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1mg |
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ARL 67156 (ARL-67156; FPL-67156) trisodium, an ATP analog, is a novel and potent inhibitor of ecto-ATPase, also acting as a weak competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1 (Kis =11, 18 and 12 μM, respectively) with immunomodulatory and anticancer activity.
Targets |
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ln Vitro |
In a concentration-dependent manner, ARL67156 trisodium (1-100 μM) improves neurogenic contractions [4]. On the cell membrane surface of ATP-treated HMC-1 cells, ARL67156 trisodium (10 μg/mL, 24 h) increases the expression of CXCR3 [5]. The release of norepinephrine in guinea pig cardiac synaptosomes stimulated by ATP is improved by ARL67156 trisodium (30 μM, 5s) [6]. Significantly less HIV-1 replication occurs in macrophages when treated with ARL67156 trisodium (100 μM, 4h) [7].
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ln Vivo |
Trisodium, ARL67156 (1.1 μg/kg/day, subcutaneous inlet osmotic pump for 28 days), protects warfarin-treated deposits against calcific aortic valve damage [2]. Increases in blood adenosine concentrations caused by fructose-1,6-bisphosphate (FBP) can be avoided by ARL67156 trisodium (intraperitoneal injection, 2 mg/kg) [3].
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Animal Protocol |
Animal/Disease Models: Warfarin-induced mineralization rat model [2]
Doses: 1.1 μg/kg/day Route of Administration: Osmotic administration subcutaneously (sc) (sc) implanted pump for 28 days Experimental Results: By lowering the aortic valve/aorta levels of apoptosis and mineralization to prevent the development of aortic stenosis. Normalization of levels of pAkt, an important kinase involved in survival pathways. Animal/Disease Models: C57BL/6 mice [3] Doses: 2 mg/kg Route of Administration: intraperitoneal (ip) injection 1 hour before administration of FBP (100 mg/kg) Experimental Results: Complete elimination of the anti-inflammatory effect of FBP (via neutrophils Infiltration observation), hyperalgesia and joint edema). |
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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. |
Molecular Formula |
C15H24BR2N5NA3O12P3
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Molecular Weight |
788.08
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CAS # |
1021868-83-6
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Related CAS # |
ARL67156 trisodium hydrate;ARL67156 triethylamine
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=P(C(Br)(P(O)(O)=O)Br)(OP(O[C@H]1O[C@@H](N2C=NC3=C(N(CC)CC)N=CN=C23)[C@H](O)[C@@H]1O)(OC)=O)O
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Chemical Name |
[dibromo-[[[(2R,3S,4R,5R)-5-(6-diethylaminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl]methyl]phosphonic acid
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Synonyms |
ARL-67156 FPL-67156 ARL67156FPL67156 ARL 67156
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
H2O : ~25 mg/mL (~31.85 mM)
DMSO : ~1 mg/mL (~1.27 mM) |
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.2689 mL | 6.3445 mL | 12.6891 mL | |
5 mM | 0.2538 mL | 1.2689 mL | 2.5378 mL | |
10 mM | 0.1269 mL | 0.6345 mL | 1.2689 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.