產(chǎn)品目錄

規(guī)格	5mg 10mg 25mg 50mg 100mg
CAS	682741-29-3
別名	N/A
化學(xué)名	N/A
分子式	C14H11NO5S2
分子量	337.37
溶解度	DMSO : ≥ 150 mg/mL (444.62 mM);H2O : < 0.1 mg/mL (insoluble)
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

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.

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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