Tocris/Lu AA 47070/4783/50/50 mg
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

Lu AA 47070 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 463.39
Formula C17H20F2N3O6PS
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 913842-25-8
PubChem ID 11947802
InChI Key MSWIQSFUBYCFJE-UHFFFAOYSA-N
Smiles FC1=C(NC(CC(C)(C)C)=O)C(F)=CC(C(/N=C2SC=CN2COP(O)(O)=O)=O)=C1

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

Product Datasheets

Certificate of Analysis / Product Datasheet
Safety Datasheet

References

References are publications that support the products' biological activity.

Sams et 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

Collins et 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


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