ARL67156 trisodium hydrate
PRODUCTS SPECIFICATIONS
DESCRIPTION
Overview
| MDL | - |
|---|---|
| Molecular Weight | 834.61 |
| Molecular Formula | C15H23Br2N5Na3O13P3 |
| 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.O.[2.75] |
2 Publications Citing Use of MCE
Summary
ARL67156 (FPL 67156) trisodium hydrate is a selective ecto-ATPase inhibitor. ARL67156 trisodium hydrate is a competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with K i s of 11, 18 and 12 μM, respectively. ARL67156 trisodium hydrate can be used in the research of disease like calcific aortic valve disease, asthma [1] [2] .
IC50 & Target
Ki: 11 μM (NTPDase1), 18 μM (NTPDase3), 12 μM (NPP1) [1]
In Vitro
ARL67156 trisodium hydrate (1-100 μM) potentiates neurogenic contractions in a concentration-dependent manner
[4]
.
ARL67156 trisodium hydrate (10 μg/mL, 24 h) increases the surface expression of CXCR3 on ATP-treated HMC-1 cells
[5]
.
ARL67156 trisodium hydrate (30 μM, 5s) potentiates the norepinephrine release promoted by ATP in guinea pig heart synaptosomes
[6]
.
ARL67156 trisodium hydrate (100 μM, 4h) significantly decreases HIV-1replication in macrophages
[7]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
ARL67156 trisodium hydrate (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
[2]
.
ARL67156 trisodium hydrate (intraperitoneal injection, 2 mg/kg) prevents the increase of serum adenosine concentration induced by Fructose 1,6-bisphosphate (FBP)
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Warfarin-induced mineralization rat model [2] |
| 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 [3] |
| 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). |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
- [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.
- [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.
- [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.
- [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.
- [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.
- [7] Julieta Schachter, et al. Inhibition of ecto-ATPase activities impairs HIV-1 infection of macrophages. Immunobiology. 2015 May;220(5):589-96.