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AICAR (Synonyms: Acadesine, AICA-Riboside, NSC 105823)

Katalog-Nr.GC10518

Ein Aktivator von AMPK

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AICAR Chemische Struktur

Cas No.: 2627-69-2

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10mM (in 1mL DMSO)
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

Nine human MCL cell lines (GRANTA-519, JVM-2, JEKO-1, Z-138, MAVER-1, REC-1, UPN-1, HBL-2 and MINO)

Preparation Method

MCL cell lines were incubated with AICAR at doses ranging from 0.1 to 2 mM for 24 or 48 hours.

Reaction Conditions

0.1 to 2 mM for 24 or 48 hours.

Applications

Most of the cell lines analyzed (REC-1, JEKO-1, UPN-1, JVM-2, MAVER-1 and Z-138) showed a IC50 lower than 1 mM after 48 hours of acadesine incubation.

Animal experiment [2]:

Animal models

Female Nude NMRI Mice

Preparation Method

Mice were randomized into two experimental groups, each containing 15 animals. Animals in both groups received a 100 µl injection of 5*106 K562 leukemia cells on both flanks. When tumors reached 150-200 mm3, animals were injected intraperitoneally with NaCl 0.9% or AICAR at dose level of 50 mg/kg body weight.

Dosage form

Intraperitoneal injection, 0, 0.25, 0.5, 1 or 2 mg

Applications

AICAR significantly reduced tumor formation in nude mice. Statistical analysis of tumor size shows a robust reduction of 68% at day 16 and 51% at day 20.

References:

[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.

Background

AICAR (auch Acadesin genannt) ist ein Purinnukleosid. Drei pharmakologische Anwendungen von AICAR wurden identifiziert: i) Stimulation der kardialen Produktion des Vasodilatators Adenosin unter ischämischen Bedingungen [1]; ii) Hemmung der hepatischen Gluconeogenese auf Ebene der Fructose-1,6-bisphosphatase [2], mit therapeutischem Potenzial bei Diabetes; und iii) Stimulation der AMP-aktivierten Proteinkinase (AMPK), die ursprünglich zur Hemmung der hepatischen Synthese von Triglyceriden und Cholesterin angewendet wurde [3].

AICAR (behandelt für 48 Stunden) hemmte die Zellproliferation von Mantelzelllymphom (MCL)-Zelllinien REC-1, JEKO-1, UPN-1, JVM-2, MAVER-1 und Z-138 mit IC50-Werten von jeweils 0,28; 0,59; 0,64; 0.98; 0.50 und 0.14 Mm [4]. AICAR hemmte das Wachstum und den Abbau von Pyrimidinnukleotid-Pools in Fibroblasten [5], beschleunigte die Wiederherstellung der Purinnukleotid-Pools im Herzen [6], hemmte Fettsäure-, Sterolsynthese und Gluconeogenese in Hepatozyten sowie erhöhte die Glukoseaufnahme in Muskeln [7].

AICAR (500 mg/kg) wurde intraperitoneal in C57BL/6J-Mäuse injiziert, eine Stunde vor der Verabreichung von LPS. LPS induzierte die Expression von TF-mRNA in vielen wichtigen Organen, einschließlich der Lunge und Leber [8]. Eine tägliche Verabreichung von 400mg/kg AICAR bei Mäusen, die zuvor mit einem MCL-Xenotransplantat geimpft wurden, reduzierte signifikant die Tumorlast im Vergleich zu Kontrolltieren bereits nach 7 Tagen Behandlung [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.

Chemical Properties

Cas No. 2627-69-2 SDF
Überlieferungen 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
Löslichkeit ≥ 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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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