AICAR phosphate (Synonyms: Acadesine phosphate; AICA Riboside phosphate)

Name: AICAR phosphate
Brand: MedChemExpress
SKU: HY-13417A
Rating: 5.0 (131 reviews)

Cat. No.: HY-13417A Purity: 99.80%: FAQs
Data Sheet SDS COA Handling Instructions

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AICAR phosphate (Acadesine phosphate) is an adenosine analog and a AMPK activator. AICAR phosphate regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR phosphate is also an autophagy, YAP and mitophagy inhibitor.

For research use only. We do not sell to patients.

AICAR phosphate Chemical Structure

CAS No. : 681006-28-0

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in Water ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in Water	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
50 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 94	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 156	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 336	In-stock	Estimated Time of Arrival: December 31
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Based on 131 publication(s) in Google Scholar

Other Forms of AICAR phosphate:

AICAR In-stock

121 Publications Citing Use of MCE AICAR phosphate

RT-PCR

: AICAR phosphate purchased from MedChemExpress. Usage Cited in: Antioxid Redox Signal. 2023 Apr 13. [Abstract]; AICAR (0.5 mM; 12 h) significantly increases the expression of Mfn2 in BUMPT Cells.

: AICAR phosphate purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 May 1;9(5):515. [Abstract]; 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 phosphate purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta Mol Basis Dis. 2018 Nov;1864(11):3723-3738. [Abstract]; The effect of AICAR on the expression of AMPK, p-AMPK, mTOR, p-mTOR, and autophagy-related protein by Western blot analysis.

: AICAR phosphate purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Apr 16;9:345. [Abstract]; AMP-activated protein kinase (AMPK) activation by AST blunts dysfunction of lipid metabolism and resistance in HepG2 cells. Representative bands of SREBP-1c nuclear protein and cytoplasmic proteins are visualized in the immunoblotting assay.

: AICAR phosphate purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Apr 16;9:345. [Abstract]; 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 phosphate purchased from MedChemExpress. Usage Cited in: J Cell Physiol. 2018 Dec;233(12):9701-9715. [Abstract]; 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 phosphate purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Jul 16;9:761. [Abstract]; 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 phosphate purchased from MedChemExpress. Usage Cited in: Int J Mol Med. 2018 May;41(5):2535-2544. [Abstract]; 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.

: AICAR phosphate purchased from MedChemExpress. Usage Cited in: Int J Mol Med. 2018 May;41(5):2535-2544. [Abstract]; 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 phosphate purchased from MedChemExpress. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2018 Feb 1;50(2):144-155. [Abstract]; 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.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

AMPK

Autophagy

Mitophagy

Human Endogenous Metabolite

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.

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 body wt^-1*day^-1 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^[3]. 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^[4].

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

Clinical Trial

Molecular Weight

356.23

Formula

C₉H₁₇N₄O₉P

CAS No.

681006-28-0

Appearance

Solid

Color

White to off-white

SMILES

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

Structure Classification

Alkaloids

Initial Source

Animals

Body

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (280.72 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.8072 mL	14.0359 mL	28.0718 mL
5 mM	0.5614 mL	2.8072 mL	5.6143 mL
10 mM	0.2807 mL	1.4036 mL	2.8072 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

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: ≥ 2.08 mg/mL (5.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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: 33.33 mg/mL (93.56 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: 99.80%

Select Batch:

Data Sheet (285 KB) SDS (252 KB)

COA (254 KB) LCMS (87 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]

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 (Lep^ob/+ or Lep^ob/+) and ob/ob (Lep^ob/Lep^ob/) 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. 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. AICAR or saline (control) is injected subcutaneously into the lateral distal portion of the back. AICAR is administered at 0.5 mgg body wt^-1day^-1 one time per day 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	[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O	1 mM	2.8072 mL	14.0359 mL	28.0718 mL	70.1794 mL
	5 mM	0.5614 mL	2.8072 mL	5.6144 mL	14.0359 mL
	10 mM	0.2807 mL	1.4036 mL	2.8072 mL	7.0179 mL
	15 mM	0.1871 mL	0.9357 mL	1.8715 mL	4.6786 mL
	20 mM	0.1404 mL	0.7018 mL	1.4036 mL	3.5090 mL
	25 mM	0.1123 mL	0.5614 mL	1.1229 mL	2.8072 mL
	30 mM	0.0936 mL	0.4679 mL	0.9357 mL	2.3393 mL
	40 mM	0.0702 mL	0.3509 mL	0.7018 mL	1.7545 mL
	50 mM	0.0561 mL	0.2807 mL	0.5614 mL	1.4036 mL
	60 mM	0.0468 mL	0.2339 mL	0.4679 mL	1.1697 mL
	80 mM	0.0351 mL	0.1754 mL	0.3509 mL	0.8772 mL
	100 mM	0.0281 mL	0.1404 mL	0.2807 mL	0.7018 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

AICAR phosphate Related Classifications

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AICAR681006-28-0AcadesineAICA RibosideAMPKAutophagyYAPMitophagyEndogenous MetaboliteAMP-activated protein kinaseYes-associated proteinMitochondrial AutophagyInhibitorinhibitorinhibit

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AICAR phosphate (Synonyms: Acadesine phosphate; AICA Riboside phosphate)

Customer Review

Other Forms of AICAR phosphate:

AICAR phosphate Related Antibodies

121 Publications Citing Use of MCE AICAR phosphate

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•Related Screening Libraries:

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View All AMPK Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

AICAR phosphate Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

AICAR phosphate Related Classifications

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