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Tozadenant

Catalog No. T7320 CAS 870070-55-6

Synonyms: SYN115

Tozadenant (SYN115) is an adenosine A2A receptor antagonist(Ki of 11.5 nM and 6 nM on human and rhesus,respectively)

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Tozadenant, CAS 870070-55-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 38.00
2 mg	In stock	$ 54.00
5 mg	In stock	$ 89.00
10 mg	In stock	$ 147.00
25 mg	In stock	$ 275.00
50 mg	In stock	$ 478.00
100 mg	In stock	$ 689.00
500 mg	In stock	$ 1,480.00
1 mL * 10 mM (in DMSO)	In stock	$ 97.00

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Purity: 98%

Biological Description

Chemical Properties

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Description	Tozadenant (SYN115) is an adenosine A2A receptor antagonist(Ki of 11.5 nM and 6 nM on human and rhesus,respectively)
Targets&IC50	A2A receptor (rhesus):6 nM(Ki), A2A receptor (human):11.5 nM(Ki)
In vivo	When compared to the drugs tested alone, Radiprodil and Tozadenant combination led to a significant increase of motor activity and an improvement of motor disability in MPTP-treated marmosets. In addition, the motor restoration brought about by the combination was almost completely devoid of dyskinesia[1]
Animal Research	Before initiating the Radiprodil & Tozadenant combination experiment, 14 primates were challenged with a dose of 8 mg/kg (po) of L-Dopa and behaviour was recorded for 5 hours. This "Pre-L-Dopa-test" was used to select the 12 subjects required for the study. Their response to the L-Dopa challenge was subsequently used as a comparator to the ensuing response to the different drug treatments and combinations. The effects of the drugs alone or in combination were assessed after acute oral gavage.This experiment investigated the effects on motor deficits of Radiprodil plus Tozadenant twice daily at an interval of 5 hrs according to a modified Latin square design in n = 12 MPTP-treated marmosets. At the time of the second drugs administration a novel object (cotton reel, table tennis ball) was placed into the cage. The four different treatments were (1) Tozadenant (150 mg/kg) plus Radiprodil (2.0 mg/kg), (2) Tozadenant (150 mg/kg) plus vehicle, (3) Radiprodil (2.0 mg/kg) plus vehicle, (4) vehicle[1].

Synonyms	SYN115
Molecular Weight	406.5
Formula	C19H26N4O4S
CAS No.	870070-55-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (123.00 mM)

References and Literature

1. Anne M , Jean-Marie N , Sarah R , et al. Antiparkinsonian effects of the \"Radiprodil and Tozadenant\" combination in MPTP-treated marmosets[J]. PLOS ONE, 2017, 12(8):e0182887-. 2. Hauser R A , Olanow C W , Kieburtz K D , et al. Tozadenant (SYN115) in patients with Parkinson\"s disease who have motor fluctuations on levodopa: a phase 2b, double-blind, randomised trial[J]. The Lancet Neurology, 2014, 13(8):767-776. 3. Barret O , Hannestad J , Alagille D , et al. Adenosine 2A Receptor Occupancy by Tozadenant and Preladenant in Rhesus Monkeys[J]. Journal of Nuclear Medicine, 2014, 55(10):1712-1718.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Neurodegenerative Disease Compound Library Anti-Parkinson's Disease Compound Library

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Keywords

Tozadenant 870070-55-6 GPCR/G Protein Neuroscience Adenosine Receptor P1 receptor SYN 115 SYN115 SYN-115 Inhibitor inhibit inhibitor

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