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Istradefylline

Cat. No. M3188
Istradefylline Structure
Synonym:

KW-6002

Size Price Availability Quantity
5mg USD 90 In stock
25mg USD 300 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Istradefylline (KW-6002) is a selective adenosine A2A receptor (A2AR) antagonist with Ki of 2.2 nM. Oral administration of Istradefylline improves motor disability in MPTP-treated parkinsonian marmosets in a dose-dependent manner without provoking dyskinesia. Combination of Istradefylline with a low dose of L-DOPA or with the selective dopamine D2 receptor agonist quinpirole or the D1 receptor agonist SKF80723 produces an additive improvement in motor disability but not dyskinesia in MPTP-treated common marmosets. Blockade of A2AR by Istradefylline treatment rescues locomotor impairment in dopamine D2 receptor-deficient mice, with the level of expression of enkephalin and substance P reestablished to normal levels. Istradefylline treatment potentiates rotational behavior induced by dopaminergic drugs in hemi-Parkinsonian rats. Istradefylline treatment alone causes an approximately 20% reduction in the striatal levels of preproenkephalin mRNA, whereas neither the coadministration of KW-6002 and L-DOPA nor L-DOPA alone significantly alters the expression of this transcript in the dopamine-denervated striatum. Either alone or in combination with L-DOPA, Istradefylline does not have any modulatory effect on prodynorphin mRNA expression or FosB/DeltaFosB-like immunoreactivity in the dopamine-denervated striatum. Treatment with Istradefylline prevents the loss of dopaminergic striatal terminals and nigral cell bodies and inhibits the nigral microglia activation in MPTP treated mice. A Phase II study of Istradefylline (monotherapy) and a Phase III study of Istradefylline in combination with levodopa for the treatment of Parkinson's disease have been completed.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Common marmosets (Callithrix jacchus) with MPTP treatment
Formulation Suspended in 0.3% Tween-80 and 10% sucrose solution
Dosages 10 mg/kg
Administration Oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 384.43
Formula C20H24N4O4
CAS Number 155270-99-8
Purity >99%
Solubility DMSO
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Istradefylline, KW-6002 supplier, Adenosine Receptor, inhibitors

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