Tozadenant
(Synonyms: 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) 目录号 : GC15973
An adenosine A2A receptor antagonist
Cas No.:870070-55-6
Sample solution is provided at 25 µL, 10mM.
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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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| Human experiment [1]: | |
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Patients |
Patients with Parkinson’s disease. |
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Dosage form |
60, 120, 180, or 240 mg twice daily for 12 weeks. |
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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. |
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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. |
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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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| Cas No. | 870070-55-6 | SDF | |
| 别名 | 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 | ||
| Canonical SMILES | CC1(CCN(CC1)C(=O)NC2=NC3=C(C=CC(=C3S2)N4CCOCC4)OC)O | ||
| 分子式 | C19H26N4O4S | 分子量 | 406.5 |
| 溶解度 | ≥ 20.35 mg/mL in DMSO | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.46 mL | 12.3001 mL | 24.6002 mL |
| 5 mM | 0.492 mL | 2.46 mL | 4.92 mL |
| 10 mM | 0.246 mL | 1.23 mL | 2.46 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet