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Reagents and instruments for immunology, cell biology and molecular biology.

AICAR [2627-69-2]

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Cat# HY-13417-50mg

Size : 50mg

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Phone : +1 850 650 7790

Brand : MedChemExpress

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Phone : +1 850 650 7790

Description

AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR is also an autophagy, YAP and mitophagy inhibitor. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR inhibits autophagy through a mechanism independent of AMPK activity^[1]^[2]^[6].

IC₅₀ & Target^[1]

AMPK

Autophagy

Mitophagy

Human Endogenous Metabolite

Cellular Effect

Cell Line	Type	Value	Description	References
CCRF-CEM	IC₅₀	210 μM Compound: 13, AICA	Cytostatic activity against human CEM cells assessed as growth inhibition after 3 days by particle counting analysis Cytostatic activity against human CEM cells assessed as growth inhibition after 3 days by particle counting analysis	[PMID: 24177359]
HCT-116	EC₅₀	>100 μM Compound: AICAR	Cytotoxicity against human HCT-116 cells incubated for 48 hrs by MTT assay Cytotoxicity against human HCT-116 cells incubated for 48 hrs by MTT assay	[PMID: 36518704]
HCT-116	EC₅₀	>100 μM Compound: AICAR	Cytotoxicity against human HCT-116 cells overexpressing human BCRP incubated for 48 hrs by MTT assay Cytotoxicity against human HCT-116 cells overexpressing human BCRP incubated for 48 hrs by MTT assay	[PMID: 36518704]
HCT-116	EC₅₀	>100 μM Compound: AICAR	Cytotoxicity against human HCT-116 cells overexpressing human MDR1 incubated for 48 hrs by MTT assay Cytotoxicity against human HCT-116 cells overexpressing human MDR1 incubated for 48 hrs by MTT assay	[PMID: 36518704]
HEK293	EC₅₀	>100 μM Compound: AICAR	Cytotoxicity against human HEK293 cells incubated for 48 hrs by MTT assay Cytotoxicity against human HEK293 cells incubated for 48 hrs by MTT assay	[PMID: 36518704]
HEL	EC₅₀	>100 μM Compound: 13, AICA	Antiviral activity against acyclovir-resistant thymidine kinase-deficient Herpes simplex virus 1 KOS infected in HEL cells assessed as inhibition of virus-induced cytopathicity Antiviral activity against acyclovir-resistant thymidine kinase-deficient Herpes simplex virus 1 KOS infected in HEL cells assessed as inhibition of virus-induced cytopathicity	[PMID: 24177359]
HEL	EC₅₀	>100 μM Compound: 13, AICA	Antiviral activity against Herpes simplex virus 1 KOS infected in HEL cells assessed as inhibition of virus-induced cytopathicity Antiviral activity against Herpes simplex virus 1 KOS infected in HEL cells assessed as inhibition of virus-induced cytopathicity	[PMID: 24177359]
HEL	EC₅₀	>100 μM Compound: 13, AICA	Antiviral activity against Herpes simplex virus 2 G infected in HEL cells assessed as inhibition of virus-induced cytopathicity Antiviral activity against Herpes simplex virus 2 G infected in HEL cells assessed as inhibition of virus-induced cytopathicity	[PMID: 24177359]
HeLa	IC₅₀	>=250 μM Compound: 13, AICA	Cytostatic activity against thymidine kinase-deficient human HeLa cells assessed as growth inhibition after 3 days by particle counting analysis Cytostatic activity against thymidine kinase-deficient human HeLa cells assessed as growth inhibition after 3 days by particle counting analysis	[PMID: 24177359]
HeLa	IC₅₀	≥ 250 μM Compound: 13, AICA	Cytostatic activity against thymidine kinase-deficient human HeLa cells assessed as growth inhibition after 3 days by particle counting analysis Cytostatic activity against thymidine kinase-deficient human HeLa cells assessed as growth inhibition after 3 days by particle counting analysis	[PMID: 24177359]
HeLa	IC₅₀	165 μM Compound: 13, AICA	Cytostatic activity against human HeLa cells assessed as growth inhibition after 3 days by particle counting analysis Cytostatic activity against human HeLa cells assessed as growth inhibition after 3 days by particle counting analysis	[PMID: 24177359]
K562	IC₅₀	800 μM Compound: Aca	Antileukemic activity against human K562 cells after 48 hrs by XTT assay Antileukemic activity against human K562 cells after 48 hrs by XTT assay	[PMID: 28094938]
K562	IC₅₀	800 μM Compound: AICAR	Cytotoxicity in drug sensitive human K562 cells assessed as reduction cell viability incubated for 48 hrs by XTT assay Cytotoxicity in drug sensitive human K562 cells assessed as reduction cell viability incubated for 48 hrs by XTT assay	[PMID: 29655981]
K-562R	IC₅₀	800 μM Compound: AICAR	Cytotoxicity in imatinib-resistant human K562R cells assessed as reduction cell viability incubated for 48 hrs by XTT assay Cytotoxicity in imatinib-resistant human K562R cells assessed as reduction cell viability incubated for 48 hrs by XTT assay	[PMID: 29655981]
L1210	IC₅₀	>=250 μM Compound: 13, AICA	Cytostatic activity against mouse L1210 cells assessed as growth inhibition after 2 days by particle counting analysis Cytostatic activity against mouse L1210 cells assessed as growth inhibition after 2 days by particle counting analysis	[PMID: 24177359]
L1210	IC₅₀	≥ 250 μM Compound: 13, AICA	Cytostatic activity against mouse L1210 cells assessed as growth inhibition after 2 days by particle counting analysis Cytostatic activity against mouse L1210 cells assessed as growth inhibition after 2 days by particle counting analysis	[PMID: 24177359]
MDA-MB-231	IC₅₀	1 mM Compound: AICAR	Anticancer activity against human MDA-MB-231 cells after 48 hrs by XTT assay Anticancer activity against human MDA-MB-231 cells after 48 hrs by XTT assay	[PMID: 28325600]
MDA-MB-231	IC₅₀	1000 μM Compound: AICAR	Anticancer activity against human MDA-MB-231 cells after 48 hrs by XTT assay Anticancer activity against human MDA-MB-231 cells after 48 hrs by XTT assay	[PMID: 28325600]
MDA-MB-453	IC₅₀	1700 μM Compound: AICAR	Antiproliferation activity against human MDA-MB-453 cells assessed as reduction in cell viability measured after 4 days by Celltiter-glo luminescent cell viability assay Antiproliferation activity against human MDA-MB-453 cells assessed as reduction in cell viability measured after 4 days by Celltiter-glo luminescent cell viability assay	[PMID: 32007387]
RCC4	IC₅₀	250 μM Compound: AICAR	Anticancer activity against human RCC4 cells after 48 hrs by XTT assay Anticancer activity against human RCC4 cells after 48 hrs by XTT assay	[PMID: 28325600]
SK-BR-3	IC₅₀	180 μM Compound: AICAR	Antiproliferation activity against human SK-BR-3 cells assessed as reduction in cell viability measured after 4 days by Celltiter-glo luminescent cell viability assay Antiproliferation activity against human SK-BR-3 cells assessed as reduction in cell viability measured after 4 days by Celltiter-glo luminescent cell viability assay	[PMID: 32007387]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Solvent & Solubility

In Vitro:

DMSO : 116.67 mg/mL (451.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (19.36 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (19.36 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (19.36 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 110 mg/mL (425.98 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.99%

Data Sheet (286 KB) SDS (393 KB)

COA (255 KB) HNMR (283 KB) RP-HPLC (255 KB) MS (69 KB) Elemental Analysis Report (113 KB)

Handling Instructions (2659 KB)

References

[1]. Nakamaru K, et al. AICAR, an activator of AMP-activated protein kinase, down-regulates the IR expression in HepG2 cells. Biochem Biophys Res Commun. 2005 Mar 11;328(2):449-54 [Content Brief]

[2]. Giri S, 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. [Content Brief]

[3]. Drake JC, et al. AICAR treatment for 14 days normalizes obesity-induced dysregulation of TORC1 signaling and translational capacity in fasted skeletal muscle. Am J Physiol Regul Integr Comp Physiol. 2010 Dec;299(6):R1546-54. [Content Brief]

[4]. Pold R, et al. Long-term AICAR administration and exercise prevents diabetes in ZDF rats.Diabetes. 2005 Apr;54(4):928-34. [Content Brief]

[5]. Ajaybabu V Pobbati, et al. A combat with the YAP/TAZ-TEAD oncoproteins for cancer therapy. Theranostics. 2020 Feb 18;10(8):3622-3635. [Content Brief]

[6]. Viana R, et al. Role of AMP-activated protein kinase in autophagy and proteasome function. Biochem Biophys Res Commun. 2008 May 9;369(3):964-8. [Content Brief]

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Cat# HY-13417-50mg

Contact local distributor :

Brand : MedChemExpress

Contact local distributor :

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