AICAR
AICAR is a cell-permeable, allosteric activator of AMP-activated protein kinase (AMPK).
AMPK is a heterodimeric protein serine/threonine kinase that regulates the energy status of cells to protect cell from metabolic stress. AMPK phosphorylates various metabolic enzymes to activate catabolic pathways (e.g. ketogenesis) and block anabolic pathways (e.g. protein synthesis).
In rat primary astrocytes, microglia, and peritoneal macrophages, AICAR does-dependently inhibits the LPS-induced production of TNFα, IL-1β, and IL-6. AICAR treatment also blocks LPS-induced nitrite production and iNOS gene expression in those cells in a dose-dependent manner by activation of AMPK. Moreover, AICAR inhibits the LPS-induced C/EBP nuclear relocation via downregulating the expression of C/EBP-δ. [1]
In LPS-injected rats, AICAR treatment abolishes LPS-mediated increased levels of IL-1β and IFN-γ in serum. AICAR treatment also strongly inhibits the LPS-induced expression of iNOS in peritoneal macrophages isolated from these rats. Furthermore, the intraperitoneal injection of LPS significantly induces the expression of TNFα, IL-1β, and IFN-γ message in the rat spleen.
Reference:
1. Giri S, Nath N, Smith B et al. 5-aminoimidazole-4-carboxamide-1-beta-4-ribofuranoside inhibits proinflammatory response in glial cells: a possible role of AMP-activated protein kinase. J Neurosci. 2004 Jan 14;24(2):479-87.
- 1. Alexei Vazquez, et al. "Inhibition of mitochondrial folate metabolism drives differentiation through mTORC1 mediated purine sensing." Nat Commun. 2024 Mar 2;15(1):1931. PMID: 38431691
- 2. Lin Xu, et al. "Hygrothermal stress increases malignant arrhythmias susceptibility by inhibiting the LKB1-AMPK-Cx43 pathway." Sci Rep. 2024 Feb 29;14(1):5010. PMID: 38424223
- 3. Yachun Han, Shan Xiong, et al. "Lipophagy deficiency exacerbates ectopic lipid accumulation and tubular cells injury in diabetic nephropathy." Cell Death Dis. 2021 Oct 30;12(11):1031. PMID: 34718329
- 4. Mengqiu Yuan, Ronghui Yan, et al. "CARS senses cysteine deprivation to activate AMPK for cell survival." EMBO J. 2021 Nov 2;40(21):e108028. PMID: 34472622
- 5. Siwei Xia, Zhimin Wang, et al. "Dihydroartemisinin regulates lipid droplet metabolism in hepatic stellate cells by inhibiting lncRNA-H19-induced AMPK signal." Biochem Pharmacol. 2021 Oct;192:114730. PMID: 34400125
- 6. Duan Li, XiaoyanWang, et al. "LncRNA ZNF674-AS1 regulates granulosa cell glycolysis and proliferation by interacting with ALDOA." Cell Death Discov. 2021 May 16;7(1):107. PMID: 33993190
- 7. Li N, Wang Y, et al. "Tankyrase disrupts metabolic homeostasis and promotes tumorigenesis by inhibiting LKB1-AMPK signalling." Nat Commun. 2019 Sep 25;10(1):4363.nbsp;PMID: 31554794
- 8. Murakami S, Nemazanyy I, et al. "A Yap-Myc-Sox2-p53 Regulatory Network Dictates Metabolic Homeostasis and Differentiation in Kras-Driven Pancreatic Ductal Adenocarcinomas." Dev Cell. 2019 Aug 12. pii: S1534-5807(19)30628-8. PMID: 31447265
- 9. Wei Q, Zhang B, et al. "Maslinic Acid Inhibits Colon Tumorigenesis by the AMPK-mTOR Signaling Pathway." J Agric Food Chem. 2019 Apr 17;67(15):4259-4272. PMID: 30913881
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| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 258.23 |
| Cas No. | 2627-69-2 |
| Formula | C9H14N4O5 |
| Synonyms | GP 1-110 |
| Solubility | insoluble in EtOH; ≥12.9 mg/mL in DMSO; ≥52.9 mg/mL in H2O |
| Chemical Name | 5-amino-1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]imidazole-4-carboxamide |
| SDF | Download SDF |
| Canonical SMILES | CC(C=C(C)C=CC(=O)NO)C(=O)C1=CC=C(C=C1)N(C)C |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
Rat primary astrocytes, microglia and peritoneal macrophages |
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Preparation method |
The solubility of this compound in DMSO is limited. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 °C for several months. |
|
Reaction Conditions |
0.01 ~ 1 mM; 2 hrs |
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Applications |
In rat primary astrocytes, microglia and peritoneal macrophages, AICAR does-dependently inhibited the LPS-induced production of TNFα, IL-1β and IL-6. |
| Animal experiment [1]: | |
|
Animal models |
LPS-injected rats |
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Dosage form |
100 mg/kg; i.p. |
|
Applications |
In LPS-injected rats, AICAR abolished LPS-mediated increased levels of IL-1β and IFN-γ in serum. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Giri S, Nath N, Smith B et al. 5-aminoimidazole-4-carboxamide-1-beta-4-ribofuranoside inhibits proinflammatory response in glial cells: a possible role of AMP-activated protein kinase. J Neurosci. 2004 Jan 14;24(2):479-87. |
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