM ARL 67156 trisodium salt处理4小时可降低巨噬细胞中的HIV-1复制[3]。30μM ARL 67156 trisodium salt处理5秒后，增强了豚鼠心脏突触体中ATP促进的去甲肾上腺素的释放[4]。
体内实验中，给予ARL 67156 trisodium salt（2mg/kg；腹腔注射）处理24小时可完全阻止小鼠中FBP诱导的血清腺苷浓度升高[5]。
| Cell experiment [1]: | |
Cell lines | HMC-1 cell |
Preparation Method | HMC-1 cells were placed into 6-well plates. After reaching 70% confluence, the cells were stimulated with ATP(10mM) in the absence or presence of exogenous CD39 or ARL 67156 trisodium salt (10μg/ml). |
Reaction Conditions | 10μg/ml; 24h |
Applications | CD39 decreased the surface expression of CXCR3 on both control and ATP-treated HMC-1 cells. ARL 67156 trisodium salt increased the surface expression of CXCR3 on ATP-treated HMC-1 cells. |
| Animal experiment [2]: | |
Animal models | Male C57BL/6 mice |
Preparation Method | Mice were pre-treated with ARL 67156 trisodium salt(2mg/kg) intraperitoneally 1h before treatment with FBP (Fructose 1,6-bisphosphate; 100mg/kg) and blood was withdrawn from by cardiac punction 24h later. Then, serum adenosine quantification was performed. |
Dosage form | 2mg/kg; i.p. |
Applications | ARL 67156 trisodium salt completely prevented the increase of serum adenosine concentration induced by FBP |
References: | |
| Cas No. | 1021868-83-6 | SDF | |
| 别名 | FPL 67156 trisodium | ||
| Canonical SMILES | CCN(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 tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.2738 mL | 6.3689 mL | 12.7379 mL |
| 5 mM | 254.8 μL | 1.2738 mL | 2.5476 mL |
| 10 mM | 127.4 μL | 636.9 μL | 1.2738 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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