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M1069
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
M1069图片
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
M1069 是一种口服有效、选择性的 A2A/A2B型双腺苷受体拮抗剂,比对 A1、 A3亚型的选择性高出 100 多倍。M1069 能够拮抗腺苷引起的免疫抑制机制,具有抗肿瘤活性。
生物活性

M1069 is a selective and orall active, dual A2A/A2Badenosine receptor antagonistwith a selectivity of >100 fold against the A1and A3receptors. M1069 counteracts immune-suppressive mechanisms of adenosine, and exhibits anti-tumor activity[1][2][3].

IC50& Target

A2AR

 

A2BR

 

体外研究
(In Vitro)

Metabolically stressful conditions, including inflammation and cancer, induces extracellular concentrations of adenosine increase[1].
M1069 dose-dependently suppresses 5’-N-ethylcarboxamide adenosine (stable analog of adenosine)-stimulated cyclic adenosine monophosphate (cAMP) and phosphorylated cAMP- response element binding protein (pCREB) induction, inhibits interleukin (IL)-2 production[1].
M1069 suppresses vascular endothelial growth factor (VEGF) production from human macrophages in adenosine-rich settings[1].
M1069 inhibits protumorigenic cytokine secretion, such as CXCL1, CXCL5 and granulocyte-colony stimulating factor, and reduces IL-12 secretion from adenosine-differentiated dendritic cells[1].
M1069 enhances T-cells activation in adenosine-differentiated dendritic cells[1].

体内研究
(In Vivo)

M1069 inhibits breast tumor (CD73hi/adenosine-rich 4T1 syngeneic) growth in vivo in mice and enhances chemotherapeutic agents efficacy[1].

Clinical Trial
分子量

546.59

Formula

C25H30N4O8S

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.