AICAR (Synonyms: Acadesine, AICA-Riboside, NSC 105823) |
| Catalog No.GC10518 |
AICAR（아카데신으로도 알려져 있습니다）는 퓨린 뉴클레오사이드의 일종이다.
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（아카데신으로도 알려져 있습니다）는 퓨린 뉴클레오사이드의 일종이다. AICAR의 세 가지 의학적 응용이 식별되었다: i) 혈액 공급이 결함이 있는 조건에서 심장에서 혈관 확장제인 아데노신을 생성하는 것을 자극하는 것[1]；ii) 과당-1,6-디포스포팜팡이 수준에서 간의 혈당 생성을 억제하는 것[2]，당뇨병 치료의 잠재력이 있다；iii) AMP활성화 단백질 킨아제（AMPK）를 자극하는 것，최초로 간의 트리글리세라이드 및 콜레스테롤 합성을 억제하는 데 사용되었다[3].
AICAR（48시간 처리）는mantle cell lymphoma（MCL）의 REC-1, JEKO-1, UPN-1, JVM-2, MAVER-1, Z-138 세포계에서의 세포 증식을 억제했으며, 그 IC50 값은 각각 0.28, 0.59, 0.64, 0.98, 0.50, 0.14 mM였다[4]. AICAR은 피브로블라스트 내의 퓨리민 핵간산 풀의 성장과 소진을 억제하고[5], 심장 내의 퓨린 핵간산 풀의 보충을 가속화하며[6], 간세포 내의 지방산, 콜레스테롤 합성과 혈당 생성을 억제하고[7], 근육 내의 혈당 흡수를 증가시켰다.
AICAR（500 mg/kg）는 C57BL/6J 쥐에게 복강내 주사로 LPS 투여 1시간 전에 주어졌다. LPS는 폐와 간을 포함한 많은 주요 장기에서 TF mRNA의 표현을 유도했다[8]. MCL 이종 이식을 미리 접종한 쥐에게 매일 400mg/kg AICAR을 투여한 경우, 7일간 치료 후에 대조 동물에 비해 종양 부담이 현저히 감소했다[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.
| 세포 실험 [1]: | |
세포 라인 | 9개 종류의 인간의 맨틀 셀 림프종 (MCL) 세포 라인 (GRANTA-519, JVM-2, JEKO-1, Z-138, MAVER-1, REC-1, UPN-1, HBL-2 그리고 MINO)입니다. |
제조 방법 | MCL 세포계는 0.1에서 2 mM의 용량 범위에서 AICAR과 함께 24 또는 48시간 동안 배양되었습니다. |
반응 조건 | 0.1에서 2 mM ,24또는 48 시간 동안 |
응용 분야 | 분석된 대부분의 세포 라인 (REC-1, JEKO-1, UPN-1, JVM-2, MAVER-1, Z-138)는 아카데신 배양 48시간 후 1 mM 미만의 IC50 값을 보였습니다. |
| 동물 실험 [2]: | |
동물 모형 | 암컷 누드 NMRI 쥐 |
제조 방법 | 쥐는 두 개의 실험 그룹으로 무작위로 분류되었으며, 각 그룹에는 15마리의 동물이 포함되었습니다. 두 그룹의 동물 모두 양쪽 복강에 100µl의 5×106 K562 백혈병 세포를 주사 받았습니다. 종양이 150-200㎜³에 도달했을 때 동물들은 복강 내 주사로 0.9% NaCl 또는 체중당 50mg의 AICAR을 주사 받았습니다. |
제형 | 복강 내 주사, 0, 0.25, 0.5, 1 또는 2mg |
응용 분야 | AICAR은 누드 쥐의 종양 형성을 현저하게 감소시켰습니다. 종양 크기에 대한 통계 분석은 16일째에 68%, 20일째에 51%의 강력한 감소를 보여줍니다. |
참고문헌: [1]: 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.[2]: Robert G, Ben Sahra I, Puissant A, et al. Acadesine kills chronic myelogenous leukemia (CML) cells through PKC-dependent induction of autophagic cell death[J]. PloS one, 2009, 4(11): e7889. | |
| Cas No. | 2627-69-2 | SDF | |
| Synonyms | 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 |
| Solubility | ≥ 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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