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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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500mg |
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Purity: ≥98%
ARN272 is a novel, potent inhibitor of anandamide transport. The systemic administration of ARN272 produced a dose-dependent suppression of nausea-induced conditioned gaping in rats, and produced a dose-dependent reduction of vomiting in shrews. The systemic co-administration of SR141716 with ARN272 (at 3.0 mg·kg(-1)) in rats produced a complete reversal of ARN272-suppressed gaping at 1.0 mg·kg(-1). SR141716 alone did not differ from the vehicle solution. Anandamide transport inhibition by the compound ARN272 tonically activates CB1 receptors and as such produces a type of indirect agonism to regulate toxin-induced nausea and vomiting. The results also provide behavioural evidence in support of a facilitated transport mechanism used in the cellular reuptake of anandamide.
References |
Br J Pharmacol.2013 Nov;170(5):1130-6.
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Molecular Formula |
C27H20N4O2
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Molecular Weight |
432.473305702209
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CAS # |
488793-85-7
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SMILES |
OC(C=C1)=CC=C1C2=NN=C(C3=C2C=CC=C3)NC4=CC=C(C(NC5=CC=CC=C5)=O)C=C4
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Synonyms |
ARN272; ARN-272; ARN 272
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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) |
DMSO : ~125 mg/mL (~289.04 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.81 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.81 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.3123 mL | 11.5615 mL | 23.1230 mL | |
5 mM | 0.4625 mL | 2.3123 mL | 4.6246 mL | |
10 mM | 0.2312 mL | 1.1561 mL | 2.3123 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.
Mean (+SEM) number of gapes by rats on drug-free test day, in experiment 1, by each of the groups.Br J Pharmacol.2013 Nov;170(5):1130-6. th> |
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Mean (±SEM) cumulative volume of saccharin consumed by rats 24 h after TR test day and immediately following water restriction, at 30 and 120 min, in experiment 1.Br J Pharmacol.2013 Nov;170(5):1130-6. td> |
Mean (±SEM) number of vomiting episodes displayed byS. murinusduring the 45 min post-LiCl administration observation period.Br J Pharmacol.2013 Nov;170(5):1130-6. td> |