GlpBio

Tozadenant

目录号: GC15973纯度: >99.50%同义词: 4-羟基-N-[4-甲氧基-7-(4-吗啉基)-2-苯并噻唑基]-4-甲基-1-哌啶甲酰胺,SYN-115;SYN115;SYN 115
An adenosine A2A receptor antagonist
Tozadenant
Cas No.: 870070-55-6
规格价格库存数量操作
5mg¥280.00现货
1
10mg¥455.00现货
1
25mg¥864.00现货
1
50mg¥1,400.00现货
1
100mg¥2,240.00现货
1
10mM (in 1mL DMSO)¥251.00现货
1
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文献被引

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    187(9):2288-2304 (2024)
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产品描述 Description

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:

[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 Aug;13(8):767-76

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实验参考方法 Experimental Reference Method

Human experiment [1]:

Patients

Patients with Parkinson’s disease.

Dosage form

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

Applications

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.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
870070-55-6
同义词
4-羟基-N-[4-甲氧基-7-(4-吗啉基)-2-苯并噻唑基]-4-甲基-1-哌啶甲酰胺,SYN-115;SYN115;SYN 115
化学名
4-hydroxy-N-(4-methoxy-7-morpholin-4-yl-1,3-benzothiazol-2-yl)-4-methylpiperidine-1-carboxamide
SMILES
CC1(CCN(CC1)C(=O)NC2=NC3=C(C=CC(=C3S2)N4CCOCC4)OC)O
分子式
C19H26N4O4S
分子量
406.5 g/mol
溶解性
≥ 20.35 mg/mL in DMSO
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol