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Chemical Structure| 163042-96-4 同义名 : 2-Cl-IB-MECA; CF-102; Chloro-IB-MECA; Cl-IB-MECA; 2-Chloro-IB-MECA
CAS号 : 163042-96-4
货号 : A138589
分子式 : C18H18ClIN6O4
纯度 : 99%+
分子量 : 544.73
MDL号 : MFCD01861178
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 2-Cl-IB-MECA is a selective A3 adenosine receptor (A3AR) agonist (Ki=0.33 nM). Intravenous administration of 200 micrograms/kg 2-Cl-IB-MECA resulted in a short-lasting hypotension, which was accompanied by a 50-100-fold increase in plasma histamine concentrations. Administration of a second dose of 2-Cl-IB-MECA did not elicit any hemodynamic effects. Also no histamine release was observed after the second dose[3]. Pretreating wild-type (WT) mice with Cl-IB-MECA reduced myocardial infarct size induced by 30 min of coronary occlusion and 24 h of reperfusion at doses (30 and 100 mug/kg) that concomitantly reduced blood pressure and stimulated systemic histamine release. Cl-IB-MECA protects against myocardial ischemia/reperfusion injury in mice principally by activating the A(3)AR (A(3) adenosine receptor) [4]. Cl-IB-MECA is able to enhance TNF-α production in LPS-treated macrophages in an NF-κB- dependent manner[5]. Cl-IB-MECA suppressed erythroblast growth and maturation at doses >/=50 mumol/l through a mechanism of cell cycle inhibition and accumulation of cells in the G1/G0 phase[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.84mL

0.37mL

0.18mL

9.18mL

1.84mL

0.92mL

18.36mL

3.67mL

1.84mL
参考文献

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

[2]Van Schaick EA, Jacobson KA, 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.

[3]Van Schaick EA, Jacobson KA, Kim HO, IJzerman AP, Danhof M. 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

[4]Ge ZD, Peart JN, Kreckler LM, Wan TC, Jacobson MA, Gross GJ, Auchampach JA. Cl-IB-MECA [2-chloro-N6-(3-iodobenzyl)adenosine-5'-N-methylcarboxamide] reduces ischemia/reperfusion injury in mice by activating the A3 adenosine receptor. J Pharmacol Exp Ther. 2006 Dec;319(3):1200-10

[5]Forte G, Sorrentino R, Montinaro A, Pinto A, Morello S. Cl-IB-MECA enhances TNF-α release in peritoneal macrophages stimulated with LPS. Cytokine. 2011 May;54(2):161-6

[6]Bhanu NV, Aerbajinai W, Gantt NM, Jackson EK, Goh SH, Terry Lee Y, Miller JL. Cl-IB-MECA inhibits human erythropoiesis. Br J Haematol. 2007 May;137(3):233-6