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化合T23016

化合T23016用途

MRS1220是一种高度有效和选择性的人类A3腺苷受体(hA3AR)拮抗剂,Ki为0.59 nM,在中枢神经系统疾病的研究中具有治疗潜力[1]。MRS1220可减少体内胶质母细胞瘤的肿瘤大小和血管形成[2]。

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化合T23016名称

[ CAS 号 ]:
183721-15-5

[ 中文名 ]:
N-[9-CHLORO-2-(2-FURANYL)[1,2,4]-TRIAZOLO[1,5-C]QUINAZOLIN-5-YL]BENZENE ACETAMIDE

[ 英文名 ]:
MRS 1220

[英文别名 ]:

MRS 1220
Tocris-1217
MFCD01321046

化合T23016生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 腺苷受体

[体外研究]

MRS 1220逆转A3激动剂诱导的抑制人巨噬细胞U-937细胞系中肿瘤坏死因子-α形成的效应,IC50为0.3μM[1]。缺氧72小时后,U87MG胶质母细胞瘤干细胞样细胞(GSC)中的VEGF分泌在MRS1220中减少约25%[2]。细胞活力测定[2]细胞系：U87MG GSCs浓度：10μM培养时间：72小时结果：VEGF分泌减少约25%。

[体内研究]

MRS1220(0.15 mg/kg；腹腔接种)减少体内肿瘤大小和血管形成。MRS1220具有很强的体内抗血管生成作用[2]。动物模型：8周龄雄性Sprague-Dawley大鼠,携带C6(GSCs)[2]剂量：0.15 mg/kg/72 h给药：通过腹腔接种给药,持续15天结果：与载体治疗组相比,在治疗后第10天和第15天,肿瘤体积分别减少近80%和90%。

[参考文献]

[1]. K A Jacobson, et al. Pharmacological characterization of novel A3 adenosine receptor-selective antagonists. Neuropharmacology. 1997 Sep;36(9):1157-65.

[2]. René Rocha, et al. The Adenosine A₃ Receptor Regulates Differentiation of Glioblastoma Stem-Like Cells to Endothelial Cells under Hypoxia. Int J Mol Sci. 2018 Apr 18;19(4):1228.

化合T23016物理化学性质

[ 密度 ]:
1.49g/cm3

[ 分子式 ]:
C₂₁H₁₄ClN₅O₂

[ 分子量 ]:
403.82

[ 精确质量 ]:
403.08400

[ PSA ]:
85.32000

[ LogP ]:
4.44510

[ 折射率 ]:
1.744

[ 储存条件 ]:
2-8°C，密封，干燥

化合T23016MSDS

详细MSDS(安全技术说明书)

化合T23016安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

化合T23016文献

Fragment-Based Discovery of Subtype-Selective Adenosine Receptor Ligands from Homology Models.

J. Med. Chem. 58 , 9578-90, (2015)

Fragment-based lead discovery (FBLD) holds great promise for drug discovery, but applications to G protein-coupled receptors (GPCRs) have been limited by a lack of sensitive screening techniques and s...

Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype.

J. Med. Chem. 39 , 4142-4148, (1996)

The adenosine antagonist 9-chloro-2-(2-furanyl)[1,2,4]triazolo[1,5-c]quinazolin-5-amine (CGS15943) binds to human A3 receptors with high affinity (Ki = 14 nM), while it lacks affinity at rat A3 recept...

Pharmacological characterization of novel A3 adenosine receptor-selective antagonists.

Neuropharmacology 36 , 1157-1165, (1997)

The effects of putative A3 adenosine receptor antagonists of three diverse chemical classes (the flavonoid MRS 1067, the 6-phenyl-1,4-dihydropyridines MRS 1097 and MRS 1191, and the triazoloquinazolin...

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