AICAR（也稱為 acadesine）是一種嘌呤核苷。確定了 AICAR 的三種藥理學(xué)應(yīng)用:i) 在缺血條件下刺激心臟產(chǎn)生血管擴(kuò)張劑腺苷 [1]； ii) 在 fructose-1,6-bisphosphatase [2] 水平抑制肝糖異生，具有治療糖尿病的潛力； iii) 刺激 AMP 活化蛋白激酶 (AMPK)，最初用于抑制肝臟合成甘油三酯和膽固醇[3]。

AICAR（處理 48 小時(shí)）抑制套細(xì)胞淋巴瘤 (MCL) 細(xì)胞系 REC-1、JEKO-1、UPN-1、JVM-2、MAVER-1 和 Z-138 的細(xì)胞增殖，IC50 為 0.28 , 0.59, 0.64, 0.98, 0.50, 0.14 Mm [4]。 AICAR 抑制成纖維細(xì)胞 [5] 中嘧啶核苷酸庫(kù)的生長(zhǎng)和消耗，加速心臟中嘌呤核苷酸庫(kù)的補(bǔ)充 [6]，抑制脂肪酸、甾醇合成，和肝細(xì)胞中的糖異生，以及肌肉中葡萄糖攝取的增加[7]。

AICAR (500 mg/kg) 在 LPS 給藥前 1 小時(shí)腹膜內(nèi)注射到 C57BL/6J 小鼠中。 LPS 在許多主要器官中誘導(dǎo) TF mRNA 的表達(dá)，包括肺和肝[8]。與對(duì)照動(dòng)物相比，在預(yù)先接種 MCL 異種移植物的小鼠中每天給予 400 毫克/千克 AICAR，只要治療 7 天[9]。

產(chǎn)品性質(zhì)：

Cas No.:2627-69-2

別名:阿卡地新; Acadesine; AICA Riboside

化學(xué)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

儲(chǔ)存條件:Store at -20°C

注意事項(xiàng)：

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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.