| Identification | Back Directory | [Name]
HTS 01037 | [CAS]
682741-29-3 | [Synonyms]
HTS 01037
HTS 01037
(HTS01037
4-{[2-(methoxycarbonyl)-5-(2-thinyl)-3-thienyl]amino}-4-oxo-2-butenoic acid
[2,2'-Bithiophene]-5-carboxylic acid, 4-[(3-carboxy-1-oxo-2-propen-1-yl)amino]-, 5-methyl ester | [Molecular Formula]
C14H11NO5S2 | [MOL File]
682741-29-3.mol | [Molecular Weight]
337.37 |
| Chemical Properties | Back Directory | [Boiling point ]
621.2±55.0 °C(Predicted) | [density ]
1.493±0.06 g/cm3(Predicted) | [storage temp. ]
RT | [solubility ]
Soluble in DMSO (up to 50 mg/ml) | [form ]
solid | [pka]
3.39±0.10(Predicted) | [color ]
Yellow | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months. |
| Hazard Information | Back Directory | [Description]
Adipocyte fatty acid binding protein (A-FABP/aP2) is a carrier protein expressed in both adipocytes and macrophages where it functions in intracellular fatty acid solubilization, trafficking, and metabolism. Molecular disruption of A-FABP/aP2 in mice results in improved insulin sensitivity and protection from atherosclerosis. HTS 01037 is a high-affinity ligand of adipocyte fatty acid binding protein (A-FABP/aP2) (Ki = 0.67 μM) that presumably competes with fatty acids for functional binding in the ligand-binding cavity of A-FABP/aP2. At a concentration of 10 μM, HTS 01037 antagonizes the protein-protein interaction of A-FABP/aP2 with hormone sensitive lipase in cultured C8PA lipocytes. HTS 01037 inhibits lipolysis in 3T3L1 adipocytes and reduces lipopolysaccharide-stimulated inflammation in bone marrow-derived macrophages, both effects of which are similar to the phenotype of A-FABP/aP2 knockout mice. | [Uses]
HTS 01037 is an inhibitor of fatty acid binding protein and a competitive antagonist of protein-protein interactions mediated by AFABP/aP2. | [Definition]
ChEBI: HTS 01037 is a ring assembly and a member of thiophenes. | [References]
1) Hertzel?et al. (2009),?Identification and characterization of a small molecule inhibitor of Fatty Acid binding proteins; J. Med. Chem,?52?6024
2) Long?et al. (2012),?Fatty acids induce leukotriene C4 synthesis in macrophages in a fatty acid binding protein-dependent manner;?Biochim. Biophys. Acta,?1831?1199
3) Xu?et al.?(2015),?Uncoupling lipid metabolism from inflammation through fatty acid binding protein-dependent expression of USP2; Mol. Cell. Biol.,?35?1055
4) Steen?et al. (2016),?FABP4/aP2 regulates macrophage redox signaling and inflammasome activation via control of UCP2; Mol. Cell. Biol.,?37 e00282
5) Boss?et al.?(2015),?FABP4 inhibition suppresses PPARgamma activity and VLDL-induced foam cell formation in IL-4-polarized human macrophages; Atherosclerosis,?240?424 |
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BOC Sciences
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https://www.bocsci.com |
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