ARL67156 trisodium
Based on 3 publication(s) in Google Scholar
ARL67156 (FPL 67156) trisodium is a selective small molecular inhibitor, targeting to ecto-ATPase, CD39, and CD73. ARL67156 trisodium is also a competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with Kis of 11, 18 and 12?μM, respectively. ARL67156 trisodium can be used in the research of calcific aortic valve disease, asthma.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.94%
- CAS 番号: 1021868-83-6
- 分子式: C15H21Br2N5Na3O12P3
- 分子量:785.05
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保管条件:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 ARL67156 trisodium
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生物活性
Ki: 11 μM (NTPDase1), 18 μM (NTPDase3), 12 μM (NPP1)[1]; 0.97 μM (CD39), 0.45 μM (CD73)[8]
ARL67156 trisodium (1-100 μM) potentiates neurogenic contractions in a concentration-dependent manner[4].
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ARL67156 trisodium (10 μg/mL, 24 h) increases the surface expression of CXCR3 on ATP-treated HMC-1 cells[5].
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ARL67156 trisodium (30 μM, 5s) potentiates the norepinephrine release promoted by ATP in guinea pig heart synaptosomes[6].
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ARL67156 trisodium (100 μM, 4h) significantly decreases HIV-1replication in macrophages[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
? ARL67156 trisodium (intraperitoneal injection, 2?mg/kg) prevents the increase of serum adenosine concentration induced by Fructose 1,6-bisphosphate (FBP)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Warfarin-induced mineralization rat model[2]
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Dosage:1.1 μg/kg/day
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Administration:Administered with osmotic pumps implanted subcutaneously, for 28 days
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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).
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Animal Model:C57BL/6 mice[3]
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Dosage:2 mg/kg
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Administration:Intraperitoneal injection, 1 h before administration of FBP (100 mg/kg)
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Result:Completely abolished the anti-inflammatory effects of FBP (observed by the neutrophil infiltration, hyperalgesia and oedema of the joint).
化学情報
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CAS 番号 1021868-83-6
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性状 Solid
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分子量 785.05
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分子式 C15H21Br2N5Na3O12P3
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Color White to light yellow
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SMILES
O[C@H]1[C@@H](O[C@H](COP(OP(C(Br)(Br)P(O)(O[Na])=O)(O[Na])=O)(O[Na])=O)[C@H]1O)N2C3=NC=NC(N(CC)CC)=C3N=C2
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別名
FPL 67156 trisodium
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
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Journal Impact Factor
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Most Recent
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Neuron
2022 Mar 2;110(5):770-782.e5. PMID: 34942116 -
Front Immunol
CD38+CD39+ NK cells associate with HIV disease progression and negatively regulate T cell proliferation. [Abstract]2022 Oct 4:13:946871. PMID: 36268017 -
Curr Eye Res
Integrated Spatiotemporal and Correlative Analysis of ATP-Related Signaling Components in Lens Development. [Abstract]2026 Apr;51(4):359-373. PMID: 41310968
溶剤 & 溶解度
H2O : 2.5 mg/mL (3.18 mM; ultrasonic and warming and heat to 60°C)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (286 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
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. [Content Brief]
[2]. Nancy Côté, 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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[7]. Julieta Schachter, et al. Inhibition of ecto-ATPase activities impairs HIV-1 infection of macrophages. Immunobiology. 2015 May;220(5):589-96. [Content Brief]
[8]. Schäkel L, et al. Nucleotide Analog ARL67156 as a Lead Structure for the Development of CD39 and Dual CD39/CD73 Ectonucleotidase Inhibitors. Front Pharmacol. 2020 Sep 8;11:1294. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 1.2738 mL | 6.3690 mL | 12.7380 mL | 31.8451 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
ARL67156 trisodium 関連分類
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