SML2374
HTS01037
≥98% (HPLC)
别名:
(E)-4-(5-(Methoxycarbonyl)-2,2′-bithiophen-4-ylamino)-4-oxobut-2-enoic acid, 4-[(3-Carboxy-1-oxo-2-propenyl)amino]-[2,2′-bithiophene]-5-carboxylic acid 5-methyl ester, 4-{[2-(Methoxycarbonyl)-5-(2-thienyl)-3-thienyl]amino}-4-oxo-2-butenoic acid, HTS 01037, HTS-01037
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关于此项目
经验公式（希尔记法）:
C14H11NO5S2
化学文摘社编号:
分子量:
337.37
UNSPSC Code:
12352200
MDL number:
NACRES:
NA.21
产品名称
HTS01037, ≥98% (HPLC)
SMILES string
[s]1c(cc(c1C(=O)OC)NC(=O)C=CC(=O)O)c2[s]ccc2
InChI
1S/C14H11NO5S2/c1-20-14(19)13-8(15-11(16)4-5-12(17)18)7-10(22-13)9-3-2-6-21-9/h2-7H,1H3,(H,15,16)(H,17,18)
InChI key
GJODSFZNKNHKML-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
−20°C
Biochem/physiol Actions
HTS01037 is a selective, high-affinity fatty acid-binding protein FABP4 (AFABP; aP2) antagonist (aP2 Ki = 0.67 μM; EFABP/HF/IFABP/LFABP Ki = 3.40/9.07/6.57/8.17 μM) that targets aP2 long-chain fatty acid-binding site. HTS01037 is shown to downregulate basal and fatty acid-stimulated LTC4 levels in primary murine peritoneal macrophages (0.2-20 μM), upregulate murine macrophage RAW 264.7 intracellular free fatty acids and uncoupling protein 2 (UCP2) mRNA levels (30 μM), as well as suppress PPARγ target genes expression in IL-4 polarized human primary macrophages (10-25 μM).
Selective, high-affinity fatty acid-binding protein FABP4 (AFABP; aP2) antagonist that blocks aP2-mediated responses in human and murine macrophages.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Kaylee A Steen et al.
Molecular and cellular biology, 37(2) (2016-11-01)
Obesity-linked metabolic disease is mechanistically associated with the accumulation of proinflammatory macrophages in adipose tissue, leading to increased reactive oxygen species (ROS) production and chronic low-grade inflammation. Previous work has demonstrated that deletion of the adipocyte fatty acid-binding protein (FABP4/aP2)
Yuta Okamura et al.
Pflugers Archiv : European journal of physiology, 469(9), 1177-1188 (2017-04-14)
Fatty acid-binding protein (FABP) 4 is an adipocytokine mainly expressed in adipocyte and macrophage. Blood FABP4 is related not only to metabolic disorders including insulin resistance and atherosclerosis but also increased blood pressure. We tested the hypothesis that FABP4 plays
Eric K Long et al.
Biochimica et biophysica acta, 1831(7), 1199-1207 (2013-04-16)
Obesity results in increased macrophage recruitment to adipose tissue that promotes a chronic low-grade inflammatory state linked to increased fatty acid efflux from adipocytes. Activated macrophages produce a variety of pro-inflammatory lipids such as leukotriene C4 (LTC4) and 5-, 12-
Kuok Teong Ong et al.
Journal of lipid research, 55(5), 808-815 (2014-03-13)
Adipose TG lipase (ATGL) catalyzes the rate-limiting step in TG hydrolysis in most tissues. We have shown that hepatic ATGL preferentially channels hydrolyzed FAs to β-oxidation and induces PPAR-α signaling. Previous studies have suggested that liver FA binding protein (L-FABP)
Cayla M Duffy et al.
Molecular and cellular neurosciences, 80, 52-57 (2017-02-20)
Hypothalamic inflammation contributes to metabolic dysregulation and the onset of obesity. Dietary saturated fats activate microglia via a nuclear factor-kappa B (NFκB) mediated pathway to release pro-inflammatory cytokines resulting in dysfunction or death of surrounding neurons. Fatty acid binding proteins
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