Istradefylline
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 315137

CAS#: 155270-99-8

Description: Istradefylline (KW-6002) is a selective antagonist at the A2A receptor. It has been found to be useful in the treatment of Parkinson's disease. Istradefylline reduces dyskinesia resulting from long-term treatment with classical antiparkinson drugs such as levodopa. Istradefylline is an analog of caffeine.


Chemical Structure

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Istradefylline
CAS# 155270-99-8

Theoretical Analysis

MedKoo Cat#: 315137
Name: Istradefylline
CAS#: 155270-99-8
Chemical Formula: C20H24N4O4
Exact Mass: 384.17976
Molecular Weight: 384.43
Elemental Analysis: C, 62.49; H, 6.29; N, 14.57; O, 16.65

Price and Availability

Size Price Availability Quantity
50.0mg USD 150.0 Same day
100.0mg USD 250.0 Same day
200.0mg USD 450.0 Same day
500.0mg USD 750.0 Same day
1.0g USD 1250.0 2 Weeks
2.0g USD 1950.0 2 Weeks
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Synonym: KW6002; KW 6002; KW-6002; Istradefylline; Nourianz.

IUPAC/Chemical Name: 8-[(E)-2-(3,4-dimethoxyphenyl)vinyl]-1,3-diethyl-7-methyl-3,7-dihydro-1H-purine-2,6-dione

InChi Key: IQVRBWUUXZMOPW-PKNBQFBNSA-N

InChi Code: InChI=1S/C20H24N4O4/c1-6-23-18-17(19(25)24(7-2)20(23)26)22(3)16(21-18)11-9-13-8-10-14(27-4)15(12-13)28-5/h8-12H,6-7H2,1-5H3/b11-9+

SMILES Code: O=C(N1CC)N(CC)C2=C(N(C)C(/C=C/C3=CC=C(OC)C(OC)=C3)=N2)C1=O

Appearance: Light green to green solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO.

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Certificate of Analysis:

Safety Data Sheet (SDS):

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.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Deutschländer AB. Treatment with istradefylline for postural abnormalities in Parkinson's disease. Neurol Neurochir Pol. 2019;53(4):239-241. doi: 10.5603/PJNNS.2019.0038. PubMed PMID: 31469906.

2: Fujioka S, Yoshida R, Nose K, Hayashi Y, Mishima T, Fukae J, Kitano K, Kikuchi H, Tsuboi Y. A new therapeutic strategy with istradefylline for postural deformities in Parkinson's disease. Neurol Neurochir Pol. 2019;53(4):291-295. doi: 10.5603/PJNNS.a2019.0036. Epub 2019 Aug 23. PubMed PMID: 31441493.

3: Iijima M, Orimo S, Terashi H, Suzuki M, Hayashi A, Shimura H, Mitoma H, Kitagawa K, Okuma Y. Efficacy of istradefylline for gait disorders with freezing of gait in Parkinson's disease: A single-arm, open-label, prospective, multicenter study. Expert Opin Pharmacother. 2019 Aug;20(11):1405-1411. doi: 10.1080/14656566.2019.1614167. Epub 2019 May 28. PubMed PMID: 31039621.

4: Nagayama H, Kano O, Murakami H, Ono K, Hamada M, Toda T, Sengoku R, Shimo Y, Hattori N. Effect of istradefylline on mood disorders in Parkinson's disease. J Neurol Sci. 2019 Jan 15;396:78-83. doi: 10.1016/j.jns.2018.11.005. Epub 2018 Nov 5. PubMed PMID: 30423541.

5: Takahashi M, Fujita M, Asai N, Saki M, Mori A. Safety and effectiveness of istradefylline in patients with Parkinson's disease: interim analysis of a post-marketing surveillance study in Japan. Expert Opin Pharmacother. 2018 Oct;19(15):1635-1642. doi: 10.1080/14656566.2018.1518433. Epub 2018 Oct 3. PubMed PMID: 30281377.

6: Yasuda Y. Reversible istradefylline-induced pleurothotonus in a patient with Parkinson's disease: A case report and literature review. eNeurologicalSci. 2018 Sep 10;13:5-7. doi: 10.1016/j.ensci.2018.09.001. eCollection 2018 Dec. PubMed PMID: 30258991; PubMed Central PMCID: PMC6153187.

7: Ishibashi K, Miura Y, Wagatsuma K, Toyohara J, Ishiwata K, Ishii K. Occupancy of adenosine A(2A) receptors by istradefylline in patients with Parkinson's disease using (11)C-preladenant PET. Neuropharmacology. 2018 Dec;143:106-112. doi: 10.1016/j.neuropharm.2018.09.036. Epub 2018 Sep 22. PubMed PMID: 30253174.

8: Torti M, Vacca L, Stocchi F. Istradefylline for the treatment of Parkinson's disease: is it a promising strategy? Expert Opin Pharmacother. 2018 Nov;19(16):1821-1828. doi: 10.1080/14656566.2018.1524876. Epub 2018 Oct 11. Review. PubMed PMID: 30232916.

9: Kataoka H, Sugie K. Does istradefylline really have a dystonic mechanism? J Neurol Sci. 2018 May 15;388:233-234. doi: 10.1016/j.jns.2018.03.020. Epub 2018 Mar 14. PubMed PMID: 29559176.

10: Suzuki K, Miyamoto T, Miyamoto M, Uchiyama T, Hirata K. Authors' reply to the comments of Kataoka et al. regarding "Could istradefylline be a treatment option for postural abnormalities in mid-stage Parkinson's disease?" J Neurol Sci. 2018 May 15;388:235-236. doi: 10.1016/j.jns.2018.03.019. Epub 2018 Mar 14. PubMed PMID: 29555107.

11: Nuermaimaiti M, Oyama G, Kasemsuk C, Hattori N. Istradefylline for Restless Legs Syndrome Associated with Parkinson's Disease. Tremor Other Hyperkinet Mov (N Y). 2018 Jan 8;8:521. doi: 10.7916/D86H5R1H. eCollection 2018. PubMed PMID: 29423337; PubMed Central PMCID: PMC5803507.

12: Suzuki K, Miyamoto T, Miyamoto M, Uchiyama T, Hirata K. Could istradefylline be a treatment option for postural abnormalities in mid-stage Parkinson's disease? J Neurol Sci. 2018 Feb 15;385:131-133. doi: 10.1016/j.jns.2017.12.027. Epub 2017 Dec 24. PubMed PMID: 29406892.

13: Sako W, Murakami N, Motohama K, Izumi Y, Kaji R. The effect of istradefylline for Parkinson's disease: A meta-analysis. Sci Rep. 2017 Dec 21;7(1):18018. doi: 10.1038/s41598-017-18339-1. PubMed PMID: 29269791; PubMed Central PMCID: PMC5740127.

14: Orr AG, Lo I, Schumacher H, Ho K, Gill M, Guo W, Kim DH, Knox A, Saito T, Saido TC, Simms J, Toddes C, Wang X, Yu GQ, Mucke L. Istradefylline reduces memory deficits in aging mice with amyloid pathology. Neurobiol Dis. 2018 Feb;110:29-36. doi: 10.1016/j.nbd.2017.10.014. Epub 2017 Oct 31. PubMed PMID: 29100987; PubMed Central PMCID: PMC5747997.

15: Matsuura K, Kajikawa H, Tabei KI, Satoh M, Kida H, Nakamura N, Tomimoto H. The effectiveness of istradefylline for the treatment of gait deficits and sleepiness in patients with Parkinson's disease. Neurosci Lett. 2018 Jan 1;662:158-161. doi: 10.1016/j.neulet.2017.10.018. Epub 2017 Oct 13. PubMed PMID: 29031781.

16: Yabe I, Kitagawa M, Takahashi I, Matsushima M, Sasaki H. The Efficacy of Istradefylline for Treating Mild Wearing-Off in Parkinson Disease. Clin Neuropharmacol. 2017 Nov/Dec;40(6):261-263. doi: 10.1097/WNF.0000000000000249. PubMed PMID: 28976411.

17: Mukai M, Uchimura T, Zhang X, Greene D, Vergeire M, Cantillon M. Effects of Rifampin on the Pharmacokinetics of a Single Dose of Istradefylline in Healthy Subjects. J Clin Pharmacol. 2018 Feb;58(2):193-201. doi: 10.1002/jcph.1003. Epub 2017 Sep 7. PubMed PMID: 28881378; PubMed Central PMCID: PMC5811788.

18: Suzuki K, Miyamoto M, Miyamoto T, Uchiyama T, Watanabe Y, Suzuki S, Kadowaki T, Fujita H, Matsubara T, Sakuramoto H, Hirata K. Istradefylline improves daytime sleepiness in patients with Parkinson's disease: An open-label, 3-month study. J Neurol Sci. 2017 Sep 15;380:230-233. doi: 10.1016/j.jns.2017.07.045. Epub 2017 Jul 29. PubMed PMID: 28870576.

19: Ko WKD, Camus SM, Li Q, Yang J, McGuire S, Pioli EY, Bezard E. An evaluation of istradefylline treatment on Parkinsonian motor and cognitive deficits in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated macaque models. Neuropharmacology. 2016 Nov;110(Pt A):48-58. doi: 10.1016/j.neuropharm.2016.07.012. Epub 2016 Jul 14. PubMed PMID: 27424102.

20: Kitta T, Yabe I, Takahashi I, Matsushima M, Sasaki H, Shinohara N. Clinical efficacy of istradefylline on lower urinary tract symptoms in Parkinson's disease. Int J Urol. 2016 Oct;23(10):893-894. doi: 10.1111/iju.13160. Epub 2016 Jul 8. PubMed PMID: 27388933.