2. GPCR/G Protein
  3. Adenosine Receptor
  4. A2AAR antagonist 4

A2AAR antagonist 4 是一种口服有效的 A2A 腺苷受体 (A2A Adenosine receptor) 拮抗剂，对人 A2AAR 上的 Ki 值为 0.36 nM，KB 值为 1 nM。A2AAR antagonist 4 在 10 μM 时可完全抑制人 A2AAR 和人 A2bAR。A2AAR antagonist 4 可用于癌症的研究，如 MC38 肿瘤。

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A2AAR antagonist 4

A2AAR antagonist 4 Chemical Structure

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A2AAR antagonist 4 相关抗体

Top Publications Citing Use of Products

查看 Adenosine Receptor 亚型特异性产品:

查看所有亚型
Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

A2AAR antagonist 4 is an orally active A2A Adenosine receptor antagonist with a Ki of 0.36 nM and a KB of 1 nM at hA2AAR. A2AAR antagonist 4 fully inhibits hA2AAR and hA2bAR at 10 μM. A2AAR antagonist 4 can be used for research of cancer, such as MC38 tiumor[1].

IC50 & Target[1]

hA2AAR

0.36 nM (Ki)

hA2AAR

1 nM (Kb)

hA2B

85.8 nM (Ki)

hA3

98.4 nM (Ki)

hA1AR

286 nM (Ki)

体外研究
(In Vitro)

A2AAR antagonist 4 (Compound 4d) (10 μM) 可在 CHO-A2A 细胞系中完全抑制 hA2AAR、hA2BAR 和 hA3AR[1]。
A2AAR antagonist 4 (0.1-1000 nM) 通过完全置换 NECA 来恢复 PBMC 细胞中 IL-2 的分泌，其 EC50 值为 2.06 nM[1]。

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

A2AAR antagonist 4 相关抗体:
体内研究
(In Vivo)

A2AAR antagonist 4 (Compound 4d) (100 mg/kg，口服或 50 mg/kg，腹腔注射，每天两次，持续 14 天) 可显著抑制 MC38 肿瘤小鼠的肿瘤生长[1]。

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

Animal Model: MC38 tumor mice models[1]
Dosage: 50 or 100 mg/kg
Administration: P.O or intraperitoneally injection (i.p.), twice a day for 14 days
Result: Demonstrated significant tumor growth inhibition (TGI) of 33% TGI (p.o.) and 59% (i.p.).
分子量

367.40

Formula

C19H21N5O3
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 4 相关分类

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  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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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.

Keywords:

A2AAR antagonist 4Adenosine ReceptorP1 receptorA2A Adenosine receptorMC38CHO-A2AIL-2Inhibitorinhibitorinhibit

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产品名称：
A2AAR antagonist 4
目录号：
HY-175487
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