2. GPCR/G Protein
  3. Adenosine Receptor
  4. Adenosine receptor antagonist 7

Adenosine receptor antagonist 7 是一种具有口服活性的三重 A1/A2A/A2B 腺苷受体拮抗剂，其 Ki 值分别为 1.5、0.6 和 21 nM。Adenosine receptor antagonist 7 在 A2AR-HEK293 细胞中对环磷酸腺苷 (cAMP) 的产生具有强效抑制活性 (IC50 值为 0.8 nM)。Adenosine receptor antagonist 7 与 Avelumab (HY-108730) 联合使用时，可增强效应 T 细胞的浸润，并提高 CD8+/Treg的比例。Adenosine receptor antagonist 7 可用于癌症研究，如结肠癌。

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Adenosine receptor antagonist 7

Adenosine receptor antagonist 7 Chemical Structure

CAS No. : 2570904-69-5

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Adenosine receptor antagonist 7 相关抗体

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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

Adenosine receptor antagonist 7 is an orally active triple A1/A2A/A2B adenosine receptor antagonist with Ki values of 1.5, 0.6 and 21 nM. Adenosine receptor antagonist 7 shows potent inhibitory activity (IC50 = 0.8 nM) of cAMP production in A2AR-HEK293 cells. Adenosine receptor antagonist 7 can enhance infiltration of effector T cells and increase the CD8+/Treg ratio companied with Avelumab (HY-108730). Adenosine receptor antagonist 7can be used for the research of cancer, such as colon cancer[1].

IC50 & Target[1]

A1

1.5 nM (Ki)

A2A

0.6 nM (Ki)

A2B

21 nM (Ki)

体外研究
(In Vitro)

Adenosine receptor antagonist 7 (Compound 14a) (0.32-1000 nM, 30 mins) 可抑制人 CD8+T 细胞中 NECA (HY-103173) 诱导的 cAMP 积累 (IC50 = 18 nM)[1]。br> Adenosine receptor antagonist 7 (10-100 nM, 30 mins) 可抑制 A1R 过表达的 SK-BR-3 细胞中 ERK 和 JNK 的磷酸化，下调 MMP-2 和 MMP-9 的 mRNA 表达[1]。br>

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

Adenosine receptor antagonist 7 相关抗体:

Western Blot Analysis[1]

Cell Line: A1R-overexpressing SK-BR-3 cells
Concentration: 10 and 100 nM
Incubation Time: 30 mins
Result: Reduced the phosphorylation of ERK and JNK.
体内研究
(In Vivo)

Adenosine receptor antagonist 7 (Compound 14a) (50 mg/kg，口服，每天两次，持续 14 天) 可抑制携带 CT26 肿瘤的 BALB/c 裸鼠的肿瘤生长[1]。

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

Animal Model: BALB/c nude mice bearing CT26 tumors[1]
Dosage: 50 mg/kg
Administration: Orally administration, twice a day for 14 days
Result: Inhibited tumor growth without adverse reactions such as weight loss.
Increased the number of tumor-infiltrating effector T cells and improved the CD8+/Treg ratio when combined with Avelumab.
分子量

390.44

Formula

C21H22N6O2
CAS 号
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

Adenosine receptor antagonist 7 相关分类

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  • 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:

Adenosine receptor antagonist 72570904-69-5Adenosine receptor antagonist7Adenosine receptor antagonist-7Adenosine ReceptorP1 receptorNECAERKJNKMMP-2MMP-9CT26Inhibitorinhibitorinhibit

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