| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
AR-420626 targets the free fatty acid receptor 3 (FFAR3, GPR41), a G protein-coupled receptor. It acts as a selective and moderately potent positive allosteric modulator (PAM)-agonist. It has an IC50 of 117 nM. By activating FFAR3, it modulates various physiological processes, including inflammation and metabolism.
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|---|---|
| ln Vitro |
In vitro, AR-420626 is a selective agonist of FFAR3 with an IC50 of 117 nM. It inhibits nicotine and serotonin-induced changes in motility of isolated muscle strips from rat colon. It induces apoptosis via the TNF-α-induced extrinsic apoptotic pathway. These activities demonstrate its FFAR3 agonism and functional effects.
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| ln Vivo |
In vivo, AR-420626 suppresses serotonin-induced fecal output in rats. It provides protective effects against salsolionl (SALS), which were totally blocked by beta-hydroxy butyrate (BHB), a selective FFAR3 antagonist. It has potential for the treatment of neurogenic diarrheal disorders.
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| Enzyme Assay |
The in vitro receptor binding/functional assay for AR-420626 measures its ability to activate FFAR3. These assays typically use cells expressing FFAR3 and measure downstream signaling, such as calcium mobilization or inhibition of cAMP accumulation. The compound's potency (pEC50) is determined from these functional assays.
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| Cell Assay |
In vitro cellular assays for AR-420626 assess its effects on FFAR3-mediated signaling. Cells expressing FFAR3 are treated with AR-420626, and downstream signaling is measured. Its effects on intestinal smooth muscle motility are assessed using isolated muscle strips from rat colon. These assays demonstrate the compound's functional activity in a relevant cellular context.
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| Animal Protocol |
In vivo animal studies for AR-420626 have been conducted in rat models to assess its effects on gastrointestinal motility. Its ability to suppress serotonin-induced fecal output and its protective effects against SALS have been demonstrated. These studies support its potential for treating neurogenic diarrheal disorders.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for AR-420626 are not extensively detailed in the available literature. As a small molecule, its pharmacokinetic properties would be important for its in vivo efficacy. However, specific parameters such as half-life and bioavailability are not provided. It is intended for research use only.
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| Toxicity/Toxicokinetics |
Specific toxicity data for AR-420626 are not extensively detailed in the available literature. As a FFAR3 agonist, its toxicity profile is likely related to its mechanism of action. However, its potential for treating inflammatory and metabolic diseases suggests a manageable safety profile. It is intended for research purposes only.
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| References | |
| Additional Infomation |
AR-420626 is a selective allosteric agonist of FFAR3 (GPR41) with anti-inflammatory, anticancer, and antidiabetic activities. It has potential for the treatment of neurogenic diarrheal disorders. It is a research compound and is not approved for clinical use.
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| Molecular Formula |
C21H18CL2N2O3
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|---|---|
| Molecular Weight |
417.285223484039
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| Exact Mass |
416.069
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| Elemental Analysis |
C, 60.45; H, 4.35; Cl, 16.99; N, 6.71; O, 11.50
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| CAS # |
1798310-55-0
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| PubChem CID |
91885415
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
619.3±55.0 °C at 760 mmHg
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| Flash Point |
328.3±31.5 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.653
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| LogP |
3.71
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
28
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| Complexity |
733
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C=CC(=CC=1NC(C1=C(C)NC2CCCC(C=2C1C1=CC=CO1)=O)=O)Cl
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| InChi Key |
GGTYQECCGLBHGS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H18Cl2N2O3/c1-11-18(21(27)25-15-10-12(22)7-8-13(15)23)20(17-6-3-9-28-17)19-14(24-11)4-2-5-16(19)26/h3,6-10,20,24H,2,4-5H2,1H3,(H,25,27)
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| Chemical Name |
N-(2,5-dichlorophenyl)-4-(furan-2-yl)-2-methyl-5-oxo-4,6,7,8-tetrahydro-1H-quinoline-3-carboxamide
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| Synonyms |
AR 420626; AR-420626; AR420626
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~20 mg/mL (~47.9 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2 mg/mL (4.79 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2 mg/mL (4.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2396 mL | 1.1982 mL | 2.3964 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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