2. GPCR/G Protein Epigenetics Cell Cycle/DNA Damage PI3K/Akt/mTOR Neuronal Signaling MAPK/ERK Pathway Membrane Transporter/Ion Channel Apoptosis
  3. Free Fatty Acid Receptor Histone Methyltransferase HDAC mTOR CaMK p38 MAPK Epigenetic Reader Domain GLUT nAChR TNF Receptor
  4. AR420626

AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3) (IC50=117 nM). AR420626 has anti-inflammatory, anticancer and antidiabetic activities. AR420626 improves neurogenic diarrhea by inhibiting nAChR mediated neural pathways. AR420626 inhibits the growth of HepG2 xenografts and inhibits the proliferation of hepatoma cells by inducing apoptosis. AR420626 also suppresses allergic asthma and eczema and has the ability to activate GPR41 to increase Ca2+ signal-mediated glucose uptake and improve diabetes.

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AR420626 Chemical Structure

AR420626 Chemical Structure

CAS No. : 1798310-55-0

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Based on 3 publication(s) in Google Scholar

AR420626 Related Antibodies

Top Publications Citing Use of Products

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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mTOR mTORC1 mTORC2

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CaMK III CaMK II

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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GLUT1 GLUT2 GLUT3 GLUT4

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TNFRSF1A/CD120a TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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  • Customer Review

Description

AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3) (IC50=117 nM). AR420626 has anti-inflammatory, anticancer and antidiabetic activities. AR420626 improves neurogenic diarrhea by inhibiting nAChR mediated neural pathways. AR420626 inhibits the growth of HepG2 xenografts and inhibits the proliferation of hepatoma cells by inducing apoptosis. AR420626 also suppresses allergic asthma and eczema and has the ability to activate GPR41 to increase Ca2+ signal-mediated glucose uptake and improve diabetes[1][2][3][4].

In Vitro

AR420626 (10 μM) inhibits 100 μM nicotine-induced contraction and 10 μM nicotine-induced relaxation of rat proximal colon circular muscle strips[1].
AR420626 (10 μM) reverses NO-mediated relaxation of circular muscles induced by 5-HT (100 μM)[1].
AR420626 (10 and 25 µM; 48 h) inhibits the proliferation of HLE cells and HepG2 cells at a concentration of 25 µM for 48 h, and induces apoptosis of HepG2 cells and HLE cells by inhibiting HDAC-induced TNF-α[2].
AR420626 (25 µM; 1, 3, 12 and 24 h) induces mTOR phosphorylation at the 1 h time point and for 24 h in HepG2 and HLE cells [2].
AR420626 (0.25, 0.5 and 1 µM; 1 h) increases Ca2+ influx and GLUT4 translocation via activation of CaMKII, CREB and p38 in C2C12 myotubes, thereby enhancing basal and insulin-stimulated glucose uptake[4].

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

AR420626 Related Antibodies

Cell Proliferation Assay[2]

Cell Line: HepG2 cells and HLE cells
Concentration: 10, 25 µM
Incubation Time: 24, 48 and 72 h
Result: Inhibited the proliferation of HepG2 cells at 25 µM for 24 h, 10 µM and 25 µM for 48 h and 72 h, and inhibited the proliferation of HLE cells at 25 µM for 48 h, 10 µM and 25 µM for 72 h.

Western Blot Analysis[2]

Cell Line: HCC cells
Concentration: 10, 25 µM
Incubation Time: 48 h
Result: Increased the expression of cleaved caspase-3 in a dose-dependent manner.
Increased cleaved caspase-8 in HCC cells in a dose-dependent manner and slightly increased cleaved caspase-9 in HepG2 cells at 25 µM.

Western Blot Analysis[2]

Cell Line: HCC cells
Concentration: 25 µM
Incubation Time: 1, 3, 12 and 24 h
Result: Reduced the levels of HDAC 4-7 at 1 h and gradually decreased to 24h, reduced the levels of HDAC 1-3 at 24h, and reduced the levels of HDAC8 at 1h and gradually decreased to 24h in HepG2 cells.
Upregulated histone H3 acetylation level at 3 h and gradually increased to 24 h in HepG2 cells.

RT-PCR[2]

Cell Line: HCC cells
Concentration: 10, 25 µM
Incubation Time: 1, 3, 12 and 24 h
Result: Increased the TNF-α mRNA level in HepG2 cells from 1 to 24 hours, reaching a peak at around 24 hours at a dose of 25µM, the TNF-α mRNA level in HLE cells from 1 to 24 hours was dose-dependent, reaching a peak at around 3 hours.
In Vivo

AR420626 (0.1 mg/kg, i.p.; single dose) inhibits serotonin-induced defecation volume in male Sprague-Dawley rats[1].
AR420626 (0.1 mg/kg, i.p.; days 0-4; 0.2 mg/kg, i.p.; days 7-11) inhibits the growth of HepG2 xenografted male SHO nude mice[2].
AR420626 (0.1 mg/kg, i.p.; administered 30 minutes before modeling) inhibits the immune response in bronchoalveolar lavage fluid (BALF) and lung tissue of the allergic asthma model induced by ovalbumins (HY-W250978) in BALB/c mice; and inhibits the skin inflammatory immune response, cervical lymph node immune response and the development of eczema symptoms in the eczema model induced by 1-chloro-2, 4-dinitrobenzene (DNCB) in BALB/c mice[3].
AR420626 (13.32 and 26.64 μg/kg, i.p.; once a day for 7 days) at a dose of 26.64 μg/kg improves glucose tolerance by increasing plasma insulin levels and skeletal muscle glycogen content in male ICR mice with Streptozotocin (HY-13753) induced diabetes and C57BL/6 mice with high-fat diet-induced diabetes[4].

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

Animal Model: HepG2 xenograft model in male SHO nude mice [2]
Dosage: 0.1 mg/kg on days 0-4 after tumors reach 500-1000 mm3
0.2 mg/kg on days 7-11 after tumors reach 500-1000 mm3
Administration: Intraperitoneal injection (i.p.)
Result: Inhibited the growth of HepG2 xenograft mice, and still had an inhibitory effect on the weight of mice after stopping administration.
Animal Model: Ovalbumin (OVA)-induced asthma induction in BALB/c mice [3]
Dosage: 0.1 mg/kg
Administration: Intraperitoneal injection 30 min before OVA sensitization (D0 and D14) or 30 min before OVA challenge (D28, D29, and D30)
Result: Suppressed the increased IL-4 and IL-17A levels.
Suppressed the increase in the number of eosinophils and total immune cells in bronchoalveolar lavage fluid (BALF).
Inhibited the increase of cytokine (IL-4, IL-13, IFN-γ and IL-17a) levels.
Animal Model: 1-chloro-2, 4-dinitrobenzene (DNCB)-induced eczema model in BALB/c mice[3]
Dosage: 0.1 mg/kg
Administration: Intraperitoneal injection 30 min before the DNCB challenge from day 19
Result: Reduced the number of accumulated immune cells and mast cells, inhibited acanthosis and epidermal thickening and mast cell accumulation, and inhibited IL-17A, TSLP and IL-8 levels.
Inhibited immune responses in the cervical lymph nodes, size enlargement, and expression of inflammatory cytokines and chemokines, but did not enhance the proportion of CD4+FoxP3+ Treg cells.
Molecular Weight

417.29

Formula

C21H18Cl2N2O3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

ClC1=CC(NC(C2=C(NC(CCC3)=C(C2C4=CC=CO4)C3=O)C)=O)=C(C=C1)Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (47.93 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3964 mL 11.9821 mL 23.9641 mL
5 mM 0.4793 mL 2.3964 mL 4.7928 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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    90% (20% SBE-β-CD in Saline)

    Solubility: 2 mg/mL (4.79 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2 mg/mL (4.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 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 (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3964 mL 11.9821 mL 23.9641 mL 59.9104 mL
5 mM 0.4793 mL 2.3964 mL 4.7928 mL 11.9821 mL
10 mM 0.2396 mL 1.1982 mL 2.3964 mL 5.9910 mL
15 mM 0.1598 mL 0.7988 mL 1.5976 mL 3.9940 mL
20 mM 0.1198 mL 0.5991 mL 1.1982 mL 2.9955 mL
25 mM 0.0959 mL 0.4793 mL 0.9586 mL 2.3964 mL
30 mM 0.0799 mL 0.3994 mL 0.7988 mL 1.9970 mL
40 mM 0.0599 mL 0.2996 mL 0.5991 mL 1.4978 mL
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Help & FAQs
  • 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:

AR4206261798310-55-0AR 420626AR-420626Free Fatty Acid ReceptorHistone MethyltransferaseHDACmTORCaMKp38 MAPKEpigenetic Reader DomainGLUTnAChRTNF ReceptorFFARHistone deacetylasesMammalian target of RapamycinCalmodulin-dependent protein kinasesCalmodulin-dependent kinasesGlucose transporter Nicotinic acetylcholine receptorsTumor Necrosis Factor ReceptorTNFRInhibitorinhibitorinhibit

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