| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg | |||
| 50mg | |||
| Other Sizes |
| Targets |
GPR40 Activator 2 targets the GPR40 receptor (free fatty acid receptor 1, FFAR1), a G protein-coupled receptor expressed primarily in pancreatic beta-cells. GPR40 is activated by medium- and long-chain free fatty acids and couples to the Gq family of G proteins. Upon activation, GPR40 stimulates phospholipase C, leading to the production of inositol trisphosphate (IP3) and diacylglycerol (DAG), which mobilizes intracellular calcium and activates protein kinase C. This signaling cascade enhances glucose-stimulated insulin secretion from pancreatic beta-cells. By activating GPR40, GPR40 Activator 2 mimics the effects of fatty acids and promotes insulin secretion in a glucose-dependent manner. This mechanism makes GPR40 agonists promising therapeutic candidates for type 2 diabetes.
|
|---|---|
| ln Vitro |
GPR40 Activator 2 demonstrates potent in vitro activity as a GPR40 agonist. The compound is a highly effective activator of the GPR40 receptor. In cell-based assays using cells expressing recombinant GPR40, the compound activates the receptor and stimulates downstream signaling, including calcium mobilization and insulin secretion. The compound's potency and efficacy have been characterized in various in vitro systems. GPR40 Activator 2 is extracted from patent literature, where its activity and selectivity are described. The compound's mechanism of action involves binding to the GPR40 receptor and activating the Gq signaling pathway. Its activity is concentration-dependent, with potent effects observed at nanomolar to micromolar concentrations.
|
| ln Vivo |
In vivo, GPR40 Activator 2 has been evaluated in animal models of type 2 diabetes. As a GPR40 agonist, the compound would be expected to enhance glucose-stimulated insulin secretion and improve glucose tolerance. In preclinical studies, GPR40 agonists have demonstrated efficacy in reducing blood glucose levels and improving glucose tolerance in diabetic animal models. GPR40 Activator 2's in vivo activity has been described in patent literature. The compound's oral bioavailability and pharmacokinetic properties support its potential for development as a therapeutic agent for type 2 diabetes. Comprehensive in vivo efficacy data for GPR40 Activator 2 specifically are available in the patent literature.
|
| Enzyme Assay |
In vitro receptor binding assays for GPR40 Activator 2 involve measuring the compound's ability to bind to and activate the GPR40 receptor. Radioligand binding assays can be performed using membranes from cells expressing GPR40 and a radiolabeled GPR40 ligand. Membranes are incubated with the radiolabeled ligand and varying concentrations of the test compound, and bound radioactivity is measured. Alternatively, functional assays measure receptor activation using calcium mobilization assays or other second messenger assays. Cells expressing GPR40 are loaded with a calcium-sensitive fluorescent dye and treated with varying concentrations of the test compound. The increase in intracellular calcium is measured using a fluorescence plate reader. EC50 values are calculated from dose-response curves using non-linear regression analysis. Selectivity assays compare the compound's activity against related receptors.
|
| Cell Assay |
In vitro cellular assays for GPR40 Activator 2 are performed using cells expressing recombinant GPR40 or pancreatic beta-cell lines. Commonly used cell lines include CHO-K1 or HEK293 cells stably expressing human GPR40. Cells are treated with varying concentrations of the test compound, and receptor activation is measured by calcium mobilization using fluorescent calcium indicators such as Fluo-4 or Fura-2. In insulin secretion assays, pancreatic beta-cell lines (such as MIN6 or INS-1) or primary islets are treated with the compound in the presence of various glucose concentrations. Insulin secreted into the culture medium is measured by ELISA or radioimmunoassay. Cytotoxicity is assessed in parallel using standard viability assays to ensure that observed effects are not due to cell death. EC50 values are calculated from dose-response curves.
|
| Animal Protocol |
In vivo animal studies for GPR40 Activator 2 are conducted using rodent models of type 2 diabetes, such as db/db mice, ob/ob mice, or high-fat diet-induced obese mice. Animals are administered the compound via oral gavage at various doses and schedules. Blood glucose levels are measured at various time points after administration. Oral glucose tolerance tests (OGTT) are performed by administering a glucose load and measuring blood glucose levels over time. Insulin levels are measured in serum samples to assess the compound's effects on insulin secretion. Pharmacokinetic studies assess drug concentrations in plasma. Body weight and food intake are monitored as safety indicators. Efficacy is expressed as the reduction in blood glucose or improvement in glucose tolerance compared to vehicle-treated controls.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of GPR40 Activator 2 have been characterized in preclinical studies. The compound has a molecular formula of C28H29NO6S2 and a molecular weight of 539.66 g/mol. It is soluble in DMSO at 10 mM. The compound is orally bioavailable, making it suitable for convenient dosing regimens in research settings. Comprehensive pharmacokinetic parameters including half-life, volume of distribution, clearance, and oral bioavailability have been characterized in animal models. The compound's pharmacokinetic profile supports its use in preclinical studies of type 2 diabetes. Detailed pharmacokinetic data are available in the patent literature.
|
| Toxicity/Toxicokinetics |
GPR40 Activator 2 is intended for laboratory research use only and has not undergone comprehensive toxicology testing. As a GPR40 agonist, the compound would be expected to have effects on insulin secretion and glucose metabolism. Standard in vitro cytotoxicity assays in cell lines are typically performed alongside efficacy studies to rule out nonspecific toxicity. In vivo, animals are monitored for signs of toxicity including body weight changes, behavioral abnormalities, and clinical observations. Comprehensive toxicological characterization including genotoxicity, cardiotoxicity, and repeated-dose toxicity studies has not been reported in the public domain. The compound is not approved for human use and is strictly intended for research purposes.
|
| References |
WO 2012147516 A1, WO 2012046869A1 and WO 2011078371 A1.
|
| Additional Infomation |
GPR40 Activator 2 is a potent and highly effective activator (agonist) of the GPR40 receptor (free fatty acid receptor 1, FFAR1). It is extracted from patents WO 2012147516 A1, WO 2012046869 A1, and WO 2011078371 A1. The compound has a molecular formula of C28H29NO6S2 and a molecular weight of 539.66 g/mol. GPR40 Activator 2 activates GPR40, which is expressed primarily in pancreatic beta-cells and plays a critical role in glucose-stimulated insulin secretion. By activating GPR40, the compound promotes insulin secretion in a glucose-dependent manner, making it a potential therapeutic candidate for type 2 diabetes. GPR40 Activator 2 has not entered clinical trials and has not received regulatory approval for any indication. It is available from research chemical suppliers for non-clinical research purposes only. GPR40 Activator 2 is a valuable research tool for studying GPR40 biology and developing new therapies for type 2 diabetes.
|
| Molecular Formula |
C28H29NO6S2
|
|---|---|
| Molecular Weight |
539.662965536118
|
| Exact Mass |
539.144
|
| CAS # |
1312787-30-6
|
| PubChem CID |
67121842
|
| Appearance |
White to off-white solid powder
|
| LogP |
7.154
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
10
|
| Heavy Atom Count |
37
|
| Complexity |
925
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
AUYCNSCKGNAXFS-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C28H29NO6S2/c1-19-14-25(34-12-5-13-37(3,32)33)15-20(2)28(19)23-7-4-6-21(16-23)18-35-24-10-8-22(9-11-24)26-17-27(30)29-36(26)31/h4,6-11,14-17H,5,12-13,18H2,1-3H3,(H,29,30)
|
| Chemical Name |
5-[4-[[3-[2,6-dimethyl-4-(3-methylsulfonylpropoxy)phenyl]phenyl]methoxy]phenyl]-1-oxo-1,2-thiazol-3-one
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~231.63 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (3.85 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.85 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 20.8 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 | 1.8530 mL | 9.2651 mL | 18.5302 mL | |
| 5 mM | 0.3706 mL | 1.8530 mL | 3.7060 mL | |
| 10 mM | 0.1853 mL | 0.9265 mL | 1.8530 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
