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HTS01037

CAS No. : 682741-29-3

MCE 站：HTS01037

产品活性：HTS01037是结合脂肪酸的抑制剂。它也是由AFABP / aP2介导的蛋白质-蛋白质相互作用的拮抗剂，K_i值为0.67 μM。

研究领域：Metabolic Enzyme/Protease

作用靶点：FABP

In Vitro: 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.

相关产品：Covalent Screening Library Plus  |  Bioactive Compound Library Plus  |  Metabolism/Protease Compound Library  |  Covalent Screening Library  |  BMS-309403

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