516567
PPARβ/δ拮抗剂，GSK3787
The PPARβ/δAntagonist II, PT-S58, also referenced under CAS 188591-46-0, controls the biological activity of PPARβ/δ. This small molecule/inhibitor is primarily used for Biochemicals applications.
别名:
PPARβ/δ拮抗剂，GSK3787, 4-氯-N-（2-（（5-三氟甲基）-2-吡啶基）磺酰基）乙基）苯甲酰胺，PPARβ拮抗剂I，PPARδ拮抗剂I
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关于此项目
经验公式（希尔记法）:
C15H12ClF3N2O3S
化学文摘社编号:
分子量:
392.78
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
产品名称
PPARβ/δ拮抗剂，GSK3787, The PPARβ/δAntagonist II, PT-S58, also referenced under CAS 188591-46-0, controls the biological activity of PPARβ/δ. This small molecule/inhibitor is primarily used for Biochemicals applications.
SMILES string
FC(F)(F)c1cnc(cc1)[S](=O)(=O)CCNC(=O)c2ccc(cc2)Cl
InChI
1S/C15H12ClF3N2O3S/c16-12-4-1-10(2-5-12)14(22)20-7-8-25(23,24)13-6-3-11(9-21-13)15(17,18)19/h1-6,9H,7-8H2,(H,20,22)
InChI key
JFUIMTGOQCQTPF-UHFFFAOYSA-N
assay
≥99% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
white
solubility
DMSO: 50 mg/mL, clear, colorless
shipped in
ambient
storage temp.
2-8°C
Quality Level
Disclaimer
毒性：标准处理（A）
General description
一种可渗透细胞且可口服的吡啶砜化合物，可作为选择性的高亲和力PPARβ（PPARδ）配体（PPAR配体移位试验中的IC50=针对人PPARβ的200 nM和针对PPARα或PPAR的γ>10 µM），并通过在Cys249处共价修饰PPARβ有效拮抗在体外培养物中（对CV-1细胞中2 nM GW501516诱导的报告基因转录IC50=126 nM）和在小鼠体内（通过10 mg/kg GSK3787结肠上皮中分别抑制10 mg/kg GW0742诱导的Adrp 和Angptl4 mRNA上调的82%和71%；p.o.）激动剂诱导的但不是基础的PPARβ转录活性。还显示GSK3787对PPARγ表现出较弱的激动活性（比基础水平增加1 µM GSK3787的1.2倍），并且从进一步刺激（在存在或不存在1 µM GSK3787的情况下，分别为基础0.3 M µGW1929的1.5 倍和3.5倍）中有效地阻断了更有效的激动剂GW1929（目录号370695）。
Other Notes
Palkar, P.S., et al. 2010.Mol.Pharmacol.78, 419.
Shearer, B,G., et al. 2010.J. Med. Chem.53, 1857.
Shearer, B,G., et al. 2010.J. Med. Chem.53, 1857.
Packaging
用惰性气体包装
Preparation Note
复溶后，等分并冷冻保存（-20°C）。贮备液在-20°C下可稳定保存至多6个月。
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Yanying Wang et al.
Nature communications, 12(1), 6314-6314 (2021-11-04)
Hepatocellular carcinoma (HCC) accounts for the majority of primary liver cancers and is characterized by high recurrence and heterogeneity, yet its mechanism is not well understood. Here we show that N1-methyladenosine methylation (m1A) in tRNA is remarkably elevated in hepatocellular
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