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    Istradefylline (KW-6002)
    Istradefylline (KW-6002)

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

    Description: 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 inhibits A2A receptor (A2AR) with a Ki of 2.2 nM. It has been approved to be used as an add-on treatment to levodopa/carbidopa for patients with Parkinson's disease experiencing 'off' episodes. Istradefylline reduces 'off' periods resulting from long-term treatment with the antiparkinson drug levodopa. 

    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)

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    Molecular Weight (MW)384.43
    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; 

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    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.

    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.


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