AICAR (Acadesine)
Catalog No.S1802 Synonyms: NSC105823
Molecular Weight(MW): 258.23
AICAR (Acadesine), an AMPK activator, results in accumulation of ZMP, which mimics the stimulating effect of AMP on AMPK and AMPK kinase. Phase 3.
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Cultured hepatocytes were treated with 10 μM Compound C (Comp.C) for 30 min before treatment with 10 μM SAL, 1 mM AICAR for 3 h. Cell lysates were immunoblotted for the phosphorylation of AMPK, ACC, Akt and GSK3β. *P < 0.05, **P < 0.01 versus control; ##P < 0.01 versus SAL alone; †P < 0.05, ††P < 0.01 versus AICAR alone. Values are means ± SEM (n = 4).
British Journal of Pharmacology, 2015, 172(13):3284–3301.. AICAR (Acadesine) purchased from Selleck.
Representative western blots and quantitative analysis of NRF-1 and TFAM (A), SOD2 and UCP2 (B).
Sci Rep, 2016, 6:30272.. AICAR (Acadesine) purchased from Selleck.
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Activation of AMPK with AICAR reduced INH-caused inhibition of mitochondrial biogenesis by activation of SIRT1-PGC1α pathway. HepG2 cells were exposed to INH (60mM) for 24 h in the presence or absence of an AMPK activator AICAR (0.095 mM). Expressions of PGC1α, NRF1 and COX IV (B) were analyzed by western blotting.
J Appl Toxicol, 2017, 37(10):1219-1224. AICAR (Acadesine) purchased from Selleck.
Relative StAR (D) mRNAs levels in granulosa cells cultured for 4 h in the absence or presence of 10 ng/ml FSH, or together with AMPK activator (1 mM AICAR). Relative expression level was normalized to 18S rRNA. Data are expressed as fold differences ± SEM of three independent experiments using tissues from different hens and are compared to control cells. *, P < 0.05 compared to control cells; #, P < 0.05 compared to cells only stimulated by 10 ng/ml FSH.
PLoS One, 2017, 12(1):e0170409. AICAR (Acadesine) purchased from Selleck.
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Biological Activity
| Description | AICAR (Acadesine), an AMPK activator, results in accumulation of ZMP, which mimics the stimulating effect of AMP on AMPK and AMPK kinase. Phase 3. | |||||||||||||||||||||||
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| Features | A potential first-in-class adenosine regulating agent (ARA). | |||||||||||||||||||||||
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| In vitro |
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. [1] 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. [2] 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. [3] Acadesine causes a concentration-related reduction in CD18 expression on LPS-stimulated neutrophils in vitro. [4] Acadesine significantly (1 mM) inhibits N-formyl-methionyl-leucyl-phenylalanine-induced granulocyte CD11b up-regulation by a mean of 61% in blood. [5] |
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| Cell Data |
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| In vivo | Acadesine (50 mg/kg) significantly reduces tumor formation in a mouse xenograft model of K562 cells. [3] 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. [4] |
Protocol
| Cell Research: |
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Solubility (25°C)
| In vitro | DMSO | 51 mg/mL (197.49 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 2% DMSO+40% PEG 300+2% Tween 80+ddH2O For best results, use promptly after mixing. |
6mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 258.23 |
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| Formula | C9H14N4O5 |
| CAS No. | 2627-69-2 |
| Storage | powder |
| in solvent | |
| Synonyms | NSC105823 |
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Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01813838 | Terminated | SMD | Groupe Francophone des Myelodysplasies|Advancell - Advanced In Vitro Cell Technologies S.A. | June 2013 | Phase 1|Phase 2 |
| NCT00872001 | Terminated | Coronary Artery Bypass|Myocardial Infarction|Ventricular Dysfunction Left|Stroke|Cardiopulmonary Bypass | Merck Sharp & Dohme Corp.|Duke Clinical Research Institute | April 2009 | Phase 3 |
| NCT00559624 | Completed | Leukemia B-Cell Chronic | Advancell - Advanced In Vitro Cell Technologies S.A.|Nexus Oncology Ltd | December 2007 | Phase 1|Phase 2 |
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