Description: Prodrug of a potent and selective adenosine A2A receptor antagonist
Chemical Name: 4-[(3,3-Dimethyl-1-oxobutyl)amino]-3,5-difluoro-N-[3-[(phosphonooxy)methyl]-2(3H)-thiazolylidene]benzamide
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Prodrug of a potent and selective adenosine A2A receptor antagonist (Ki values are 5.9, 260, 410 and <10,000 nM for A2A, A2B, A1 and A3 receptors respectively. Reverses parkinsonian motor impairment and motivational effects produced by dopamine D2 receptor blockade in rats. Orally bioavailable.
Compound Libraries
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The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
46.34
100
Preparing Stock Solutions
The following data is based on the product molecular weight 463.39. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
2.16 mL
10.79 mL
21.58 mL
5 mM
0.43 mL
2.16 mL
4.32 mL
10 mM
0.22 mL
1.08 mL
2.16 mL
50 mM
0.04 mL
0.22 mL
0.43 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Samset al (2011) Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA2A receptor antagonist. J.Med.Chem. 54 751 PMID: 21210664
Collinset al (2012) The novel adenosine A2A antagonist Lu AA47070 reverses the motor and motivational effects produced by dopamine D2 receptor blockade. Pharmacol.Biochem.Behav. 100 498 PMID: 22037410