| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 500mg |
| Targets |
TUG-499 targets the free fatty acid receptor 1 (FFAR1/GPR40), a G protein-coupled receptor that is activated by medium- and long-chain free fatty acids. FFAR1 is predominantly expressed in pancreatic beta-cells and enteroendocrine cells. Activation of FFAR1 by agonists like TUG-499 enhances glucose-stimulated insulin secretion (GSIS) from pancreatic beta-cells, providing a mechanism for improving glycemic control in type 2 diabetes.
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|---|---|
| ln Vitro |
TUG-499 (Compound 7) has good Caco-2 permeability, no inhibitory effects on specific CYP enzymes, and strong chemical stability. Rat insulinoma cell line INS-1E and recombinant human FFA1 receptor are both effectively inhibited by TUG-499 [1].
In vitro, TUG-499 demonstrates potent activity on recombinant human FFAR1 receptors. It has a pEC50 of 7.39, indicating high potency. It shows selectivity for FFAR1 over related receptors FFA2 and FFA3, as well as PPARγ. Its activity can be assessed in cell-based assays, such as those measuring calcium mobilization or insulin secretion in response to receptor activation. |
| ln Vivo |
In vivo, TUG-499 has been studied in preclinical models for its ability to improve glycemic control without causing hypoglycemia. Its effect on insulin secretion and blood glucose levels can be measured in animal models of type 2 diabetes.
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| Enzyme Assay |
The agonist activity of TUG-499 is assessed using cell-based functional assays, such as calcium flux assays or insulin secretion assays. Cells expressing FFAR1 are treated with the compound, and the resulting intracellular signaling (e.g., calcium mobilization) or functional response (e.g., insulin secretion) is measured. The pEC50 is calculated from the dose-response curve.
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| Cell Assay |
The cellular activity of TUG-499 is evaluated in cell lines expressing FFAR1, such as INS-1E rat insulinoma cells. Its effect on glucose-stimulated insulin secretion is measured by treating cells with the compound in the presence of varying glucose concentrations and quantifying the insulin released into the medium by ELISA.
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| Animal Protocol |
In animal studies, TUG-499 is typically administered orally to rodent models of type 2 diabetes. Its effect on blood glucose levels is measured in glucose tolerance tests. Its effect on insulin secretion can be assessed by measuring plasma insulin levels.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of TUG-499 are not detailed in the provided literature. As a small molecule, its absorption, distribution, metabolism, and excretion would need to be characterized for in vivo applications.
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| Toxicity/Toxicokinetics |
Toxicology data for TUG-499 is not provided. As a research compound, its safety profile has not been established.
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| References | |
| Additional Infomation |
Free fatty acid receptor 1 (FFA1) agonist; structure described in the first article.
TUG-499 (CAS: 1206629-08-4) is a selective FFAR1 agonist with a pEC50 of 7.39. It is a valuable research tool for studying the role of FFAR1 in glucose homeostasis and for developing potential treatments for type 2 diabetes. |
| Molecular Formula |
C16H11CL2NO2
|
|---|---|
| Molecular Weight |
320.170042276382
|
| Exact Mass |
319.016
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| CAS # |
1206629-08-4
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| PubChem CID |
54669771
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| Appearance |
White to off-white solid powder
|
| LogP |
4.6
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| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
5
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| Heavy Atom Count |
21
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| Complexity |
411
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1(CCC(O)=O)=CC=C(C#CC2C=C(Cl)N=C(Cl)C=2)C=C1
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| InChi Key |
GCWBKYDSSJIRNJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H11Cl2NO2/c17-14-9-13(10-15(18)19-14)6-5-11-1-3-12(4-2-11)7-8-16(20)21/h1-4,9-10H,7-8H2,(H,20,21)
|
| Chemical Name |
3-[4-[2-(2,6-dichloropyridin-4-yl)ethynyl]phenyl]propanoic acid
|
| 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 | 3.1233 mL | 15.6167 mL | 31.2334 mL | |
| 5 mM | 0.6247 mL | 3.1233 mL | 6.2467 mL | |
| 10 mM | 0.3123 mL | 1.5617 mL | 3.1233 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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