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Tozadenant
Adenosine 2a receptor antagonist,novel and selective

Tozadenant

Catalog No. A3885
Size Price Stock Qty
10mg $205.00 In stock
50mg $585.00 In stock
250mg $1,439.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Tozadenant

Biological Activity

Description Tozadenant is an antagonist of adenosine A2A receptor.
Targets adenosine A2A receptor          
IC50            

Protocol

Human experiment [1]:

Patients

Patients with Parkinson’s disease.

Dosage form

60, 120, 180, or 240 mg twice daily for 12 weeks.

Application

Tozadenant increases mean daily total on-time and improved total UPDRS scores for parts I-III in the combined tozadenant 120 mg twice-daily and 180 mg twice-daily group and in the 120 mg twice-daily group. Also, tozadenant significantly improved CGI-S and CGI-I scores.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Hauser RA, Olanow CW, Kieburtz KD, et al. Tozadenant (SYN115) in patients with Parkinson's disease who have motor fluctuations on levodopa: a phase 2b, double-blind, randomised trial. Lancet Neurol,2014, 13(8): 767-776.

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Chemical Properties

Cas No. 870070-55-6 SDF Download SDF
Synonyms SYN-115;SYN115;SYN 115
Chemical Name 4-hydroxy-N-(4-methoxy-7-morpholin-4-yl-1,3-benzothiazol-2-yl)-4-methylpiperidine-1-carboxamide
Canonical SMILES CC1(CCN(CC1)C(=O)NC2=NC3=C(C=CC(=C3S2)N4CCOCC4)OC)O
Formula C19H26N4O4S M.Wt 406.5
Solubility Soluble in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

Tozadenant (SYN115) is an orally active, selective adenosine A2A receptor antagonist.

In animal models of Parkinson’s disease, tozadenant improves motor neuron function.

Tozadenant (60 mg twice daily) was not associated with a signi?cant reduction in o?-time, and tozadenant (240 mg twice daily) was associated with an increased rate of discontinuation because of adverse events (17 of 84 patients [20%]). Tozadenant at dose of 120 or 180 mg twice daily was e?ective at reducing o?-time and was generally well tolerated. Further investigation of tozadenant treatment in phase 3 trials is guaranteed . Perfusion MRI showed that tozadenant induced highly signi?cant suppressed in regional cerebral blood ?ow, with the most important decreases occurring in bilateral thalami.

Reference:
Hauser RA, Olanow CW, Kieburtz KD et al.  Tozadenant (SYN115) in patients with Parkinson's disease who have motor fluctuations on levodopa: a phase 2b, double-blind, randomised trial. Lancet Neurol. 2014 Aug;13(8):767-76.