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.
Front Oncol. 2022 Jul 28;12:968547.
Comprehensive analysis of the glutathione S-transferase Mu (GSTM) gene family in ovarian cancer identifies prognostic and expression significance
AICAR purchased from AbMole
Research Square. 2022 May.
Perfluorooctane sulfonic acid induces liver lipid accumulation through AMPK/ACC signaling
AICAR purchased from AbMole
 |
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 |
| Molecular Weight | 258.23 |
| Formula | C9H14N4O5 |
| CAS Number | 2627-69-2 |
| Solubility (25°C) | DMSO ≥ 50 mg/mL Water 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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