1. GPCR/G Protein
  2. Adenosine Receptor
  3. A2AAR antagonist 5

A2AAR antagonist 5 是一种选择性的 A2AAR 拮抗剂。A2AAR antagonist 5 在表达 hA2AAR 的 CHO 细胞中抑制 NECA 刺激的腺苷酸环化酶活性,其 IC50 值为 1863 nM。A2AAR antagonist 5 具有较强的清除自由基活性,在 DPPH 实验中的 EC50 值为 22.21 μM。A2AAR antagonist 5 在体外脑缺血模型中表现出显著的神经保护作用。A2AAR antagonist 5 可用于脑缺血的研究。

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A2AAR antagonist 5

A2AAR antagonist 5 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

A2AAR antagonist 5 is a selective A2AAR antagonist. A2AAR antagonist 5 inhibits NECA-stimulated adenylyl cyclase activity in hA2AAR-expressing CHO cells with an IC50 value of 1863 nM. A2AAR antagonist 5 possesses strong free radical scavenging activity, with an EC50 value of 22.21 μM in the DPPH assay. A2AAR antagonist 5 exerts notable neuroprotective effects in in vitro cerebral ischemia models. A2AAR antagonist 5 can be used for the study of cerebral ischemia[1].

IC50 & Target[1]

hA2AAR

1863 nM (IC50)

hA2AAR

57 nM (Ki)

hA1AR

> 30000 nM (Ki)

hA3

358 nM (Ki)

hA2B

> 30000 nM (Ki)

体外研究
(In Vitro)

A2AAR antagonist 5 (Compound 3) 对 hA2A 腺苷受体表现出很强的亲和力,其 Ki 值为 57 nM;对 hA1 腺苷受体无亲和力 (Ki > 30,000 nM);对 hA3 腺苷受体具有中等亲和力 (Ki = 358 nM);对 hA2B 腺苷受体无活性 (IC50 > 30,000 nM)[1]
A2AAR antagonist 5 在表达 hA2A 腺苷受体的 CHO 细胞中对 hA2A 腺苷受体发挥拮抗作用,其抑制 NECA 刺激的腺苷酸环化酶活性的 IC50 值为 1416 nM[1]
A2AAR antagonist 5 显示出较强的清除自由基活性,其 EC50 值为 22.21 μM[1]
A2AAR antagonist 5 (200 nM,分别在氧糖剥夺 (OGD) 前 15 min、OGD 期间以及 OGD 后 5 min 给药) 可显著延迟在急性大鼠海马切片 CA1 区检测到的由缺氧-低糖 (OGD) 诱导的缺氧去极化 (AD) 的发生[1]
A2AAR antagonist 5 (1-10 μM,在 30 min OGD 期间以及随后 24 h 恢复期内给药) 可发挥显著的神经保护作用,减轻在大鼠器官型海马切片 CA1 区检测到的 OGD 诱导的神经元损伤[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

456.46

Formula

C23H20N8O3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

A2AAR antagonist 5 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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A2AAR antagonist 5
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HY-175851
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