ARL67156 trisodium
Based on 4 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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- Purity: 99.94%
- CAS No.: 1021868-83-6
- 화학식: C15H21Br2N5Na3O12P3
- 분자량:785.05
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보관:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) ARL67156 trisodium
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Customer Validation & Images
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Flow Cytometry
Biological Activity
제품 설명
IC50 & Target
Ki: 11 μM (NTPDase1), 18 μM (NTPDase3), 12 μM (NPP1)[1]; 0.97 μM (CD39), 0.45 μM (CD73)[8]
In Vitro
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.
In Vivo
? 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).
Chemical Information
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CAS No. 1021868-83-6
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Appearance Solid
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분자량 785.05
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화학식 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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Synonyms
FPL 67156 trisodium
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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (4)
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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
ARL67156 trisodium purchased from MedChemExpress. Usage Cited in: Front Immunol. 2022 Oct 4:13:946871. [Abstract]
ARL67156 trisodium (100 μM; 30 min) restored the proliferation of the CD4+ T and CD8+ T cells on NK cells.
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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
용액&용해도
In Vitro:
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (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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Handling Instructions (2659 KB)
References
[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 Related Classifications
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