Istradefylline
Based on 16 publication(s) in Google Scholar
Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.
For research use only. We do not sell to patients.
- Purity: 99.89%
- CAS No.: 155270-99-8
- Formula: C20H24N4O4
- Molecular Weight:384.43
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Istradefylline
More- Cancer Res. 2023 Jul 5;83(13):2248-2261. [Abstract]
- Int J Oral Sci. 2024 Jun 18;16(1):46. [Abstract]
- J Pharm Anal. 2022 Oct;12(5):725-732. [Abstract]
- Phytomedicine. 2026 May:154:158030. [Abstract]
- EMBO Rep. 2022 Jun 7;23(6):e53932. [Abstract]
- Pharmaceutics. 2023 Jul 8;15(7):1909. [Abstract]
- Front Pharmacol. 2020 Aug 7;11:1212. [Abstract]
- Invest Ophthalmol Vis Sci. 2026 Jan 5;67(1):15. [Abstract]
- Mol Pharm. 2025 Oct 6;22(10):6067-6082. [Abstract]
- J Lipid Res. 2025 Jan 21:100746. [Abstract]
- Neurochem Int. 2021 Feb:143:104935. [Abstract]
- J Neurochem. 2019 Aug;150(3):282-295. [Abstract]
- Sci Rep. 2025 Nov 20;15(1):41110. [Abstract]
- ACS Chem Neurosci. 2024 Feb 7;15(3):645-655. [Abstract]
- J Pharm Sci. 2025 Feb;114(2):1444-1454. [Abstract]
- Iran J Basic Med Sci. 2021 Oct;24(10):1380-1387. [Abstract]
Customer Validation & Images
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IF
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In Vivo Efficacy Study
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Cell Proliferation/Viability Assay
All Adenosine Receptor Isoforms
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Biological Activity
Ki: 2.2 nM (adenosine A2A receptor)
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
5250 nM
Compound: 2, KW 6002
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Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
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[PMID: 23602401] |
Istradefylline has 70-fold greater affinity for the A2AR than the A1 receptor with Ki of 2.2 nM versus 150 nM[1]. Istradefylline causes concentration-dependent abolition of bFGF induction of astrogliosis in primary rat striatal astrocytes[4]. Istradefylline binds to A1 receptor, A2A receptor, and A3 receptor in human with Kis of >287 nM, 9.12 nM, and >681 nM, respectively, 50.9 nM and 1.57 nM for A1 receptor and A2A receptor in rat, 105.02 nM and 1.87 nM for A1 receptor and A2A receptor in mouse, respectively[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 155270-99-8
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Appearance Solid
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Molecular Weight 384.43
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Formula C20H24N4O4
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Color Off-white to yellow
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SMILES
O=C1C2=C(N=C(/C=C/C3=CC(OC)=C(OC)C=C3)N2C)N(CC)C(N1CC)=O
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Synonyms
KW-6002
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (16)
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Journal Impact Factor
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Most Recent
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Cancer Res
Caffeine supplementation and FOXM1 inhibition enhance the antitumor effect of statins in neuroblastoma. [Abstract]2023 Jul 5;83(13):2248-2261. PMID: 37057874
Istradefylline purchased from MedChemExpress. Usage Cited in: Cancer Res. 2023 Jul 5;83(13):2248-2261. [Abstract]
Immunoblot analysis showed that the adenosine receptor antagonist KW6002 (Istradefylline: 5 μM) inhibited simvastatin-induced processing of Srebp2 in CHO-K1 cells.
Istradefylline purchased from MedChemExpress. Usage Cited in: Cancer Res. 2023 Jul 5;83(13):2248-2261. [Abstract]
Neuroblastoma cell lines were treated with DMSO, KW6002 (Istradefylline: 5 μM), caffeine, simvastatin, or simvastatin in combination with KW6002 or caffeine for 48 hours before cell growth was measured.
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Int J Oral Sci
Nociceptive adenosine A2A receptor on trigeminal nerves orchestrates CGRP release to regulate the progression of oral squamous cell carcinoma. [Abstract]2024 Jun 18;16(1):46. PMID: 38886342
Istradefylline purchased from MedChemExpress. Usage Cited in: Int J Oral Sci. 2024 Jun 18;16(1):46. [Abstract]
Phosphorylation of CREB and total CREB in trigeminal ganglia of mice carrying HSC3 tumor xenograft and tumor-bearing mice treated with 6 mg/kg KW6002 (Istradefylline) for 3 h.
Istradefylline purchased from MedChemExpress. Usage Cited in: Int J Oral Sci. 2024 Jun 18;16(1):46. [Abstract]
Istradefylline (6 mg/kg KW6002). Represented immunostaining of CGRP (red, arrowheads) in TRPV1+ neuronal niche (green, circled 1 000 µm2). The curves in the upper panels delineated the tumor area (T, blue).
Istradefylline purchased from MedChemExpress. Usage Cited in: Int J Oral Sci. 2024 Jun 18;16(1):46. [Abstract]
In vivo growth of HSC3 xenograft in nontreated mice and those treated with 6 mg/kg KW6002 (Istradefylline).
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J Pharm Anal
Screening of immune cell activators from Astragali Radix using a comprehensive two-dimensional NK-92MI cell membrane chromatography/C18 column/time-of-flight mass spectrometry system. [Abstract]2022 Oct;12(5):725-732. PMID: 36320599 -
Phytomedicine
Parthenolide inhibits methamphetamine-induced depressive-like behavior by targeting ADORA2A. [Abstract]2026 May:154:158030. PMID: 41795299 -
EMBO Rep
2022 Jun 7;23(6):e53932. PMID: 35403787 -
Pharmaceutics
Projection of Target Drug Particle Size in Oral Formulations Using the Refined Developability Classification System (rDCS). [Abstract]2023 Jul 8;15(7):1909. PMID: 37514095 -
Front Pharmacol
Bufei Yishen Formula Restores Th17/Treg Balance and Attenuates Chronic Obstructive Pulmonary Disease via Activation of the Adenosine 2a Receptor. [Abstract]2020 Aug 7;11:1212. PMID: 32848801 -
Invest Ophthalmol Vis Sci
2026 Jan 5;67(1):15. PMID: 41533917 -
Mol Pharm
Canine Mdr1 Knockout MDCK Cells Reliably Estimate Human Small Intestinal Permeability (Peff) and Fraction Absorbed (fa). [Abstract]2025 Oct 6;22(10):6067-6082. PMID: 40914889 -
J Lipid Res
Taurine alleviates dysfunction of cholesterol metabolism under hyperuricemia by inhibiting A2AR-SREBP-2/CREB/HMGCR axis. [Abstract]2025 Jan 21:100746. PMID: 39848583 -
Neurochem Int
2021 Feb:143:104935. PMID: 33301817 -
J Neurochem
Metabolomics-driven identification of adenosine deaminase as therapeutic target in a mouse model of Parkinson's disease. [Abstract]2019 Aug;150(3):282-295. PMID: 31121068 -
Sci Rep
Biphasic actions of the adenosine A2a receptor antagonist istradefylline in mice with obstructive uropathy. [Abstract]2025 Nov 20;15(1):41110. PMID: 41266603 -
ACS Chem Neurosci
2024 Feb 7;15(3):645-655. PMID: 38275568 -
J Pharm Sci
Advantages of the refined Developability Classification System (rDCS) in early discovery. [Abstract]2025 Feb;114(2):1444-1454. PMID: 39725230 -
Iran J Basic Med Sci
A2 adenosine receptor contributes to the development of cow's milk protein allergy via regulating regulatory T cells. [Abstract]2021 Oct;24(10):1380-1387. PMID: 35096296
Solvent & Solubility
DMSO : 25.33 mg/mL (65.89 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
A CHO cell line permanently expressing the human adenosine A1or A2A receptor is cultured in α-MEM supplemented with 10% (v/v) fetal bovine serum, 50 U/mL penicillin, and 50 μg/mL streptomycin. Cells are grown at 37°C in an environment of 5% CO2. These cells are seeded on black 96-well assay plates at a density of 15,000 cells/well, and then they are cultured for 24 h.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
The animals are housed either in pairs or alone under standard conditions at a temperature of 24-26°C and 50-60% relative humidity using a 12-h light-dark cycle. Diet consisted of standard food pellets, fresh fruit, and Mazuri marmoset jelly. The animals are treated with MPTP in a dose of 2.0 mg/kg sc daily for 5 days. Following MPTP treatment the animals are allowed to recover from the acute effects over a period of some 6-8 weeks. During MPTP treatment and throughout the following weeks, the animals are hand-fed with Mazuri marmoset jelly and fresh fruit puree until they are able to maintain them-selves. Prior to behavioral testing, from 6-8 weeks to 8 months after exposure to MPTP, all animals show a marked reduction of basal locomotor activity, slower and less coordinated movements, abnormal postures of some parts of the body, and reduced checKing movements and eye blinks. Istradefylline (KW-6002) is suspended in 0.3% Tween-80 and 10% sucrose solution and administered in a final volume of 2.0 mL/kg body weight by oral gavage.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Portuguese - PT (479 KB)
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Handling Instructions (2659 KB)
References
[1]. Chen JF, et al. Neuroprotection by caffeine and A(2A) adenosine receptor inactivation in a model of Parkinson's disease. J Neurosci. 2001 May 15;21(10):RC143. [Content Brief]
[2]. Shiozaki S, et al. Actions of adenosine A2A receptor antagonist KW-6002 on drug-induced catalepsy and hypokinesia caused by reserpine or MPTP. Psychopharmacology (Berl). 1999 Nov;147(1):90-5. [Content Brief]
[3]. Kanda T, et al. Combined use of the adenosine A(2A) antagonist KW-6002 with L-DOPA or with selective D1 or D2 dopamine agonists increases antiparkinsonian activity but not dyskinesia in MPTP-treated monkeys. Exp Neurol. 2000 Apr;162(2):321-7. [Content Brief]
[4]. Brambilla R, et al. Blockade of A2A adenosine receptors prevents basic fibroblast growth factor-induced reactive astrogliosis in rat striatal primary astrocytes. Glia. 2003 Aug;43(2):190-4. [Content Brief]
[5]. Mihara T, et al. Pharmacological characterization of a novel, potent adenosine A1 and A2A receptor dual antagonist, 5-[5-amino-3-(4-fluorophenyl)pyrazin-2-yl]-1-isopropylpyridine-2(1H)-one (ASP5854), in models of Parkinson's disease and cognition. J Pharm [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6013 mL | 13.0063 mL | 26.0125 mL | 65.0313 mL |
| 5 mM | 0.5203 mL | 2.6013 mL | 5.2025 mL | 13.0063 mL | |
| 10 mM | 0.2601 mL | 1.3006 mL | 2.6013 mL | 6.5031 mL | |
| 15 mM | 0.1734 mL | 0.8671 mL | 1.7342 mL | 4.3354 mL | |
| 20 mM | 0.1301 mL | 0.6503 mL | 1.3006 mL | 3.2516 mL | |
| 25 mM | 0.1041 mL | 0.5203 mL | 1.0405 mL | 2.6013 mL | |
| 30 mM | 0.0867 mL | 0.4335 mL | 0.8671 mL | 2.1677 mL | |
| 40 mM | 0.0650 mL | 0.3252 mL | 0.6503 mL | 1.6258 mL | |
| 50 mM | 0.0520 mL | 0.2601 mL | 0.5203 mL | 1.3006 mL | |
| 60 mM | 0.0434 mL | 0.2168 mL | 0.4335 mL | 1.0839 mL |
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