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HTS01037

Catalog No. T15506 CAS 682741-29-3

HTS01037 is an inhibitor of fatty acid-binding. HTS01037 is a competitive antagonist of protein-protein interactions mediated by AFABP/aP2 (Ki: 0.67 μM).

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HTS01037, CAS 682741-29-3

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2 mg	5 days	$ 83.00

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Biological Description

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Description	HTS01037 is an inhibitor of fatty acid-binding. HTS01037 is a competitive antagonist of protein-protein interactions mediated by AFABP/aP2 (Ki: 0.67 μM).
Targets&IC50	AFABP/aP2:0.67 μM
In vitro	HTS01037 inhibits lipolysis in 3T3-L1 adipocytes and decreases LPS-stimulated inflammation in cultured macrophages. HTS01037 functions as a high affinity ligand of AFABP/aP2 (apparent Ki: 0.67 μM). HTS01037 is somewhat selective for AFABP/aP2, but at higher concentrations is a pan-specific FABP inhibitor. Treatment of microglial cells with HTS01037 enhances expression of Ucp2 and arginase in the presence or absence of palmitic acid. 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]. Cells exposed to HTS01037 shows attenuated expression of inducible nitric oxide synthase (iNOS) compared to palmitic acid alone indicating reduced NFκB signaling[2]. Treatment of macrophages with HTS01037 causes a marked decrease in both basal and fatty acid-stimulated LTC4 secretion but no change in 5-HETE production or 5-lipoxygenase expression[3].

Molecular Weight	337.37
Formula	C14H11NO5S2
CAS No.	682741-29-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 150 mg/mL (444.62 mM)

References and Literature

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.

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Keywords

HTS01037 682741-29-3 Others HTS-01037 HTS 01037 inhibitor inhibit

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