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Submit ReviewIstradefylline
Description: Potent and selective A2A antagonist
Alternative Names: KW-6002
Chemical Name: 8-[(1E)-2-(2-(3,4-Dimethoxyphenyl)ethenyl]-1,3-diethyl-3,7-dihydro-7-methyl-1H-purine-2,6-dione
Purity: ≥99% (HPLC)
Biological Activity
Potent and selective adenosine A2A receptor antagonist (Ki values are 2.2 and 150 nM for A2A and A1 receptors respectively). Anticataleptic and antiparkinson agent; reverses drug-induced motor dysfunction in animal models.
Technical Data
| M. Wt | 384.43 |
| Formula | C20H24N4O4 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 155270-99-8 |
| PubChem ID | 5311037 |
| InChI Key | IQVRBWUUXZMOPW-PKNBQFBNSA-N |
| Smiles | O=C1N(CC)C(C(N(C)C(/C=C/C3=CC(OC)=C(OC)C=C3)=N2)=C2N1CC)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 7.69 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 384.43. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 13.01 mL | 65.03 mL | 130.06 mL |
| 1 mM | 2.6 mL | 13.01 mL | 26.01 mL |
| 2 mM | 1.3 mL | 6.5 mL | 13.01 mL |
| 10 mM | 0.26 mL | 1.3 mL | 2.6 mL |
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References
References are publications that support the biological activity of the product.
Shimada et al (1997) Adenosine A2A antagonists with potent anti-cataleptic activity. Bioorg.Med.Chem.Lett. 7 2349
Kanda et al (1998) Adenosine A2A receptors modify motor function in MPTP-treated common marmosets. Neuroreport 9 2857 PMID: 9760134
Shiozaki et al (1999) Actions of adenosine A2A receptor antagonist KW-6002 on drug-induced catalepsy and hypokinesia caused by rese. or MPTP. Psychopharmacology 147 90 PMID: 10591873
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Keywords: Istradefylline, Istradefylline supplier, Potent, selective, Adenosine, A2A, receptor, antagonists, KW-6002, KW6002, AA2AR, antiparkinsons, activity, antiparkinsonian, anticataleptics, Receptors, 5147, Tocris Bioscience
3 Citations for Istradefylline
Citations are publications that use Tocris products. Selected citations for Istradefylline include:
Orr et al (2018) Istradefylline reduces memory deficits in aging mice with amyloid pathology. Neurobiol Dis 110 29 PMID: 29100987
Wydra et al (2015) On the role of A2A and D2 receptors in control of cocaine and food-seeking behaviors in rats. PLoS One 232 1767 PMID: 25420611
Cheng et al (2017) Structures of Human A1 and A2A Adenosine Receptors with Xanthines Reveal Determinants of Selectivity. Structure 25 1275 PMID: 28712806
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