Lu AA 47070Prodrug of a potent and selective adenosine A2A receptor antagonist CAS# 913842-25-8 |
- HG-10-102-01
Catalog No.:BCC4271
CAS No.:1351758-81-0
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| Cas No. | 913842-25-8 | SDF | Download SDF |
| PubChem ID | 11947802 | Appearance | Powder |
| Formula | C17H20F2N3O6PS | M.Wt | 463.39 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in DMSO | ||
| Chemical Name | [2-[4-(3,3-dimethylbutanoylamino)-3,5-difluorobenzoyl]imino-1,3-thiazol-3-yl]methyl dihydrogen phosphate | ||
| SMILES | CC(C)(C)CC(=O)NC1=C(C=C(C=C1F)C(=O)N=C2N(C=CS2)COP(=O)(O)O)F | ||
| Standard InChIKey | MSWIQSFUBYCFJE-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C17H20F2N3O6PS/c1-17(2,3)8-13(23)20-14-11(18)6-10(7-12(14)19)15(24)21-16-22(4-5-30-16)9-28-29(25,26)27/h4-7H,8-9H2,1-3H3,(H,20,23)(H2,25,26,27) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | 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. |
Lu AA 47070 Dilution Calculator
Lu AA 47070 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.158 mL | 10.79 mL | 21.5801 mL | 43.1602 mL | 53.9502 mL |
| 5 mM | 0.4316 mL | 2.158 mL | 4.316 mL | 8.632 mL | 10.79 mL |
| 10 mM | 0.2158 mL | 1.079 mL | 2.158 mL | 4.316 mL | 5.395 mL |
| 50 mM | 0.0432 mL | 0.2158 mL | 0.4316 mL | 0.8632 mL | 1.079 mL |
| 100 mM | 0.0216 mL | 0.1079 mL | 0.2158 mL | 0.4316 mL | 0.5395 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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The novel adenosine A2A antagonist Lu AA47070 reverses the motor and motivational effects produced by dopamine D2 receptor blockade.[Pubmed:22037410]
Pharmacol Biochem Behav. 2012 Jan;100(3):498-505.
Dopamine D2 and adenosine A(2A) receptors interact to regulate aspects of motor and motivational function, and it has been suggested that adenosine A(2A) antagonists could be useful for the treatment of parkinsonism and depression. The present experiments were performed to characterize the effects of Lu AA47070, which is a phosphonooxymethylene prodrug of a potent and selective adenosine A(2A) receptor antagonist, for its ability to reverse the motor and motivational effects of D2 antagonism. In the first group of studies, Lu AA47070 (3.75-30 mg/kg IP) was assessed for its ability to reverse the effects of the D2 receptor antagonist pimozide (1.0 mg/kg IP) using several measures of motor impairment, including catalepsy, locomotion, and tremulous jaw movements, which is a rodent model of parkinsonian tremor. Lu AA47070 produced a significant reversal of the effects of pimozide on all three measures of parkinsonian motor impairment. In addition, Lu AA47070 was able to reverse the effects of a low dose of the D2 antagonist haloperidol on a concurrent lever pressing/chow feeding task that is used as a measure of effort-related choice behavior. The ability of Lu AA47070 to reverse the effects of D2 receptor blockade suggests that this compound could have potential utility as a treatment for parkinsonism, and for some of the motivational symptoms of depression.
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 hA(2A) receptor antagonist.[Pubmed:21210664]
J Med Chem. 2011 Feb 10;54(3):751-64.
The discovery and structure-activity relationship of a series of hA(2A) receptor antagonists is described. Compound 28 was selected from the series as a potent and selective compound and was shown to be efficacious in an in vivo model of Parkinson's disease. It had acceptable ADME properties; however, the low intrinsic solubility of this compound was limiting for its developability, because the oral bioavailability from dosing in suspension was significantly lower than the oral bioavailability from solution dosage. As a consequence, prodrugs of 28 were prepared with dramatically increased aqueous solubility. The prodrugs efficiently delivered 28 into systemic circulation, with no detectable levels of prodrug in plasma samples. From this investigation, we selected 32 (Lu AA47070), a phosphonooxymethylene prodrug of 28, as a drug candidate.
