HTS01037 |
| Katalog-Nr.GC31356 |
HTS01037 ist ein Inhibitor der FettsÄurebindung; und ein kompetitiver Antagonist von durch AFABP/aP2 vermittelten Protein-Protein-Wechselwirkungen mit einem Ki von 0,67 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 682741-29-3
Sample solution is provided at 25 µL, 10mM.
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HTS01037 is an inhibitor of fatty acid binding; and a competitive antagonist of protein-protein interactions mediated by AFABP/aP2 with a Ki of 0.67 μM.
HTS01037 functions as a high affinity ligand of AFABP/aP2 with an apparent Ki of 0.67 μM. HTS01037 is somewhat selective for AFABP/aP2, but at higher concentrations is a pan-specific FABP inhibitor. HTS01037 inhibits lipolysis in 3T3-L1 adipocytes and reduces LPS-stimulated inflammation in cultured macrophages. HTS01037 acts as an antagonist of the protein-protein interaction between AFABP/aP2 and hormone sensitive lipase but does not activate PPARγ in macrophage or CV-1 cells[1]. Treatment of microglial cells with HTS01037 increases expression of Ucp2 and arginase in the presence or absence of palmitic acid. Moreover, cells exposed to HTS01037 exhibits attenuated expression of inducible nitric oxide synthase (iNOS) compared to palmitic acid alone indicating reduced NFκB signaling[2]. Treatment of macrophages with HTS01037results in a marked decrease in both basal and fatty acid-stimulated LTC4 secretion but no change in 5-HETE production or 5-lipoxygenase expression[3].
[1]. Hertzel AV, et al. Identification and characterization of a small molecule inhibitor of Fatty Acid binding proteins. J Med Chem. 2009 Oct 8;52(19):6024-31. [2]. Duffy CM, et al. Identification of a fatty acid binding protein4-UCP2 axis regulating microglial mediated neuroinflammation. Mol Cell Neurosci. 2017 Apr;80:52-57. [3]. Long EK, et al. Fatty acids induce leukotriene C4 synthesis in macrophages in a fatty acid binding protein-dependent manner. Biochim Biophys Acta. 2013 Jul;1831(7):1199-207.
Kinase experiment: | To analyze the ligand (HTS01037) binding properties of the FABPs, the fluorescent ligand 1-anilinonapthalene 8-sulfonic acid (1,8-ANS) is utilized. 1,8 ANS is dissolved in absolute ethanol and diluted with 25 mM Tris-HCl (pH 7.4) to a final concentration of 5 μM (final EtOH concentration of 0.05%). Protein is titrated into 500 μL 1,8-ANS and the fluorescence enhancement is measured using a Perkin Elmer 650-10S fluorescence spectrophotometer with 4 nm excitation and emission slit widths. Quantitative analysis of ligand binding is evaluated using non-linear regression using PRISM software[1]. |
Cell experiment: | Cells are pretreated with HTS01037 or vehicle for 3 h and then challenged with or without palmitic acid for 1 h. Cells are then exposed to the ROS Deep Red Dye for 1 h in 5% CO2 at 37°C. Intracellular superoxide and hydroxyl radicals react with the deep red dye, producing a fluorescent signal which is measured using a spectrophotometer at 650Ex/675Em[2]. |
References: [1]. Hertzel AV, et al. Identification and characterization of a small molecule inhibitor of Fatty Acid binding proteins. J Med Chem. 2009 Oct 8;52(19):6024-31. | |
| Cas No. | 682741-29-3 | SDF | |
| Canonical SMILES | O=C(C1=C(NC(/C=C/C(O)=O)=O)C=C(C2=CC=CS2)S1)OC | ||
| Formula | C14H11NO5S2 | M.Wt | 337.37 |
| Löslichkeit | DMSO : ≥ 150 mg/mL (444.62 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.9641 mL | 14.8205 mL | 29.641 mL |
| 5 mM | 0.5928 mL | 2.9641 mL | 5.9282 mL |
| 10 mM | 0.2964 mL | 1.4821 mL | 2.9641 mL |
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- Purity: >99.50%
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