2. GPCR/G Protein
  3. Adenosine Receptor
  4. Istradefylline

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.

CAS No. : 155270-99-8

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Customer Review

Based on 16 publication(s) in Google Scholar

Other Forms of Istradefylline:

Istradefylline Related Antibodies

Top Publications Citing Use of Products

    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).

    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.

    View All Adenosine Receptor Isoform Specific Products:

    View All Isoforms
    Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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.

    IC50 & Target

    Ki: 2.2 nM (adenosine A2A receptor)
    Cellular Effect
    Cell Line Type Value Description References
    CHO IC50
    5250 nM
    Compound: 2, KW 6002
    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
    		[PMID: 23602401]
    In Vitro

    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.

    Istradefylline Related Antibodies
    In Vivo

    Istradefylline (3.3 mg/kg, i.p.) treatment before a single dose of MPTP attenuates the partial dopamine and DOPAC depletions measured in striata 1 week later[1]. Istradefylline reverses CGS21680-induced and reserpine-induced catalepsy with an ED50 of 0.05 mg/kg and 0.26 mg/kg, respectively. Istradefylline is over 10 times as potent in these models compared to other adenosine antagonists and dopamine agonist drugs. Istradefylline combined with L-dopa cuases potent effects on haloperidol-induced and reserpine-induced catalepsy[2]. Istradefylline (10 mg/kg, p.o.) results an increase in locomotor activity to approximately twice that of control and improves motor disability in MPTP-treated common marmosets. Istradefylline (10 mg/kg, p.o.) in combination with SKF80723, quinpirole, or L-DOPA produces a significant additive effect on locomotor activity and improvement of motor disability but not dysKinesia[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    384.43

    Formula

    C20H24N4O4
    CAS No.
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    O=C1C2=C(N=C(/C=C/C3=CC(OC)=C(OC)C=C3)N2C)N(CC)C(N1CC)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    Volume (start)

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    In Vivo:

    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.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

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    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
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    +
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    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Purity & Documentation

    Purity: 99.89%

    SDS (479 KB)

    COA (248 KB) RP-HPLC (266 KB) MS (176 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [5]

    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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    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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    Istradefylline Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Istradefylline155270-99-8KW-6002KW6002KW 6002Adenosine ReceptorP1 receptorInhibitorinhibitorinhibit

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