| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
FSG-67 specifically targets glycerol-3-phosphate acyltransferase (GPAT), a key enzyme in the de novo synthesis of glycerolipids. GPAT catalyzes the acylation of glycerol-3-phosphate to form lysophosphatidic acid, the first committed step in the biosynthesis of triglycerides and phospholipids. By inhibiting GPAT, FSG-67 reduces the synthesis of these lipids. This inhibition leads to a cascade of metabolic changes, including decreased food intake and body weight, and an increase in energy utilization, such as fatty acid oxidation. FSG-67 also alters GSK3β and Wnt/β-catenin signaling.
|
|---|---|
| ln Vitro |
After overdosing on cardiovascular fat, FSG67 decreases GSK3β phosphorylation and signaling burst [1]. In mature cells, FSG67 increases oxidation in a dose-dependent manner, with an IC50 of 27.7 ± 4.4 μM [2].
In vitro, FSG-67 is a potent inhibitor of GPAT with an IC50 of 24 μM. It results in a dose-dependent increase in oxidative metabolism in mature adipocytes with an IC50 of 27.7 ± 4.4 μM. In primary hypothalamic neurons (PHN), FSG-67 increases fatty acid oxidation (FAOx), leading to an increase in ATP and inactivation of AMPK. It also reduces oxidative stress and indicators of ER stress in PHN. Additionally, FSG-67 reduces GSK3β phosphorylation and signaling after acetaminophen overdose. |
| ln Vivo |
In diet-induced obese (DIO) mice, FSG-67 demonstrated significant in vivo efficacy. It reduced food intake, decreased body weight and adiposity, enhanced energy utilization as fatty acid oxidation, reversed hepatic steatosis, and enhanced insulin sensitivity. The compound also caused decreased gene expression for orexigenic hypothalamic neuropeptides AgRP and NPY. It blunts liver regeneration after acetaminophen overdose by altering GSK3β and Wnt/β-catenin signaling.
|
| Enzyme Assay |
The primary non-cellular assay for FSG-67 involves measuring its inhibition of GPAT enzyme activity. In a typical assay, recombinant GPAT is incubated with its substrates (glycerol 3-phosphate and acyl-CoA) and varying concentrations of the inhibitor. The production of lysophosphatidic acid is measured, and the IC50 is calculated.
|
| Cell Assay |
In vitro cellular assays for FSG-67 often employ primary hypothalamic neurons (PHN) or mature adipocytes. Cells are treated with various concentrations of FSG-67, and fatty acid oxidation (FAOX) is measured. This leads to an increase in ATP and inactivation of AMPK. Markers of oxidative and ER stress are also assessed.
|
| Animal Protocol |
In vivo, FSG-67 has been studied in diet-induced obese (DIO) mouse models. Mice are administered FSG-67, and parameters such as food intake, body weight, adipose tissue mass, hepatic steatosis, and insulin sensitivity are monitored. The expression of orexigenic hypothalamic neuropeptides like AgRP and NPY is also measured.
|
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of FSG-67 are not extensively characterized. As a small molecule with a molecular weight of 327.44, it is soluble in DMSO and ethanol (>25 mg/mL). In vivo, it can be formulated as a clear solution in 5% DMSO, 40% PEG300, 5% Tween 80, and 50% ddH2O or as a homogeneous suspension in CMC-Na.
|
| Toxicity/Toxicokinetics |
FSG-67 has demonstrated no observable in vitro or in vivo toxicity in diet-induced obese mice. However, comprehensive toxicological data are limited. It is intended for research use only and not for human therapeutic use.
|
| References |
|
| Additional Infomation |
An anorexic drug that inhibits glycerol-3-phosphoacyltransferase; structure described in the first article.
FSG-67 is a research-grade compound for laboratory use only and is not approved for clinical use. Its primary application is in metabolic research, specifically for studying the role of GPAT in lipid metabolism, food intake regulation, and obesity. It is a valuable tool for investigating potential therapeutic targets for metabolic disorders. |
| Molecular Formula |
C16H25NO4S
|
|---|---|
| Molecular Weight |
327.44
|
| Exact Mass |
327.15
|
| CAS # |
1158383-34-6
|
| PubChem CID |
44139871
|
| Appearance |
Light yellow to yellow solid powder
|
| LogP |
4.9
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
11
|
| Heavy Atom Count |
22
|
| Complexity |
416
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1C=CC(C(O)=O)=C(NS(=O)(=O)CCCCCCCCC)C=1
|
| InChi Key |
WNFXEGWGYFRRJC-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C16H25NO4S/c1-2-3-4-5-6-7-10-13-22(20,21)17-15-12-9-8-11-14(15)16(18)19/h8-9,11-12,17H,2-7,10,13H2,1H3,(H,18,19)
|
| Chemical Name |
2-(nonylsulfonylamino)benzoic acid
|
| 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 : ~100 mg/mL (~305.40 mM)
|
|---|---|
| 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 | 3.0540 mL | 15.2700 mL | 30.5399 mL | |
| 5 mM | 0.6108 mL | 3.0540 mL | 6.1080 mL | |
| 10 mM | 0.3054 mL | 1.5270 mL | 3.0540 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
