ARL 67156 trisodium salt
(Synonyms: FPL 67156 trisodium) 目录号 : GC17225ARL67156 (FPL 67156) trisodium 是一种选择性 ecto-ATPase 抑制剂。
Cas No.:1021868-83-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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]. Côté 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.
| 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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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 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 | 0.2548 mL | 1.2738 mL | 2.5476 mL |
| 10 mM | 0.1274 mL | 0.6369 mL | 1.2738 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % 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，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。