AICAR（也称为 acadesine）是一种嘌呤核苷。确定了 AICAR 的三种药理学应用:i) 在缺血条件下刺激心脏产生血管扩张剂腺苷 [1]； ii) 在 fructose-1,6-bisphosphatase [2] 水平抑制肝糖异生，具有治疗糖尿病的潜力； iii) 刺激 AMP 活化蛋白激酶 (AMPK)，最初用于抑制肝脏合成甘油三酯和胆固醇[3]。

AICAR（处理 48 小时）抑制套细胞淋巴瘤 (MCL) 细胞系 REC-1、JEKO-1、UPN-1、JVM-2、MAVER-1 和 Z-138 的细胞增殖，IC50 为 0.28 , 0.59, 0.64, 0.98, 0.50, 0.14 Mm [4]。 AICAR 抑制成纤维细胞 [5] 中嘧啶核苷酸库的生长和消耗，加速心脏中嘌呤核苷酸库的补充 [6]，抑制脂肪酸、甾醇合成，和肝细胞中的糖异生，以及肌肉中葡萄糖摄取的增加[7]。

AICAR (500 mg/kg) 在 LPS 给药前 1 小时腹膜内注射到 C57BL/6J 小鼠中。 LPS 在许多主要器官中诱导 TF mRNA 的表达，包括肺和肝[8]。与对照动物相比，在预先接种 MCL 异种移植物的小鼠中每天给予 400 毫克/千克 AICAR，只要治疗 7 天[9]。

产品性质：

Cas No.:2627-69-2

别名:阿卡地新; Acadesine; AICA Riboside

化学名:5-amino-1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]imidazole-4-carboxamide

Canonical SMILES:CC(C=C(C)C=CC(=O)NO)C(=O)C1=CC=C(C=C1)N(C)C

分子式:C9H14N4O5

分子量:258.23

溶解度:≥ 12.9 mg/mL in DMSO, ≥ 52.9 mg/mL in Water

储存条件:Store at -20°C

注意事项：

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References:

[1]. Gruber H E, Hoffer M E, McAllister D R, et al. Increased adenosine concentration in blood from ischemic myocardium by AICA riboside. Effects on flow, granulocytes, and injury[J]. Circulation, 1989, 80(5): 1400-1411.

[2]. Vincent M F, Marangos P J, Gruber H E, et al. Inhibition by AICA riboside of gluconeogenesis in isolated rat hepatocytes[J]. Diabetes, 1991, 40(10): 1259-1266.

[3]. Hardie D G, Carling D, Carlson M. The AMP-activated/SNF1 protein kinase subfamily: metabolic sensors of the eukaryotic cell?[J]. Annual review of biochemistry, 1998, 67: 821.

[4]. Montraveta A, Xargay-Torrent S, López-Guerra M, et al. Synergistic anti-tumor activity of acadesine (AICAR) in combination with the anti-CD20 monoclonal antibody rituximab in in vivo and in vitro models of mantle cell lymphoma[J]. Oncotarget, 2014, 5(3): 726.

[5]. Sabina R L, Patterson D, Holmes E W. 5-Amino-4-imidazolecarboxamide riboside (Z-riboside) metabolism in eukaryotic cells[J]. Journal of Biological Chemistry, 1985, 260(10): 6107-6114.

[6]. Swain J L, Hines J J, Sabina R L, et al. Accelerated repletion of ATP and GTP pools in postischemic canine myocardium using a precursor of purine de novo synthesis[J]. Circulation Research, 1982, 51(1): 102-105.

[7]. Hardie D G, Carling D, Carlson M. The AMP-activated/SNF1 protein kinase subfamily: metabolic sensors of the eukaryotic cell?[J]. Annual review of biochemistry, 1998, 67: 821.

[8]. Zhang W, Wang J, Wang H, et al. Acadesine inhibits tissue factor induction and thrombus formation by activating the phosphoinositide 3-kinase/Akt signaling pathway[J]. Arteriosclerosis, thrombosis, and vascular biology, 2010, 30(5): 1000-1006.

[9]. Montraveta A, de Fri?as M, Campa?s C, et al. The Nucleoside Analogue Acadesine Exerts Antitumoral Activity and Cooperates with Conventional Agents In In Vitro and In Vivo Models of Mantle Cell Lymphoma[J]. Blood, 2010, 116(21): 3918.