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    Acadesine (AICAR; NSC-105823)
    Acadesine (AICAR; NSC-105823)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0245
    CAS #: 2627-69-2Purity ≥98%

    Description: Acadesine (also known as NSC105823, AICA-riboside, and AICAR) is a novel and potent AMPK (AMP-activated protein kinase) activator with potential antitumor and antidiabetic activity. It is used for the treatment of acute lymphoblastic leukemia (AML) and may have applications in treating other disorders such as diabetes. 

    References: Eur J Biochem. 1995 Apr 15;229(2):558-65; PLoS One. 2009 Nov 18;4(11):e7889; Surgery. 1996 Mar;119(3):302-15.

    Related CAS: 681006-28-0 (AICAR phosphate)

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    Molecular Weight (MW)

    258.23

    Formula

    C9H14N4O5

    CAS No.

    2627-69-2

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: 51 mg/mL (197.5 mM)

    Water: <1 mg/mL

    Ethanol: <1 mg/mL

    Other info

    Chemical Name: 1H-Imidazole-4-carboxamide, 5-amino-1-(5-O-phosphono-beta-D-ribofuranosyl)- (9CI)
    InChi Key: NOTGFIUVDGNKRI-UUOKFMHZSA-N
    InChi Code: 1S/C9H15N4O8P/c10-7-4(8(11)16)12-2-13(7)9-6(15)5(14)3(21-9)1-20-22(17,18)19/h2-3,5-6,9,14-15H,1,10H2,(H2,11,16)(H2,17,18,19)/t3-,5-,6-,9-/m1/s1
    SMILES Code: c1nc(c(n1[[email protected]]2[[email protected]@H]([[email protected]@H]([[email protected]](O2)COP(=O)(O)O)O)O)N)C(=O)N

    Synonyms

    AICA ribonucleotide, AICA riboside, AICAR; Acadesine; AICA Riboside; ARA100; ARA-100; ARA 100; GP 1 110; SCH-900395; SCH 900395; SCH900395; AICAR

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    In Vitro

    In vitro activity: Acadesine (500 μM) increases the ZMP content in extracts of isolated hepatocytes after up to 30-40 min treatment, then remains fairly constant at approximately 4 nmol/g. Acadesine (500 μM) causes a transient 12-fold activation of AMPK at 15 min in rat hepatocytes and 2-3 fold activation of AMPK in adipocytes, without affecting levels of ATP, ADP or AMP. Acadesine (500 μM) causes a dramatic inhibition of both fatty acid and sterol synthesis in rat hepatocytes. Acadesine (500 μM) also causes a dramatic inactivation of HMG-CoA reductase. Acadesine induces apoptosis of B-CLL cells in a dose-dependent manner with EC50 of 380 μM. Acadesine (0.5 mM) decreases cell viability of B-CLL cells from 20 representative patients from 68% to 26%. Acadesine (0.5 mM) induces caspase activation and cytochrome crelease from mitochondria. Uptake and phosphorylation of Acadesine (0.5 mM) are required to induce apoptosis and activate AMPK in B-CLL cells. Acadesine (2-4 mM) only slightly affects the viability of T cells from B-CLL patients, Acadesine (0.5 mM) remarkedly reduces viability of B cells but not T cells. Acadesine triggers loss of cell metabolism in K562, LAMA-84 and JURL-MK1 and is also effective in killing imatinib-resistant K562 cells and Ba/F3 cells carrying the T315I-BCR-ABL mutation. The effect of Acadesine is abrogated by GF109203X and Ro-32-0432, both inhibitor of classical and new PKCs and accordingly, Acadesine triggers relocation and activation of several PKC isoforms in K562 cells. Acadesine dose-dependently inhibits K562 colony formation at day 10, the growth inhibitory effect of acadesine is already detected at 0.25 mM and is maximal at 2.5 mM. Acadesine causes a concentration-related reduction in CD18 expression on LPS-stimulated neutrophils in vitro. Acadesine significantly (1 mM) inhibits N-formyl-methionyl-leucyl-phenylalanine-induced granulocyte CD11b up-regulation by a mean of 61% in blood.

     

    Kinase Assay: AICAR is a cell-permeable AMP-activated protein kinase (AMPK) activator.

     

    Cell Assay: Acadesine is added to K562 cell lines or primary cells (103 CD34+ cells/mL) growing in semisolid methyl cellulose medium. MethoCult H4100 or H4236 are used for cell lines and primary CD34+ cells respectively. Colonies are detected after 10 days of culture by adding 1 mg/mL of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) reagent and are scored by Image J quantification software.

    In Vivo

    Acadesine (50 mg/kg) significantly reduces tumor formation in a mouse xenograft model of K562 cells. Acadesine (10 mg/kg) results in higher fluid required to stabilize hemodynamics in pigs. Acadesine (10 mg/kg) inhibits LPS-induced protein permeability of pulmonary capillaries, peak inspiratory pressures on constant tidal volume and dead space ventilation in pigs.

    Animal model

    Mouse xenograft model of K562 cells

    Formulation & Dosage

    Dissolved in 0.9% NaCl; 50 mg/kg; i.p. administration

    References

    Eur J Biochem. 1995 Apr 15;229(2):558-65; PLoS One. 2009 Nov 18;4(11):e7889; Surgery. 1996 Mar;119(3):302-15..


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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