Tozadenant
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Tozadenant (SYN115)是一种可口服的和选择性的腺苷A2A受体拮抗剂。
在帕金森病动物模型中,tozadenant提高运动神经元的功能。Tozadenant(60 mg,2次/天)与失能时间的显著减少不相关,而tozadenant(240 mg,2次/天)与由于不良事件(17/84患者[20%])而逐渐增加的停药率相关。Tozadenant在120或180 mg,每天2次的剂量下有效减少失能时间,且耐受性良好。灌注MRI显示,tozadenant显著抑制局部脑血流,最重要的下降发生在双侧丘脑。
参考文献:
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.
Storage | Store at -20°C |
M.Wt | 406.5 |
Cas No. | 870070-55-6 |
Formula | C19H26N4O4S |
Synonyms | SYN-115;SYN115;SYN 115 |
Solubility | insoluble in EtOH; insoluble in H2O; ≥20.35 mg/mL in DMSO |
Chemical Name | 4-hydroxy-N-(4-methoxy-7-morpholin-4-yl-1,3-benzothiazol-2-yl)-4-methylpiperidine-1-carboxamide |
SDF | Download SDF |
Canonical SMILES | CC1(CCN(CC1)C(=O)NC2=NC3=C(C=CC(=C3S2)N4CCOCC4)OC)O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
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. |
描述 | Tozadenant是腺苷A2A受体的拮抗剂。 | |||||
靶点 | adenosine A2A receptor | |||||
IC50 |
质量控制和MSDS
- 批次: