AICAR (Synonyms: Acadesine, AICA-Riboside, NSC 105823) |
| カタログ番号GC10518 |
AICAR（acadesineとも呼ばれる）はプリンヌクレオシドの一つである。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2627-69-2
Sample solution is provided at 25 µL, 10mM.
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AICAR（acadesineとも呼ばれる）はプリンヌクレオシドの一つである。AICARの三つの薬理的な応用を確認する：i)、虚血の条件では心臓に刺激を与え、血管血管拡張剤アデノシンを産生させる [1]： ii)フルクトース-1，6-ビスホスファターゼ[2]のレベルで肝臓糖異生を阻害し、糖尿病を治療する潜在力がある：iii)AMP活性化プロテインキナーゼ(AMPK)を刺激し、最初はトリグリセリドとコレステロールの肝臓合成の阻害で応用する[3]。
AICAR（48時間処理する）マントル細胞リンパ腫（MCL）細胞株REC-1、JEKO-1、UPN-1、JVM-2、MAVER-1、Z-138の細胞増殖を阻害し、IC50はそれぞれ0.28、0.59であり、それぞれ0.64、0.98、0.50、0.14 Ｍmである[4]。 AICAR線維芽細胞におけるピリミジンヌクレオチドプールの成長と消耗を阻害する[5]。心臓におけるプリンヌクレオチドバンクの補充を加速し[6]、肝細胞における脂肪酸、ステロールの合成おｙｐびグルコネオージンを阻害し、筋肉におけるグルコース摂取を増加させる[7]。
LPS投与の1時間前にC57BL/6J 鼠にAICAR (500 mg/kg)を腹腔内注射する。LPS は肺と肝臓を含んでいる大勢な臓器におけるTF mRNAの発見を誘発する[8]。対照群の動物と比較して、前にMCL異種移植片を接種した鼠にAICARを1日400mg/kg投与し、治療7日後腫瘍負荷を顕著に低下させられる[9]。
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.
| 細胞実験[1]: | |
細胞株 | 9 つの人の MCL 細胞株 (GRANTA-519、JVM-2、JEKO-1、Z-138、MAVER-1、REC-1、UPN-1、HBL-2、および MINO) |
準備方法 | MCL 細胞株を、0.1 ～ 2 mM の範囲の用量で AICAR とともに 24 または 48 時間孵化する。 |
反応条件 | 0.1 ~2 mM、24時間または48時間続く。 |
アプリケーション | 大体の分析細胞株（REC-1、JEKO-1、UPN-1、JVM-2、MAVER-1 および Z-138）アカデシンインキュベーション48時間后のIC50は1mM未満である。 |
| 動物実験 [2]: | |
動物モデル | メスのヌード NMRI 鼠 |
準備方法 | 鼠は、それぞれ 15 匹の動物を含んでいる 2 つの実験グループに無作為に分けられる。両群の動物の両脇腹に、5×106個のK562白血病細胞を100μl注射する。腫瘍が 150 ～ 200 mm3 に達したとき、動物に 0.9%の NaCl または AICAR を 50 mg/kg の体重の用量レベルで腹腔内注射する。 |
投与形態 | 腹腔内注射、0、0.25、0.5、1または2 mg |
アプリケーション | AICAR はヌード鼠の腫瘍形成を顕著に減少させる。腫瘍サイズの統計分析によって、16 日目には 68%、20 日目には 51% という大幅な減少が示される。 |
References: | |
| Cas No. | 2627-69-2 | SDF | |
| 同義語 | Acadesine, AICA-Riboside, NSC 105823 | ||
| Chemical Name | 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 | ||
| Formula | C9H14N4O5 | M.Wt | 258.23 |
| 溶解度 | ≥ 12.9 mg/mL in DMSO, ≥ 52.9 mg/mL in Water | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.8725 mL | 19.3626 mL | 38.7252 mL |
| 5 mM | 0.7745 mL | 3.8725 mL | 7.745 mL |
| 10 mM | 0.3873 mL | 1.9363 mL | 3.8725 mL |
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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