| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| Targets |
Gq-coupled free fatty acid receptor 1 (GPR40/FFAR1)
This compound targets the GPR40/FFAR1 receptor, which is a G-protein coupled receptor for free fatty acids. It acts as both an agonist and an allosteric modulator, meaning it binds to a site distinct from the orthosteric (fatty acid) binding site and enhances the receptor's response to its natural ligands or directly activates it. This unique mechanism allows for fine-tuning of receptor activity. |
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| ln Vitro |
In vitro, GPR40/FFAR1 modulator 1 is characterized by its ability to activate GPR40/FFAR1. Its activity is confirmed in cell-based functional assays, where it stimulates Gq-mediated signaling pathways, leading to an increase in intracellular calcium and activation of downstream effectors. This makes it a useful tool for studying the biology of this receptor.
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| ln Vivo |
In vivo, GPR40/FFAR1 modulator 1 is used to explore the therapeutic potential of GPR40-targeted agents in type 2 diabetes and metabolic disease models. By activating GPR40 in pancreatic β-cells, it can enhance glucose-stimulated insulin secretion (GSIS), making it a potential target for antidiabetic drugs. It is also used to study β-cell function, insulinotropic pathways, and lipid–hormone cross-talk.
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| Enzyme Assay |
The in vitro receptor binding assay for GPR40/FFAR1 modulator 1 involves measuring its affinity for the receptor. Membranes from cells expressing GPR40/FFAR1 are incubated with a radiolabeled ligand, such as [3H]-GW9508, in the presence of varying concentrations of the compound. The amount of radioligand displaced is measured to determine the binding affinity (Ki).
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| Cell Assay |
In vitro cell-based functional assays for GPR40/FFAR1 modulator 1 utilize cells expressing the receptor, often coupled to a calcium-sensitive fluorescent dye. Upon compound addition, the increase in intracellular calcium is measured. The EC50 for receptor activation is calculated from the concentration-response curve. The compound's allosteric nature can be studied by measuring its effect on the potency of a known agonist like linoleic acid.
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| Animal Protocol |
In vivo animal experiments for GPR40/FFAR1 modulator 1 are performed in rodent models of type 2 diabetes, such as the db/db mouse or the high-fat diet-fed mouse. The compound is administered orally, and its effect on blood glucose levels is measured in an oral glucose tolerance test (OGTT). Insulin levels are also measured to confirm that the glucose-lowering effect is mediated by increased insulin secretion.
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| ADME/Pharmacokinetics |
GPR40/FFAR1 modulator 1 has a molecular weight of 389.41 g/mol. It is typically stored as a powder at -20°C. It is soluble in DMSO, and stock solutions are prepared for in vitro and in vivo studies. Its formulation for in vivo studies often involves a vehicle like 10% DMSO, 40% PEG300, 5% Tween 80, and 45% saline.
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| Toxicity/Toxicokinetics |
Toxicological data for GPR40/FFAR1 modulator 1 are limited, as it is a research compound. It is not intended for human use. Comprehensive toxicity studies have not been reported. Standard safety precautions for handling chemical reagents should be followed. Its safety profile would be a key consideration if it were to be developed further.
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| References | |
| Additional Infomation |
GPR40/FFAR1 modulator 1 is a research compound with no clinical approval. It is a valuable tool for studying GPR40/FFAR1 pharmacology, biased signaling, and receptor cooperativity. It is used in drug discovery programs to explore the therapeutic potential of targeting this receptor for the treatment of type 2 diabetes and other metabolic diseases.
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| Molecular Formula |
C21H19N5O3
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|---|---|
| Molecular Weight |
389.407263994217
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| Exact Mass |
389.15
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| Elemental Analysis |
C, 64.77; H, 4.92; N, 17.98; O, 12.33
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| CAS # |
874755-26-7
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| PubChem CID |
8852666
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
3.3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
615
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC=CC=C1NC2=NC(=NC(=N2)N)COC3=CC4=C(C=C3)C(=CC(=O)O4)C
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| InChi Key |
WCRLDDWRDAIHGO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H19N5O3/c1-12-5-3-4-6-16(12)23-21-25-18(24-20(22)26-21)11-28-14-7-8-15-13(2)9-19(27)29-17(15)10-14/h3-10H,11H2,1-2H3,(H3,22,23,24,25,26)
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| Chemical Name |
7-[[4-amino-6-(2-methylanilino)-1,3,5-triazin-2-yl]methoxy]-4-methylchromen-2-one
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| Synonyms |
WUN55267; WUN-55267; GPR40/FFAR1 modulator 1; WUN 55267
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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: ~31.3 mg/mL (~80.3 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.34 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 20.8 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5680 mL | 12.8399 mL | 25.6799 mL | |
| 5 mM | 0.5136 mL | 2.5680 mL | 5.1360 mL | |
| 10 mM | 0.2568 mL | 1.2840 mL | 2.5680 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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