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| Targets |
GLP-1R agonist 3 targets the glucagon-like peptide-1 receptor (GLP-1R), a G protein-coupled receptor (GPCR) that plays a critical role in glucose homeostasis and insulin secretion. By binding to GLP-1R, this agonist enhances insulin release in response to meals, reduces glucagon secretion, and slows gastric emptying, ultimately helping to lower blood glucose levels. The compound is being studied for its potential in managing diabetes and obesity.
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| ln Vitro |
GLP-1R agonist 3 is a potent agonist of GLP-1R with demonstrated research potential in diabetes. As an imidazole derivative, it activates the GLP-1 receptor, triggering downstream signaling pathways that enhance glucose-dependent insulin secretion. The compound's activity is being studied for its effects on insulin secretion, glucose homeostasis, and metabolic regulation. Research is focused on optimizing its efficacy, safety, and long-term benefits as part of metabolic disease management.
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| ln Vivo |
In vivo activity data for GLP-1R agonist 3 are not extensively detailed, but the compound is being studied for its potential in diabetes and metabolic disorders. GLP-1R agonists are known to enhance insulin release, reduce glucagon secretion, slow gastric emptying, and lower blood glucose levels in vivo. The compound is expected to exhibit similar in vivo effects to other GLP-1R agonists. Research is focused on developing novel therapeutic strategies for diabetes and obesity management.
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| Enzyme Assay |
The in vitro receptor binding assay for GLP-1R agonist 3 typically involves measuring its affinity for the GLP-1 receptor using radioligand binding or functional assays. Membrane preparations from cells expressing GLP-1R are incubated with varying concentrations of the compound (typically 0.001-100 μM) and a labeled ligand. The binding affinity is determined by competition binding analysis. Functional assays measure cAMP production in response to receptor activation using ELISA or HTRF-based methods. The compound is dissolved in DMSO and diluted in assay buffer.
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| Cell Assay |
In vitro cellular assays for GLP-1R agonist 3 typically involve treating cells expressing the GLP-1 receptor (such as INS-1 cells or HEK-293 cells expressing GLP-1R) with the compound at concentrations ranging from 0.001 to 10 μM. cAMP production is measured using ELISA or HTRF-based assays to assess receptor activation. Insulin secretion is measured in insulinoma cell lines. The compound is dissolved in DMSO as a stock solution and diluted in cell culture medium, with DMSO-only treated cells serving as controls.
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| Animal Protocol |
In vivo animal studies for GLP-1R agonist 3 would typically involve administration to mice or rats via oral gavage or intraperitoneal injection at doses determined from preliminary studies. Diabetes models (such as diet-induced obesity or streptozotocin-induced diabetes) are used to evaluate glucose-lowering efficacy. Blood glucose levels are measured at various time points. Glucose tolerance tests are performed to assess the compound's effects on glucose homeostasis. The compound's pharmacokinetics and pharmacodynamics are evaluated in these models.
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| ADME/Pharmacokinetics |
GLP-1R agonist 3 has a molecular weight of 553.58 g/mol and formula C31H28FN5O4. It is soluble in DMSO (80 mg/mL, 144.51 mM). Recommended storage is powder at -20°C for 3 years and in solvent at -80°C for 1 year. The compound has a purity of 97.19%. Detailed PK parameters such as half-life, Cmax, AUC, and bioavailability would require experimental determination. As a small-molecule GLP-1R agonist, it may have oral bioavailability.
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| Toxicity/Toxicokinetics |
Toxicity data for GLP-1R agonist 3 are not extensively reported. The compound is intended for research use only and is not approved for human therapeutic applications. Standard preclinical toxicity assessments would include acute toxicity studies in rodents, repeated-dose toxicity studies, and assessment of off-target effects. As a GLP-1R agonist, the compound may have effects on gastrointestinal motility and other physiological processes, which could contribute to potential side effects. Appropriate safety precautions should be taken when handling.
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| Additional Infomation |
GLP-1R agonist 3 (CAS 2428640-18-8) is a potent imidazole derivative and GLP-1R agonist with a molecular weight of 553.58 g/mol and formula C31H28FN5O4. It enhances insulin release, reduces glucagon secretion, and slows gastric emptying, helping to lower blood glucose levels. The compound is being studied for its potential in diabetes and metabolic disorders. Research is focused on optimizing its efficacy, safety, and long-term benefits as part of metabolic disease management. The compound is not approved for clinical use.
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| CAS # |
2428640-18-8
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| PubChem CID |
150440053
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
41
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| Complexity |
1000
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| Defined Atom Stereocenter Count |
1
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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 : ~125 mg/mL (~225.80 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.) |
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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