My cart
In the shopping cart is not goods, to choose and buy!
  • Product Name
  • Size
  • Quantity
  • Amount
    Selected items : 0 pieces Total : CHECK OUT()
    Istradefylline (KW-6002)
    Istradefylline (KW-6002)

    Price:
    Market Price:

    This product is for research use only, not for human use. We do not sell to patients.
    Number: - + Pieces(InventoryPieces)
    InvivoChem Cat #: V1483
    CAS #: 155270-99-8Purity ≥98%

    Description: Istradefylline (also known as KW-6002) is a potent, orally bioavailable and selective adenosine A2A receptor (A2AR) antagonist with Ki of 2.2 nM. It has been found to be useful in the treatment of Parkinson's disease. The affinity of KW-6002 for the A2AR is 70-fold greater than that for the A1 receptor. The binding affinities (Ki) of KW-6002 for human A1 receptor and A2A receptor are >287 nM and 9.12 nM, respectively. Istradefylline reduces dyskinesia resulting from long-term treatment with classical antiparkinson drugs such as levodopa. Istradefylline is an analog of caffeine.

    References: J Neurosci. 2001 May 15;21(10):RC143; Psychopharmacology (Berl). 1999 Nov;147(1):90-5.

    Related CAS: 160434-48-0 (4-Desmethyl Istradefylline)

    Customer Validation
    Official Supplier of
    • VE
    • OF
    • YALE
    • hhmi
    • 香港大学
    Related Products
    Publications Citing InvivoChem Products
    • Physicochemical and Storage Information
    • Protocol
    • Quality Control Documentation
    • Related Biological Data
    • Customer Review
    Molecular Weight (MW)384.43
    FormulaC20H24N4O4
    CAS No.155270-99-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 6 mg/mL (15.6 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)30% Propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL  
    SynonymsKW-6002; KW6002; KW 6002; 


    • Molarity Calculator
    • Dilution Calculator
    • The molarity calculator equation

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

      • Mass
      • Concentration
      • Volume
      • Molecular Weight *
      • =
      • ×
      • ×
    • The dilution calculator equation

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

      This equation is commonly abbreviated as: C1V1 = C2V2

      • Concentration (start)
      • ×
      • Volume (start)
      • =
      • Concentration (final)
      • ×
      • Volume (final)
      • ×
      • =
      • ×
      • C1
      •  
      • V1
      •  
      • C2
      •  
      • V2
    In Vitro

    In vitro activity: The affinity of Istradefylline for the A2AR is 70-fold greater than that for the A1 receptor with Ki of 2.2 nM versus 150 NM. Exposure of primary rat striatal astrocytes to Istradefylline results in concentration-dependent abolition of bFGF induction of astrogliosis in vitro. Binding affinities (Ki) of Istradefylline for A1 receptor, A2A receptor, and A3 receptor in human are >287 nM, 9.12 nM, and >681 nM, respectively, for A1 receptor and A2A receptor in rat 50.9 nM and 1.57 nM, respectively, and for A1 receptor and A2A receptor in mouse 105.02 nM and 1.87 nM, respectively.


    Cell Assay: 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.

    In VivoIstradefylline reverses CGS21680-induced and reserpine-induced catalepsy with 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. Administration of Istradefylline in combination with L-dopa (50 mg/kg) exerts prominent effects on haloperidol-induced and reserpine-induced catalepsy. Oral administration of Istradefylline at 10 mg/kg to MPTP-treated common marmosets produces an increase in locomotor activity to approximately twice that of control and improves motor disability. Administration of Istradefylline (10 mg/kg, po, 90 minutes before SKF80723/quinpirole/L-DOPA) in combination with SKF80723 (1 mg/kg, ip), quinpirole (0.06 mg/kg ip), or L-DOPA (2.5 mg/kg po) produces a significant additive effect on locomotor activity and improvement of motor disability but not dyskinesia. In the MPTP mice model, Istradefylline significantly attenuates striatal dopamine depletion under various conditions. Pretreatment with Istradefylline (3.3 mg/kg, i.p.) before a single dose of MPTP attenuates the partial dopamine and DOPAC depletions measured in striata 1 week later. Oral administration of Istradefylline protects against the loss of nigral dopaminergic neuronal cells induced by 6-hydroxydopamine in rats, and prevents the functional loss of dopaminergic nerve terminals in the striatum and the ensuing gliosis caused by MPTP in mice. Chronic Istradefylline treatment does not improve the reversal deficits in dopamine-depleted rats. The tremulous jaw movements induced by pimozide are significantly reduced by co-administration of either Istradefylline or tropicamide. Pimozide-induced increases in ventrolateral striatal c-Fos expression are reduced by a behaviorally effective dose of Istradefylline, in contrast to tropicamide by which c-Fos expression in pimozide-treated rats is actually increased.
    Animal modelCommon marmosets (Callithrix jacchus) with MPTP treatment
    Formulation & DosageSuspended in 0.3% Tween-80 and 10% sucrose solution; 10 mg/kg; p.o.
    References

    J Neurosci. 2001 May 15;21(10):RC143; Psychopharmacology (Berl). 1999 Nov;147(1):90-5.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    评论

      Home Prev Next Last page / pices

      发评论

      ×
      Your information is safe with us. * Required Fields.
      Products are for research use only;  We do not sell to patients
      Tel: 1-708-310-1919
      Fax: 1-708-557-7486
      Subscribe to our E-newsletter
      • Name*
      • *
      • E-mail*
      • *
      • instructions:
      • *
      Copyright 2020 InvivoChem LLC | All Rights Reserved
      prompt
      Do you confirm the receipt?