|Istradefylline (KW-6002)Selective A2A receptor antagonist|
Sample solution is provided at 25 µL, 10mM.
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|Description||Istradefylline is a selective antagonist of adenosine A2A receptor (A2AR) with a Ki value of 2.2 nM.|
|Cas No.||155270-99-8||SDF||Download SDF|
|Solubility||Soluble in DMSO > 10 mM||Storage||Store at -20°C|
KW-6002 is a selective adenosine A2A receptor antagonist, offering a novel mechanistic approach for the treatment of Parkinson’s disease (PD). A2A blockade will increase in GABAergic inhibition on the medium-sized neurons, leading to a net decrease in excessive activation of striatopallidal output.
In vitro: The affinity of KW-6002 for the A2AR is 70-fold greater than that for the A1 receptor. The binding affinities (Ki) of KW-6002 for human A1 receptor and A2A receptor are >287 nM and 9.12 nM, respectively .
In vivo: In MPTP neurotoxin model of PD in mice, KW-6002 significantly attenuated striatal dopamine depletion under various conditions. In addition, pretreatment with KW-6002 (3.3 mg/kg, i.p.) before a single dose of MPTP attenuated the partial dopamine and DOPAC depletions 1 week later .
Clinical trial: In a clinical study, the authors evaluated the safety and efficacy of KW-6002 40 mg as monotherapy for Parkinson’s disease (PD) in 176 patients. The primary efficacy outcome was changed from baseline to endpoint, while safe and well-tolerated, failed to show a significant improvement from placebo for this endpoint .
 Park A, Stacy M. Istradefylline for the treatment of Parkinson's disease. Expert Opin Pharmacother. 2012 Jan;13(1):111-4.
 Chen JF, Xu K, Petzer JP, Staal R, Xu YH, Beilstein M, Sonsalla PK, Castagnoli K, Castagnoli N Jr, Schwarzschild MA. Neuroprotection by caffeine and A(2A) adenosine receptor inactivation in a model of Parkinson's disease. J Neurosci. 2001;21(10):RC143.