Name | HTS01037 |
Synonyms | HTS01037 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 |
CAS | 682741-29-3 |
Molecular Formula | C14H11NO5S2 |
Molar Mass | 337.37 |
Solubility | DMSO: ≥150 mg/mL |
Appearance | solid |
Color | Yellow |
Storage Condition | RT |
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. |
In vitro study | HTS01037 functions as a high affinity ligand of AFABP/aP2 with an apparent K i 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. 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. 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.964 ml | 14.82 ml | 29.641 ml |
5 mM | 0.593 ml | 2.964 ml | 5.928 ml |
10 mM | 0.296 ml | 1.482 ml | 2.964 ml |
5 mM | 0.059 ml | 0.296 ml | 0.593 ml |
biological activity | HTS01037 is an inhibitor of fatty acid binding. It is also an antagonist of protein-protein interactions mediated by AFABP / aP2 with a Ki value of 0.67 μm. |
Target | IC50: 0.67 μm (AFABP/aP2) |