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质量水平
检测方案
≥98% (HPLC)
形式
lyophilized powder
颜色
white
溶解性
DMSO: ≥30 mg/mL
储存温度
2-8°C
SMILES字符串
CCOC(=O)C1Cc2ccccc2CN1C(=O)c3ccc(SC)s3
InChI
1S/C18H19NO3S2/c1-3-22-18(21)14-10-12-6-4-5-7-13(12)11-19(14)17(20)15-8-9-16(23-2)24-15/h4-9,14H,3,10-11H2,1-2H3
InChI key
UIEBLUZPSFAFOC-UHFFFAOYSA-N
应用
SR8278可用作rev-erbα拮抗剂，研究胰高血糖素分泌对小鼠胰岛α细胞和β细胞的调节作用。
SR8278已被用作核受体亚家族1D组成员1（NR1D1）拮抗剂，以研究其对饥饿诱导的巨噬细胞的作用。
生化/生理作用
SR8278是核血红素受体REV-ERB拮抗剂。REV-ERBα通过抑制靶基因活性在调节昼夜节律中起关键作用。另外，研究表明，REV-ERBα可调节脂质和葡萄糖代谢等代谢过程。 SR8278可阻断合成激动剂GSK4112增强REV-ERBα依赖性抑制的能力、刺激参与糖异生的REV-ERBα靶基因的表达。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
NR1D1 ameliorates Mycobacterium tuberculosis clearance through regulation of autophagy
Chandra V, et al.
Autophagy, 11(11), 1987-1997 (2015)
Dapeng Yu et al.
International immunopharmacology, 73, 312-320 (2019-05-28)
Progressive lung injury and pulmonary inflammation can be induced by an intraperitoneal injection of lipopolysaccharide (LPS). Interleukin-1β (IL-1β) is a key pro-inflammatory cytokine that can further exaggerate inflammation, which is cleaved and activated by the NALP3 inflammasome. Although the nuclear
Elaine Vieira et al.
Endocrinology, 153(2), 592-601 (2011-12-15)
Disturbances of circadian rhythms have been associated with obesity and type 2 diabetes. The nuclear receptor Rev-erbα was suggested to link circadian rhythms and metabolism in peripheral tissues. The aim of the present study was to dissect the role of
Ryan D Welch et al.
Scientific reports, 7(1), 17142-17142 (2017-12-08)
Duchenne muscular dystrophy (DMD) is a debilitating X-linked disorder that is fatal. DMD patients lack the expression of the structural protein dystrophin caused by mutations within the DMD gene. The absence of functional dystrophin protein results in excessive damage from
Yihao Tian et al.
International journal of molecular medicine, 47(2), 633-642 (2021-01-09)
Melatonin, secreted in a typical diurnal rhythm pattern, has been reported to prevent osteoporosis; however, its role in osteoclastogenesis remains unclear. In the present study, the ability of melatonin to inhibit receptor activator of nuclear factor‑κB ligand (RANKL)‑induced osteoclastogenesis and
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