Tozadenant是一种选择性的腺苷 A2A 受体拮抗剂,对人 A2A 和恒河猴 A2A 的 Ki 值分别为 11.5 nM 和 6 nM,能够改善帕金森病动物模型中的运动功能。


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| 产品名称 | Adenosine Receptor ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| ZM241385 | ✔ | 99%+ | |||||||||||||||||
| Istradefylline |
+++
Adenosine A2A receptor, Ki: 2.2 nM |
98% | |||||||||||||||||
| Reversine |
+
human A3 adenosine receptor, Ki: 0.66 μM |
98% | |||||||||||||||||
| SCH58261 |
++++
bovine A2a, Ki: 2.0 nM rat A2a, Ki: 2.3 nM |
99%+ | |||||||||||||||||
| A2A receptor antagonist 1 |
++
A1R, Ki: 264 nM A2AR, Ki: 4 nM |
99%+ | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 描述 | Tozadenant is an adenosine A2A receptor antagonist, with Ki of 11.5 nM on human A2A and 6 nM on rhesus A2A. |
| Concentration | Treated Time | Description | References | |
| Rat brain slices | 12 kBq/mL (0.24 nM) | 30 min | Evaluate A2A receptor-specific binding of [11C]tozadenant in rat brain slices, showing pronounced accumulation in the striatum with specific binding of approximately 68%. | Molecules. 2024 Feb 29;29(5):1089 |
| Pig brain slices | 12 kBq/mL (0.24 nM) | 30 min | Evaluate A2A receptor-specific binding of [11C]tozadenant in pig brain slices, showing pronounced accumulation in the striatum with specific binding of approximately 68%. | Molecules. 2024 Feb 29;29(5):1089 |
| Administration | Dosage | Frequency | Description | References | ||
| Pigs | Healthy pigs | Intravenous injection | 2.5 mg/kg | Single bolus followed by continuous infusion | To evaluate the A2A adenosine receptor-specific binding of [18F]FLUDA in pig brain, results showed that tozadenant significantly decreased VT and BPND values in the striatum. | Pharmaceuticals (Basel). 2022 Apr 22;15(5):516 |
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00783276 | Cocaine Dependence | Early Phase 1 | Completed | - | United States, Texas ... 展开 >> University of Texas Health Science Center at Houston Houston, Texas, United States, 77030 收起 << |
| NCT01283594 | Parkinson's Disease | Phase 2 Phase 3 | Completed | - | - |
| NCT00605553 | Parkinson's Disease | Phase 2 | Completed | - | United States, Missouri ... 展开 >> Washington University St. Louis Saint Louis, Missouri, United States, 63110 收起 << |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.46mL 0.49mL 0.25mL |
12.30mL 2.46mL 1.23mL |
24.60mL 4.92mL 2.46mL |
|
| CAS号 | 870070-55-6 |
| 分子式 | C19H26N4O4S |
| 分子量 | 406.5 |
| SMILES Code | COC1=CC=C(N2CCOCC2)C2=C1N=C(NC(=O)N1CCC(C)(O)CC1)S2 |
| MDL No. | MFCD21642026 |
| 别名 | SYN115 |
| 运输 | 蓝冰 |
| InChI Key | XNBRWUQWSKXMPW-UHFFFAOYSA-N |
| Pubchem ID | 11618368 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, 2-8°C |
| 溶解方案 |
DMSO: 50 mg/mL(123 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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