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Tozadenant

现货
Catalog No.
A3885
腺苷2A受体拮抗剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 2,250.00
现货
10mg
¥ 2,050.00
现货
50mg
¥ 5,850.00
现货
250mg
¥ 14,390.00
Ship with 10-15 days

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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.

Chemical Properties

StorageStore at -20°C
M.Wt406.5
Cas No.870070-55-6
FormulaC19H26N4O4S
SynonymsSYN-115;SYN115;SYN 115
Solubility≥20.35 mg/mL in DMSO, <2.3 mg/mL in EtOH, <2.31 mg/mL in H2O
Chemical Name4-hydroxy-N-(4-methoxy-7-morpholin-4-yl-1,3-benzothiazol-2-yl)-4-methylpiperidine-1-carboxamide
SDFDownload SDF
Canonical SMILESCC1(CCN(CC1)C(=O)NC2=NC3=C(C=CC(=C3S2)N4CCOCC4)OC)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

临床试验 [1]:

患者

帕金森病患者

剂量

60、120、180或240 mg,每天两次,持续12周

实验结果

剂量为120 mg和180 mg的tozadenant每日两次给药增加了平均日总接触时间和I-III部分的总UPDRS评分。此外,Tozadenant显著改善CGI-S和CGI-I得分。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

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.

生物活性

描述 Tozadenant是腺苷A2A受体的拮抗剂。
靶点 adenosine A2A receptor          
IC50            

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