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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)
Citations (4)
Reviews (1)
Literature (1)

Biological Activity for Istradefylline

Istradefylline is a 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 for Istradefylline

M. Wt 384.43
Formula C20H24N4O4
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 155270-99-8
PubChem ID 5311037
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 for Istradefylline

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 7.69 20

Preparing Stock Solutions for Istradefylline

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.

Select a batch to recalculate based on the batch molecular weight:
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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Product Datasheets for Istradefylline

Certificate of Analysis / Product Datasheet
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References for Istradefylline

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

If you know of a relevant reference for Istradefylline, please let us know.

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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

4 Citations for Istradefylline

Citations are publications that use Tocris products. Selected citations for Istradefylline include:

John M et al (2021) Cannabis sativa terpenes are cannabimimetic and selectively enhance cannabinoid activity. Sci Rep 11 8232 PMID: 33859287

Cheng et al (2017) Structures of Human A1 and A2A Adenosine Receptors with Xanthines Reveal Determinants of Selectivity. Structure 25 1275 PMID: 28712806

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

Do you know of a great paper that uses Istradefylline from Tocris? Please let us know.

Reviews for Istradefylline

Average Rating: 4 (Based on 1 Review.)

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Istradefylline on D2R antagonist induced motor impairment.
By Yunmin Ding on 12/07/2018
Assay Type: In Vivo
Species: Mouse


Istradefylline from Tocris worked wonderfully. At 3 mg/kg (in suspension in 8% Tween 80 in 0.9% saline), it reversed motor impairment induced by 0.16 mg/kg of the D2R antagonist eticlopride

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

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