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氯-IB-MECA

氯-IB-MECA用途

Namodenoson (CF-102) 是一个选择性的 A3 adenosine 受体的激动剂,选择性分别是A1,A2的2500到1400倍。

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氯-IB-MECA名称

[ CAS 号 ]:
163042-96-4

[ 中文名 ]:
1-[2-氯-6-[[(3-碘苯基)甲基]氨基]-9h-嘌呤-9-基]-1-脱氧-N-甲基-beta-d-呋喃核糖酰胺

[ 英文名 ]:
2-CL-IB-MECA

[英文别名 ]:

CF102
CI-IB-MECA
2-Cl-IB-Meca
Cl-IB-MECA
Namodenoson
2-chloro-IB-MECA
UNII:Z07JR07J6C
CF-102
CF-102(2-Cl-IB-MECA)

氯-IB-MECA生物活性

[ 描述 ]:

Namodenoson (CF-102) 是一个选择性的 A3 adenosine 受体的激动剂,选择性分别是A1,A2的2500到1400倍。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 腺苷受体

研究领域 >> 癌症

[ 靶点 ]

Ki:0.33 nM (A3 adenosine receptor)[1][2].

[体外研究]

在星形胶质细胞谱系的人ADF细胞中,100nMNModenodenoson(2-Cl-IB-MECA)引起细胞骨架的显着重组,具有应力纤维和许多细胞突起的外观。高浓度的Namodenoson(2-Cl-IB-MECA)直接引起Ca2 +的流入[2]。

[体内研究]

静脉内施用200μg/ kg Namodenoson(2-Cl-IB-MECA)导致短暂的低血压,伴随着血浆组胺浓度增加50-100倍。施用第二剂量的Namodenoson(2-Cl-IB-MECA)未引起任何血液动力学效应[1]。

[参考文献]

[1]. Van Schaick EA et al. Hemodynamic effects and histamine release elicited by the selective adenosine A3 receptor agonist 2-Cl-IB-MECA in conscious rats. Eur J Pharmacol. 1996 Jul 25;308(3):311-4.

[2]. Jacobson KA et al. Adenosine A3 receptors: novel ligands and paradoxical effects. Trends Pharmacol Sci. 1998 May;19(5):184-91.

[相关活性小分子]

氯-IB-MECA物理化学性质

[ 密度 ]:
2.0±0.1 g/cm3

[ 熔点 ]:
209 °C

[ 分子式 ]:
C₁₈H₁₈ClIN₆O₄

[ 分子量 ]:
544.731

[ 精确质量 ]:
544.012268

[ PSA ]:
134.42000

[ LogP ]:
3.14

[ 外观性状 ]:
固体;White to Almost white powder to crystal

[ 折射率 ]:
1.814

[ 储存条件 ]:
0-10°C;避免加热

氯-IB-MECAMSDS

氯-IB-MECA安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
S26

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

[ 海关编码 ]:
2934999090

氯-IB-MECA合成路线

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氯-IB-MECA上游产品

氯-IB-MECA下游产品

氯-IB-MECA海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

氯-IB-MECA文献

The combination of Cl-IB-MECA with paclitaxel: a new anti-metastatic therapeutic strategy for melanoma.

Cancer Chemother. Pharmacol. 74(4) , 847-60, (2014)

Metastatic melanoma is considered one of the most aggressive malignant tumours, representing the deadliest form of skin cancer. Melanoma progression is associated with the abrogation of normal control...

Activation of hippocampal adenosine A3 receptors produces a desensitization of A1 receptor-mediated responses in rat hippocampus.

J. Neurosci. 17 , 607-614, (1997)

The adenosine A3 receptor is expressed in brain, but the consequences of activation of this receptor on electrophysiological activity are unknown. We have characterized the actions of a selective aden...

Modulation of A1 and A2B adenosine receptor activity: a new strategy to sensitise glioblastoma stem cells to chemotherapy.

Cell Death Dis. 5 , e1539, (2014)

Therapies that target the signal transduction and biological characteristics of cancer stem cells (CSCs) are innovative strategies that are used in combination with conventional chemotherapy and radio...

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