1. Epigenetics
    PI3K/Akt/mTOR
    Autophagy
  2. AMPK
    Autophagy
    Mitophagy

AICAR (Synonyms: Acadesine; AICA Riboside)

Cat. No.: HY-13417 Purity: 99.92%
Handling Instructions

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

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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Customer Review

Other Forms of AICAR:

    AICAR purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Apr 16;9:345.

    AMP-activated protein kinase (AMPK) activation by AST blunts dysfunction of lipid metabolism and insulin resistance in HepG2 cells. Representative bands of SREBP-1c nuclear protein and cytoplasmic proteins are visualized in the immunoblotting assay.

    AICAR purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Apr 16;9:345.

    AMP-activated protein kinase activation by AST inhibits the expression of sterol regulatory element binding protein-1c (SREBP-1c) and SREBP-1c related genes. AST promotes AMPKa1 mRNA expression, AMPKa2 mRNA expression, and suppresses the expression of SREBP-1c, and its downstream genes FAS, ACC1, and also AMPK downstream gene SCD1.

    AICAR purchased from MCE. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2018 Feb 1;50(2):144-155.

    Autophagy is involved in Rg1-inhibited apoptosis in macrophages Macrophages with serum deprivation are treated with 50 μM Rg1 for 48 h in the absence or presence of 3-MA (5 mM). The protein expression level of cleaved caspase-3 determined by western blot analysis in Raw264.7 macrophages.

    AICAR purchased from MCE. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2018 Feb 1;50(2):144-155.

    Raw264.7 macrophages with serum deprivation are treated with 50 μM Rg1 for 48 h in absence or presence of compound C (10 mM) or AICAR (250 μM). Western blots of the protein expressions of Atg5, Beclin1, LC3, and p62/SQSMT1.

    AICAR purchased from MCE. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2018 Feb 1;50(2):144-155.

    Raw264.7 macrophages treated without or with Rapamycin (1 μΜ) or Chloroquine (20 μΜ) for 48 h. Western blot shows the protein expression levels of Atg5, Beclin1, LC3, and p62/SQSMT1.

    AICAR purchased from MCE. Usage Cited in: Cell Death Dis. 2018 May 1;9(5):515.

    Protein expression levels of AMPKα, p-AMPKα-thr172, p-ACC-ser79, LC3, Beclin-1, ATG5 and ATG7 in WT MSCs or control CrispCas MSCs, or AMPKα DKO MSCs before and after treatment with FAC or AICAR.

    AICAR purchased from MCE. Usage Cited in: J Cell Physiol. 2018 Dec;233(12):9701-9715.

    HUVECs are pretreated with Compound C (5, 10, or 20 μM) for 18 hr or AICAR (1, 2, or 4 mM) for 1 hr, and then exposed to LSS for 30 min.

    AICAR purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Jul 16;9:761.

    Epithelial cells from colon tissue are extracted from mice in each group (n=6-8 per group) and protein level of p-AMPK (Thr172) and AMPKα1/2 are measured by western blot.

    AICAR purchased from MCE. Usage Cited in: Biochim Biophys Acta Mol Basis Dis. 2018 Nov;1864(11):3723-3738.

    The effect of AICAR on the expression of AMPK, p-AMPK, mTOR, p-mTOR, and autophagy-related protein by Western blot analysis.

    AICAR purchased from MCE. Usage Cited in: Int J Mol Med. 2018 May;41(5):2535-2544.

    Cells are treated with AICAR and AICAR (A++, 10 μM) + Compound C (C++, 1 μM) for 24 h, after which western blot analysis is performed.

    AICAR purchased from MCE. Usage Cited in: Int J Mol Med. 2018 May;41(5):2535-2544.

    MC3T3-E1 cells are treated with AICAR (10 μM) in the presence or absence of 3-MA (5 mM) or CQ (10 μM) for 24 h, after which western blot analysis is conducted.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

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

    IC50 & Target

    AMPK[1]

    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
    Solvent & Solubility
    In Vitro: 

    H2O : 65 mg/mL (251.71 mM; Need ultrasonic and warming)

    DMSO : ≥ 30 mg/mL (116.18 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent 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.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (9.68 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (9.68 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (9.68 mM); Clear solution

    References
    Cell Assay
    [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
    [2][3]

    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.
    Rats[3]
    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.

    References
    Molecular Weight

    258.23

    Formula

    C₉H₁₄N₄O₅

    CAS No.

    2627-69-2

    SMILES

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

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

    Room temperature in continental US; may vary elsewhere

    Purity: 99.92%

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    Product Name:
    AICAR
    Cat. No.:
    HY-13417
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    AICAR

    Cat. No.: HY-13417