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| Targets |
GPR41 agonist-1 specifically targets the G-protein coupled receptor 41 (GPR41/FFAR3), which is primarily expressed in enteroendocrine cells (L-cells), adipocytes, sympathetic ganglia, and immune cells. GPR41 is activated by short-chain fatty acids (SCFAs) and plays a key role in regulating energy homeostasis, gut motility, inflammation, and insulin secretion. GPR41 agonist-1 is a potent GPR41 agonist, and it can be used for researching insulin-related disorders and metabolic diseases such as diabetes and obesity. Activation of GPR41 stimulates the release of peptide YY (PYY) and glucagon-like peptide-1 (GLP-1), hormones that regulate appetite and insulin secretion.
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| ln Vitro |
In vitro, GPR41 agonist-1 is a potent and selective agonist of GPR41. In cell-based assays using GPR41-expressing cells (e.g., HEK293 cells stably transfected with human GPR41), treatment with GPR41 agonist-1 (0.01-100 uM) induces a concentration-dependent increase in intracellular calcium mobilization, as measured by fluorescence-based calcium assays (e.g., Fluo-4 AM). The compound also activates GPR41-mediated signaling pathways, including Gi/o protein coupling, leading to inhibition of adenylate cyclase and reduction of intracellular cAMP levels. It stimulates the secretion of GLP-1 and PYY from enteroendocrine cell lines. The compound is useful for studying the role of GPR41 in metabolic regulation.
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| ln Vivo |
In vivo, GPR41 agonist-1 has potential for use in studying metabolic diseases such as diabetes and obesity. By activating GPR41, the compound can stimulate the release of GLP-1 and PYY from intestinal L-cells, leading to improved glucose homeostasis, reduced food intake, and increased satiety. GPR41 activation also influences energy expenditure and adiposity. Preclinical studies with GPR41 agonists have shown that they can improve glucose tolerance and insulin sensitivity in mouse models of diet-induced obesity. GPR41 agonist-1 is a valuable tool for investigating the therapeutic potential of GPR41 activation for metabolic and insulin-related disorders.
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| Enzyme Assay |
For non-cell-based binding assays, a standard protocol uses a radioligand binding assay or a GTPgammaS binding assay to measure GPR41 activation. For the GTPgammaS binding assay, membranes prepared from GPR41-expressing HEK293 cells (50 ug protein per well) are incubated with varying concentrations of GPR41 agonist-1 (0.1-10,000 nM) in assay buffer (20 mM HEPES, pH 7.4, 100 mM NaCl, 10 uM GDP, 5 mM MgCl2) containing 0.1 nM [35S]GTPgammaS. After incubation for 60 minutes at 25degC, the reaction is terminated by rapid filtration through GF/B filters, and bound radioactivity is measured by scintillation counting. The EC50 for GPR41 activation is calculated. For calcium flux assays, cells expressing GPR41 and the promiscuous G protein Galpha16 are loaded with Fluo-4 AM, and fluorescence is measured on a plate reader; the EC50 is calculated from the concentration-response curve.
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| Cell Assay |
For in vitro cell-based assays, HEK293 cells stably expressing human GPR41 are seeded in black-walled 96-well plates at 4 × 10^4 cells/well. After 24 hours, cells are loaded with the calcium-sensitive fluorescent dye Fluo-4 AM (2-5 uM) in assay buffer (HBSS with 20 mM HEPES, pH 7.4, 0.1% BSA, 2.5 mM probenecid) for 60 minutes at 37degC. After washing to remove excess dye, varying concentrations of GPR41 agonist-1 (0.1-10,000 nM) are added, and the fluorescence signal (Ex 485 nm, Em 525 nm) is measured in real-time using a fluorescence plate reader. The EC50 for calcium mobilization is calculated. For GLP-1 secretion assays, enteroendocrine cell lines (e.g., NCI-H716 or GLUTag cells) are plated in 24-well plates. Cells are treated with GPR41 agonist-1 (0.1-100 uM) in low-glucose medium for 2-4 hours. Supernatants are collected, and GLP-1 concentration is measured by ELISA. For cAMP assays, cells are treated with the compound in the presence of forskolin (10 uM), and intracellular cAMP levels are measured by HTRF or competitive immunoassay.
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| Animal Protocol |
For in vivo animal studies, a mouse model of diet-induced obesity (DIO) or diabetes (e.g., db/db mice) is used. Male C57BL/6J mice fed a high-fat diet (60% kcal from fat) for 12-16 weeks are used as the DIO model. GPR41 agonist-1 is administered orally by gavage at doses of 10-50 mg/kg once daily for 4-6 weeks. Control animals receive vehicle (10% DMSO/90% corn oil or 0.5% methylcellulose). An oral glucose tolerance test (OGTT) is performed 30 minutes after compound administration on day 14 or 28: blood glucose is measured at 0, 15, 30, 60, 90, and 120 minutes after oral glucose challenge (2 g/kg). Blood is also collected for measurement of plasma insulin, GLP-1, and PYY levels by ELISA. Food intake and body weight are monitored daily. At study endpoint, visceral adipose tissue is weighed, and plasma lipid profiles (triglycerides, cholesterol) are analyzed.
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| ADME/Pharmacokinetics |
GPR41 agonist-1 is a small molecule with a molecular weight of 417.46 g/mol and a cLogP of approximately 3.0-4.0, indicating moderate lipophilicity and potential for oral bioavailability. The compound is soluble in DMSO (8 mg/mL, 19.16 mM). Pharmacokinetic data is not publicly available. Based on its chemical properties, it is expected to have moderate oral bioavailability (30-60%) and a half-life of 2-4 hours in rodents, supporting once- or twice-daily dosing for efficacy studies. The compound likely undergoes hepatic metabolism via CYP450 enzymes. Its volume of distribution is expected to be moderate, with distribution to multiple tissues, including the gut, where GPR41 receptors are located.
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| Toxicity/Toxicokinetics |
Formal toxicology data for GPR41 agonist-1 is not publicly available, as it is a preclinical research compound. GPR41 activation is associated with the beneficial metabolic effects of short-chain fatty acids, and agonist treatment is expected to be well tolerated in short-term studies. In cell viability assays, the compound does not exhibit significant cytotoxicity at concentrations up to 100 uM. In animal studies, GPR41 agonist-1 is likely well tolerated at doses up to 50 mg/kg (oral), although no specific toxicity data has been reported. Potential class-related adverse effects of GPR41 agonists may include gastrointestinal disturbances (due to increased motility and hormone secretion), but these have not been characterized for this specific compound. It is not a clinical drug.
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| Additional Infomation |
GPR41 agonist-1 is a research compound and is not approved for clinical use. GPR41 (FFAR3) is a receptor for short-chain fatty acids (SCFAs) that are produced by gut microbiota. Activation of GPR41 by SCFAs has been shown to improve metabolic health, including protection against diet-induced obesity, improved glucose homeostasis, and reduced inflammation. GPR41 agonist-1 is a small-molecule tool compound that allows researchers to pharmacologically activate GPR41 without the confounding effects of SCFAs on other receptors (e.g., GPR43/FFAR2). It is useful for studying the role of GPR41 in energy metabolism, insulin secretion, and gut-brain signaling. This product is for research use only.
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| Molecular Formula |
C24H23N3O4
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|---|---|
| Molecular Weight |
417.46
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| Exact Mass |
417.168
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| CAS # |
506417-09-0
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| PubChem CID |
3142532
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.6
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
31
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| Complexity |
825
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC=CC=C1NC(=O)C2=C(NC3=C(C2C4=CC(=CC=C4)[N+](=O)[O-])C(=O)CCC3)C
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| InChi Key |
UWQXWOJVNASZLI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H23N3O4/c1-14-7-3-4-10-18(14)26-24(29)21-15(2)25-19-11-6-12-20(28)23(19)22(21)16-8-5-9-17(13-16)27(30)31/h3-5,7-10,13,22,25H,6,11-12H2,1-2H3,(H,26,29)
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| Chemical Name |
2-methyl-N-(2-methylphenyl)-4-(3-nitrophenyl)-5-oxo-4,6,7,8-tetrahydro-1H-quinoline-3-carboxamide
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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 : ~10 mg/mL (~23.95 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3954 mL | 11.9772 mL | 23.9544 mL | |
| 5 mM | 0.4791 mL | 2.3954 mL | 4.7909 mL | |
| 10 mM | 0.2395 mL | 1.1977 mL | 2.3954 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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