SCH58261
SCH 58261是一个高效的选择性的A2a adenosine receptor拮抗剂，其对rat A2a和bovine A2a的Ki值分别为2.3 nM和2 nM。
SCH58261 Chemical Structure
CAS: 160098-96-4
客户使用Selleck的发表文献6篇
产品质控
SCH58261相关产品
| 相关靶点 | Adenosine A1 receptor | 点击展开 |
|---|---|---|
| 相关化合物库 | FDA药物库 天然产物库 已知活性药物库-I 生物活性库Ⅱ GPCR小分子化合物库 | 点击展开 |
Adenosine Receptor抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| HEK293 | Function assay | 100 nM | 24 hrs | Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced intracellular cAMP accumulation at 100 nM after 24 hrs (Rvb= 0.40 pmol/ml) | 20303771 |
| HEK293 | Function assay | 1 uM | 15 mins | Antagonist activity at human A2A receptor expressed in HEK293 cells assessed as decrease in NECA-induced cAMP release at 1 uM after 15 mins | 23953686 |
| HEK293 | Function assay | 60 mins | Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting analysis, Ki = 0.0006 μM. | 23200243 | |
| CHO | Function assay | 60 mins | Displacement of [3H]-ZM 241385 from human adenosine A2A receptor expressed in CHO cells after 60 mins by liquid scintillation counting, Ki = 0.0011 μM. | 22204739 | |
| HEK293 | Function assay | 60 mins | Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by rapid filtration assay, Ki = 0.00123 μM. | 20303771 | |
| HEK293 | Function assay | 60 mins | Competitive binding affinity to human adenosine A2A receptor expressed in HEK293 cells after 60 mins by fluorescence polarization assay in presence of MRS5346, Ki = 0.0019 μM. | 23200243 | |
| CHO | Function assay | 120 mins | Displacement of [3H]-DPCPX from human adenosine A1 receptor expressed in CHO cells after 120 mins by liquid scintillation counting, Ki = 0.549 μM. | 22204739 | |
| HEK293 | Function assay | 60 mins | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in HEK293 cells after 60 mins by rapid filtration assay, Ki = 0.5941 μM. | 20303771 | |
| CHO | Function assay | 120 mins | Displacement of [3H]-MRE-3008-F20 from human adenosine A3 receptor expressed in CHO cells after 120 mins by liquid scintillation counting, Ki = 10 μM. | 22204739 | |
| HEK293 | Function assay | 60 mins | Displacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins, Ki = 10 μM. | 22204739 | |
| CHO | Function assay | Displacement of [3H]-SCH- 58261 from human Adenosine A2A receptor expressed in CHO cells, Ki = 0.0011 μM. | 9622554 | ||
| HEK293 | Function assay | Displacement of specific [3H]-SCH- 58261 binding at human Adenosine A2A receptor expressed in HEK293 cells., Ki = 0.0011 μM. | 11754583 | ||
| CHO | Function assay | Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells, Ki = 0.0011 μM. | 19501513 | ||
| CHO | Function assay | Displacement of [3H]CHA from human Adenosine A1 receptor expressed in CHO cells, Ki = 0.549 μM. | 9622554 | ||
| CHO | Function assay | Displacement of specific [3H]DPCPX binding at human Adenosine A1 receptor expressed in CHO cells., Ki = 0.549 μM. | 11754583 | ||
| HEK293 | Function assay | Displacement of [3H]-AB MECA from human Adenosine A3 receptor expressed in HEK293 cells, Ki = 1 μM. | 12646033 | ||
| HEK293 | Function assay | Displacement of [125I]AB-MECA from human Adenosine A3 receptor expressed in HEK293 cells, Ki = 10 μM. | 9622554 | ||
| HEK293 | Function assay | Displacement of specific [3H]DPCPX binding at human adenosine A2B receptor expressed in HEK293 cells., Ki = 10 μM. | 11754583 | ||
| CHO | Function assay | Displacement of specific [3H]MRE3008-F20 binding at human adenosine A3 receptor expressed in CHO cells., Ki = 10 μM. | 11754583 | ||
| CHO | Function assay | Displacement of [3H]NECA from human adenosine A3 receptor expressed in CHO cells, Ki = 10 μM. | 19501513 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | SCH 58261是一个高效的选择性的A2a adenosine receptor拮抗剂，其对rat A2a和bovine A2a的Ki值分别为2.3 nM和2 nM。 | ||||
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| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | SCH 58261通过竞争性的拮抗CGS 21680的诱导作用，导致了兔子血小板凝集的抑制以及牛冠状动脉的收缩抑制。[1] |
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|---|---|---|---|---|
| 体内研究(In Vivo) | ||
| 体内研究活性 |
在脊髓损伤的小鼠模型中，SCH58261 (0.01 mg/kg, i.p.)降低了脱髓鞘作用，并且降低了TNF-α, Fas-L, PAR, Bax表达水平以及JNK MAPK的激活。慢性的SCH58261处理改善了神经缺损。[2] 在6-OHDA诱导的帕金森病模型大鼠中，SCH58261 (2 mg/kg, i.p.)改善了6-OHDA诱导的运动迟缓以及运动障碍。[3] |
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|---|---|---|
| 动物实验 | Animal Models | 脊髓损伤小鼠 |
| Dosages | 0.01 mg/kg | |
| Administration | i.p. | |
化学信息&溶解度
| 分子量 | 345.36 | 分子式 | C18H15N7O |
| CAS号 | 160098-96-4 | SDF | Download SCH58261 SDF |
| Smiles | C1=CC=C(C=C1)CCN2C3=C(C=N2)C4=NC(=NN4C(=N3)N)C5=CC=CO5 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 69 mg/mL ( (199.79 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
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）
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Selleck为您提供正确的澄清溶液配方）
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，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
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 ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：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。
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