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Cat. No. M4897
AICAR Structure


Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL In DMSO USD 58 In stock
50mg USD 50 In stock
100mg USD 80 In stock
200mg USD 120 In stock
500mg USD 240 In stock
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Quality Control
Biological Activity

In vitro: HepG2 cells are treated with various concentrations of AICAR (0.1-1.0 mM) for 12, 24, and 48 h, respectively. The expression level of IR-β significantly decreases with 0.25, 0.5, and 1.0 mM of AICAR at 48 h to 50%, 53%, and 46% of the control, respectively.

In vivo: Fourteen-week-old male, lean (L; 31.3 g body wt) wild-type andob/ob (O; 59.6 g body wt) mice are injected with the AMP-activated kinase (AMPK) activator AICAR (A) at 0.5 mg/g per day or saline control (C) for 14 days. At 24 h after the last injection (including a 12-h fast), all mice are killed, and the plantar flexor complex muscle (gastrocnemius, soleus, and plantaris) is excised for analysis. Muscle mass is lower in OC (159±12 mg) than LC, LA, and OA (176±10, 178±9, and 166±16 mg, respectively) mice, independent of a body weight change. The kidney weight is significantly higher in the untreated group when compared with both the exercise and AICAR (0.5 mg/g body wt) groups. The heart weight is higher in the exercise group than in the other groups, whereas the liver weight is significantly higher in the AICAR-treated group when compared with the exercise and untreated groups.

Customer Product Validations & Biological Datas
Source Sci Rep (2018). Figure 1. AICAR
Method Cytometric bead array assays
Cell Lines Human peripheral blood mononuclear cells
Concentrations 1 mM
Incubation Time 24 h
Results Inhibition of adenosine kinase-mediated AICAR phosphorylation to ZMP, using the inhibitor ABT-702, left suppression of LPS-induced target genes by AICAR unaltered and even potentiated the effect of low AICAR concentrations, suggesting an AMPK-independent effect.
Cell Experiment
Cell lines K562 cell lines
Preparation method 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.
Concentrations 2.5 mM
Incubation time 10 days
Animal Experiment
Animal models mouse xenograft model of K562 cells
Formulation 0.9% NaCl
Dosages 50 mg/kg
Administration Injected intraperitoneally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 258.23
Formula C9H14N4O5
CAS Number 2627-69-2
Purity >99%
Solubility DMSO: ≥ 30 mg/mL
Storage at -20°C

Acadesine kills chronic myelogenous leukemia (CML) cells through PKC-dependent induction of autophagic cell death.
Robert G, et al. PLoS One. 2009 Nov 18;4(11):e7889. PMID: 19924252.

AICAR, an activator of AMP-activated protein kinase, down-regulates the insulin receptor expression in HepG2 cells.
Nakamaru K, et al. Biochem Biophys Res Commun. 2005 Mar 11;328(2):449-54. PMID: 15694368.

Acadesine activates AMPK and induces apoptosis in B-cell chronic lymphocytic leukemia cells but not in T lymphocytes.
Campas C, et al. Blood. 2003 May 1;101(9):3674-80. PMID: 12522004.

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Keywords: AICAR, Acadesine supplier, AMPK, inhibitors

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