| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
TUG-424 targets the free fatty acid receptor 1 (FFA1/GPR40). By acting as an agonist at this receptor, it amplifies the glucose-sensing and insulin-secreting capacity of pancreatic β-cells. This mechanism is glucose-dependent, meaning that it only stimulates insulin secretion in the presence of elevated glucose levels, thereby reducing the risk of hypoglycemia. The compound shows high selectivity for FFA1 over other receptors.
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| ln Vitro |
TUG-424 was added at concentrations ranging from 100 nM to 10 µM, which had the biggest impact at 3 µM on glucose-stimulated insulin secretion at 100 nM. TUG-424's approximately two-fold stimulation of secretion in the presence of 12 mM glucose was similar to palmitate's stimulation of secretion in the same glucose concentration. At 2.8 mM glucose, TUG-424 [1] marginally but considerably lowers baseline insulin secretion.
In vitro studies have shown that TUG-424 significantly enhances glucose-stimulated insulin secretion in INS-1E cells, a rat pancreatic β-cell line. At a concentration of 100 nM, it produces a significant effect, with a maximal effect observed at 3 µM. This stimulation is comparable to that induced by palmitate, a natural FFA1 agonist. The compound also slightly reduces basal insulin secretion at low glucose concentrations, indicating a glucose-dependent mechanism of action. |
| ln Vivo |
In vivo, TUG-424 has been used to explore the role of FFA1 in metabolic diseases. In animal models, it is expected to improve glucose tolerance by enhancing insulin secretion in response to a glucose challenge. The compound's effects are mediated through its action on pancreatic β-cells, making it a valuable tool for studying the physiology and pathophysiology of glucose homeostasis.
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| Enzyme Assay |
In vitro enzyme or receptor binding (non-cell) assays for TUG-424 typically involve radioligand binding studies to determine its affinity for FFA1. Membranes from cells expressing human FFA1 are incubated with a radiolabeled agonist or antagonist. TUG-424 is added at various concentrations to compete with the radioligand, and the amount of bound radioactivity is measured to calculate the Ki or IC50. These assays confirm the compound's high affinity and selectivity for the receptor.
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| Cell Assay |
In vitro cell-based assays for TUG-424 are performed using INS-1E cells or primary pancreatic islets. Cells are cultured in media with varying glucose concentrations (e.g., 2.8 mM and 12 mM) and treated with TUG-424. Insulin secretion into the supernatant is measured using ELISA or radioimmunoassay. The compound's effect on intracellular calcium levels can also be measured using fluorescent dyes, as FFA1 activation leads to Ca²⁺ mobilization.
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| Animal Protocol |
In vivo animal experiments for TUG-424 are conducted using rodent models of diabetes and obesity. The compound is typically administered orally or intraperitoneally, followed by an oral glucose tolerance test (OGTT). Blood glucose and plasma insulin levels are measured at various time points to assess the compound's ability to enhance glucose-stimulated insulin secretion and improve glucose tolerance.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of TUG-424 have been studied to support its use as a research tool. The compound has a molecular weight of 264.32 and a formula of C₁₈H₁₆O₂. It is soluble in DMSO. As a small, lipophilic molecule, it is expected to have favorable oral bioavailability, though specific PK parameters like half-life and clearance are determined through standard LC-MS/MS analysis of plasma samples in animal studies.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for TUG-424 are typical of a research compound used in preclinical studies. At effective doses, it is generally well-tolerated. However, as an insulin secretagogue, there is a potential risk of hypoglycemia if used inappropriately. Its safety profile is being evaluated in the context of its development for metabolic diseases.
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| References |
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| Additional Infomation |
Other information: TUG-424 is a click chemistry reagent containing an alkyne group, which allows it to be used in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions. This feature makes it useful for labeling and studying FFA1 in biological systems. The compound is available as a research chemical for studying metabolic diseases.
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| Molecular Formula |
C18H16O2
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| Molecular Weight |
264.318445205688
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| Exact Mass |
264.115
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| CAS # |
1082058-99-8
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| PubChem CID |
25150014
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
448.1±38.0 °C at 760 mmHg
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| Flash Point |
205.9±21.4 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.617
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| LogP |
4.86
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
20
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| Complexity |
379
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
FODHWOBAQBTTFS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H16O2/c1-14-4-2-3-5-17(14)12-10-15-6-8-16(9-7-15)11-13-18(19)20/h2-9H,11,13H2,1H3,(H,19,20)
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| Chemical Name |
3-(4-(o-tolylethynyl)phenyl)propanoic acid
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| Synonyms |
TUG-424 TUG424 TUG 424.
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 3.7833 mL | 18.9165 mL | 37.8329 mL | |
| 5 mM | 0.7567 mL | 3.7833 mL | 7.5666 mL | |
| 10 mM | 0.3783 mL | 1.8916 mL | 3.7833 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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