货号:A120930
同义名:
SCH-420814; MK-3814
Preladenant是一种高度选择性且竞争性的A2A受体拮抗剂,Ki值为1.1 nM,用于脑部疾病的研究,如帕金森病、运动障碍和帕金森症状。


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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 |
++++
rat A2a, Ki: 2.3 nM bovine A2a, Ki: 2.0 nM |
99%+ | |||||||||||||||||
| A2A receptor antagonist 1 |
++
A2AR, Ki: 4 nM A1R, Ki: 264 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 | Preladenant is a potent competitive antagonist of the human A2A receptor (Ki=1.1 nM) and has > 1000-fold selectivity over all other adenosine receptors. |
| Concentration | Treated Time | Description | References | |
| Primary microglia | 1 μM | Preladenant prevented adenosine-induced process retraction in activated microglia | Glia. 2014 Aug;62(8):1345-60. | |
| Primary microglia | 1 μM | Preladenant prevented adenosine-induced process retraction in activated microglia. | Glia. 2014 Aug;62(8):1345-60. |
| Administration | Dosage | Frequency | Description | References | ||
| Mice | LPS-induced neuroinflammation model | Intraperitoneal injection | 3 mg/kg | Single injection, imaging after 1 hour | Preladenant accelerated the microglial response to tissue damage | Glia. 2014 Aug;62(8):1345-60. |
| Mice | LPS-induced neuroinflammation model | Intraperitoneal injection | 3 mg/kg | Single injection, lasting 1 hour | Preladenant accelerated the response of activated microglia to injury following systemic inflammation. | Glia. 2014 Aug;62(8):1345-60. |
| Mice | Parkinson's disease model | Perfusion | 5 μM | Continuous perfusion | Restored microglial response to tissue injury | Neurobiol Dis. 2014 Jul;67:191-202 |
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00406029 | Parkinson Disease ... 展开 >> Movement Disorders Central Nervous System Diseases Neurodegenerative Diseases Brain Diseases 收起 << | Phase 2 | Completed | - | - |
| NCT01155466 | Parkinson Disease | Phase 3 | Completed | - | - |
| NCT01215227 | Parkinson Disease ... 展开 >> Idiopathic Parkinson Disease 收起 << | Phase 3 | Terminated | - | - |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
1.99mL 0.40mL 0.20mL |
9.93mL 1.99mL 0.99mL |
19.86mL 3.97mL 1.99mL |
|
| CAS号 | 377727-87-2 |
| 分子式 | C25H29N9O3 |
| 分子量 | 503.56 |
| SMILES Code | NC1=NC(N(CCN2CCN(C3=CC=C(OCCOC)C=C3)CC2)N=C4)=C4C5=NC(C6=CC=CO6)=NN15 |
| MDL No. | MFCD17167056 |
| 别名 | SCH-420814; MK-3814; Privadenant |
| 运输 | 蓝冰 |
| InChI Key | DTYWJKSSUANMHD-UHFFFAOYSA-N |
| Pubchem ID | 10117987 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C |
| 溶解方案 |
DMSO: 4 mg/mL(7.94 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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