1. Epigenetics
  2. AMPK

AICAR (Synonyms: Acadesine; AICA Riboside)

Cat. No.: HY-13417 Purity: 99.90%
Handling Instructions

AICAR is an activator of AMP-activated protein kinase (AMPK), down-regulates the insulin receptor expression in HepG2 cells.

For research use only. We do not sell to patients.
AICAR Chemical Structure

AICAR Chemical Structure

CAS No. : 2627-69-2

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10 mM * 1 mL in Water USD 66 In-stock
50 mg USD 60 In-stock
100 mg USD 94 In-stock
200 mg USD 156 In-stock
500 mg USD 336 In-stock
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Other Forms of AICAR:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References


AICAR is an activator of AMP-activated protein kinase (AMPK), down-regulates the insulin receptor expression in HepG2 cells.

IC50 & Target


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[1].

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[2]. 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[3].

Clinical Trial
Preparing Stock Solutions
Concentration Volume Mass 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 7.7450 mL
10 mM 0.3873 mL 1.9363 mL 3.8725 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay

AICAR is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1].

HepG2 cells (5×105 cells) are plated in 6-well culture plate dishes and then are incubated in the serum-free media for 12 h before transfection. One microgram of plasmid is transfected with FuGENE6 Transfection Reagent. After 5 h of transfection, the culture media are removed and then media supplemented with or without AICAR (0.1-1.0 mM) are added to each well. The stimulation media are changed every 24 h[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration

AICAR is dissolved in saline (Mice)[2].

Fourteen-week-old lean (Lepob/+ or Lepob/+) and ob/ob (Lepob/Lepob) male mice are uesd. After the 14-day experimental treatment (24 h after AICAR injection, including a 12-h fast), the plantar flexor complex muscle is cleanly (tendon-to-tendon) excised from an anesthetized mouse breathing 4% isoflurane. The muscle is quickly weighed and then processed for histology or frozen in liquid nitrogen and stored at −80°C. The anesthetized mice are killed by transection of the diaphragm and removal of the entire heart, after blood collection via needle puncture directly into the heart, while breathing 4% isoflurane. AICAR or saline (control) is injected subcutaneously into the lateral distal portion of the back. AICAR is administered at 0.5 mg/g per day one time for 14 days. Saline (control) is injected in volumes identical to those used for AICAR treatment in a manner identical to that of AICAR treatment. Body weight is measured prior to death.
Male 5-week-old ZDF rats are either subcutaneously injected with a single dose of AICAR (0.5 mg/g body wt) or underwent a single bout of treadmill running (60 min, speed of 25 m/min at a 5% incline). Untreated ZDF rats serve as controls (n=5 in each group). One hour after the subcutaneous AICAR injection or immediately after treadmill running, rats are killed by cervical dislocation. To avoid any effect of muscle spasm and hypoxia, red and white gastrocnemius muscles are removed within seconds and immediately freeze clamped for later determination of AMPK activity. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight







OC[[email protected]@H]1[[email protected]@H](O)[[email protected]@H](O)[[email protected]](N2C=NC(C(N)=O)=C2N)O1

Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 30 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.90%

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