2. GPCR/G Protein Immunology/Inflammation Metabolic Enzyme/Protease
  3. Adenosine Receptor Interleukin Related IFNAR Cytochrome P450
  4. Adenosine receptor antagonist 6

Adenosine receptor antagonist 6 是一种 (S)-对映体化合物，具有口服活性且选择性的 A2A 腺苷受体(A2A adenosine receptor) (A2AAR) 拮抗剂。 Adenosine receptor antagonist 6 与 A2A adenosine receptor 结合的 Ki 值为 19.18 nM。Adenosine receptor antagonist 6 抑制 5’-N-ethylcarboxamide adenosine (NECA) (HY-103173) 介导的 cAMP 产生 (IC50 = 0.089 μM) 和免疫抑制，同时促进 IL-2 和 IFN-γ 的分泌。Adenosine receptor antagonist 6 消除腺苷对 T 细胞活化和细胞因子释放的免疫抑制作用。Adenosine receptor antagonist 6 抑制 CT26/MC38 异种移植模型中的肿瘤生长。Adenosine receptor antagonist 6 可用于结肠癌的研究。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

Adenosine receptor antagonist 6

Adenosine receptor antagonist 6 Chemical Structure

CAS No. : 2913578-04-6

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

Adenosine receptor antagonist 6 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)

查看 Interleukin Related 亚型特异性产品:

查看所有亚型
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

查看 Cytochrome P450 亚型特异性产品:

查看所有亚型
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Adenosine receptor antagonist 6, a (S)-enantiomer compound, is an orally active and selective A2A adenosine receptor (A2AAR) antagonist. Adenosine receptor antagonist 6 binds to the A2A adenosine receptor with a Ki of 19.18 nM. Adenosine receptor antagonist 6 inhibits 5’-N-ethylcarboxamide adenosine (NECA) (HY-103173)-mediated cAMP production (IC50 = 0.089 μM) and immunosuppression, while promoting IL-2 and IFN-γ secretion. Adenosine receptor antagonist 6 abolishes the immunosuppressive effects of adenosine on T-cell activation and cytokine release. Adenosine receptor antagonist 6 inhibits tumor growth in a CT26/MC38 xenograft model. Adenosine receptor antagonist 6 can be used for the study of colon cancer[1].

体外研究
(In Vitro)

Adenosine receptor antagonist 6 (Compound 11a) 对 A1、A2B 和 A3 腺苷受体表现出选择性结合，Ki 值分别为 392.23 nM、2129 nM 和 9036 nM[1]。
Adenosine receptor antagonist 6 (0.001-100 μM) 在活化的原代人外周血单核细胞 (PBMCs) 中以剂量依赖性抑制 NECA 介导的 cAMP 产生IC50 为 0.089 μM[1]。
Adenosine receptor antagonist 6 (0.1-10 μM) 在活化的原代人外周血单核细胞 (PBMCs) 中消除腺苷对 T 细胞活化和细胞因子释放的免疫抑制作用[1]。
Adenosine receptor antagonist 6 (0.03-3 μM) 在活化的原代人外周血单核细胞 (PBMCs) 中抑制 5’-N-乙基羧酰胺腺苷 (NECA) (HY-103173) 介导的免疫抑制，并恢复 IL-2 和 IFN-γ 的分泌[1]。
Adenosine receptor antagonist 6 (0.8125-50 μM, 48 h) 抑制 HCT116 细胞 (IC50 = 17.21 μM)、MDA-MB-231 细胞 (IC50 = 53.77 μM)、MC38 细胞 (IC50 = 18.91 μM) 和 CT26 细胞 (IC50 = 19.36 μM) 的增殖[1]。
Adenosine receptor antagonist 6 在 CYP450 酶的代谢清除率较低，其中 CYP1A2 在其立体选择性代谢中起主要作用[1]。

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

Adenosine receptor antagonist 6 相关抗体:
体内研究
(In Vivo)

Adenosine receptor antagonist 6 (Compound 11a) (15-25 mg/kg， 口服给药，每日一次，19-21 天) 在单独使用或与 PD-L1 单克隆抗体联合使用时，抑制 CT26/MC38 异种移植模型中的肿瘤生长[1]。

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

Animal Model: CT26 cancer cells (5 × 105 in 100 μL) were injected subcutaneously into both flanks of BALB/c mice[1]
Dosage: 25 mg/kg
Administration: p.o. once daily for 19 days
Result: Demonstrated a tumor growth inhibition rate (TGI) of 37%.
Exhibited significant enhancement of efficacy (TGI = 92%) when combined with PD-L1 monoclonal antibody (10 mg/kg, i.p., b.i.w.).
Animal Model: MC38 cancer cells (5 × 105 in 100 μL) were injected subcutaneously into both flanks of C57BL/6 mice[1]
Dosage: 15 mg/kg
Administration: p.o. once daily for 21 days
Result: Demonstrated a tumor growth inhibition rate (TGI) of 69.74%.
Exhibited significant enhancement of efficacy (TGI = 98.1%) when combined with PD-L1 monoclonal antibody (10 mg/kg, i.p., b.i.w.).
分子量

332.36

Formula

C18H16N6O
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 6 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

Adenosine receptor antagonist 62913578-04-6Adenosine receptor antagonist6Adenosine receptor antagonist-6Adenosine ReceptorInterleukin RelatedIFNARCytochrome P450P1 receptorILInterferon-α/β receptorInterferon-alpha/beta receptor CYPsAdenosine receptorcolon cancerchiral compoundInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
Adenosine receptor antagonist 6
目录号：
HY-175195
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z