Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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Purity: ≥98%
Istradefylline (formerly KW6002; KW 6002; KW-6002; Nourianz), a caffeine derivative, is an orally bioavailable and selective adenosine A2A receptor (A2AR) antagonist with anti-PD (Parkinson's disease) effects. It suppresses the A2A receptor (A2AR) with a Ki of 2.2 nM. It is authorized for use as a supplement to levodopa/carbidopa in Parkinson's disease patients who are having "off" episodes. Istradefylline lessens the "off" periods brought on by continuous administration of the Parkinson's disease medication levodopa.
Targets |
Adenosine A2A receptor ( Ki = 2.2 nM )
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ln Vitro |
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ln Vivo |
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Cell Assay |
The human adenosine A1 or A2A receptor is permanently expressed in a CHO cell line that is cultured in α-MEM supplemented with 10% (v/v) fetal bovine serum, 50 U/mL penicillin, and 50 μg/mL streptomycin. In a 5% CO2 environment, cells are grown at 37°C. These cells are cultivated for twenty-four hours after being seeded at a density of 15,000 cells per well on black 96-well assay plates.
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Animal Protocol |
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References |
Molecular Formula |
C20H24N4O4
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Molecular Weight |
384.43
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Exact Mass |
384.18
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Elemental Analysis |
C, 62.49; H, 6.29; N, 14.57; O, 16.65
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CAS # |
155270-99-8
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Related CAS # |
Istradefylline-13C,d3; 2749234-46-4
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Appearance |
Light green to green solid powder
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SMILES |
CCN1C2=C(C(=O)N(C1=O)CC)N(C(=N2)/C=C/C3=CC(=C(C=C3)OC)OC)C
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InChi Key |
IQVRBWUUXZMOPW-PKNBQFBNSA-N
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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+
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Chemical Name |
8-[(E)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methylpurine-2,6-dione
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: 30% Propylene glycol , 5% Tween 80 , 65% D5W: 30mg/mL  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.6013 mL | 13.0063 mL | 26.0125 mL | |
5 mM | 0.5203 mL | 2.6013 mL | 5.2025 mL | |
10 mM | 0.2601 mL | 1.3006 mL | 2.6013 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05333549 | Recruiting | Drug: Istradefylline | Parkinson Disease Cognitive Impairment |
Virginia Commonwealth University | July 18, 2022 | Phase 2 |
NCT05182151 | Active Recruiting |
Drug: Istradefylline 40 mg | Parkinson Disease Apathy |
Medical University of South Carolina |
April 6, 2021 | N/A |
NCT05217498 | Not yet recruiting | Drug: Istradefylline Device: low oxygen therapy |
Spinal Cord Injuries Myelopathy |
Randy Trumbower, PT, PhD | September 1, 2024 | Phase 1 Phase 2 |
NCT05377424 | Recruiting | Drug: Consume 20mg of istradefylline Other: Low Oxygen therapy |
ALS | University of Florida | June 21, 2022 | Phase 1 Phase 2 |