G0673
GSK4112
≥98% (HPLC)
别名:
1,1-二甲基乙基 N-[（4-氯苯基）甲基]-N-[（5-硝基-2-噻吩基）甲基])甘氨酸酯, SR6452
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关于此项目
经验公式（希尔记法）:
C18H21ClN2O4S
化学文摘社编号:
分子量:
396.89
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
off-white to tan
溶解性
DMSO: >20 mg/mL
创始人
GlaxoSmithKline
储存温度
2-8°C
SMILES字符串
CC(C)(C)OC(=O)CN(Cc1ccc(Cl)cc1)Cc2ccc(s2)[N+]([O-])=O
InChI
1S/C18H21ClN2O4S/c1-18(2,3)25-17(22)12-20(10-13-4-6-14(19)7-5-13)11-15-8-9-16(26-15)21(23)24/h4-9H,10-12H2,1-3H3
InChI key
WYSLOKHVFKLWOU-UHFFFAOYSA-N
相关类别
生化/生理作用
GSK4112是rev-erbα，（孤儿核受体NR1D1）激动剂，是第一种能够以相位依赖的方式重置生物钟的药物。Rev-erbα通过借助核受体共阻遏物复合物（NCoR）和HDAC3抑制靶基因活性来影响生物钟的精密度。GSK4112与血红素（rev-erb′s天然配体）竞争，并增强共阻遏物复合物的募集，从而抑制转录，这表明通过Rev-erb进行药理调节可能为治疗代谢性疾病，尤其是由rev-erba调节的脂肪形成紊乱提供新途径。
GSK4112是reverb（REV-ERBα，孤儿核受体NR1D1）激动剂；重置生物钟。
特点和优势
该化合物是基因调控研究推荐产品。点击此处 ，查看更多基因调控精选产品。想要了解有关生物活性小分子在其他研究领域应用的更多信息，请访问 sigma.com/discover-bsm。
该化合物由 GlaxoSmithKline开发。想浏览其他制药公司开发的化合物和已批准药物/候选药物目录， 请单击此处。
警示用语：
Danger
危险声明
危险分类
Eye Dam. 1 - Resp. Sens. 1
储存分类代码
11 - Combustible Solids
WGK
WGK 1
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Norimitsu Morioka et al.
Brain, behavior, and immunity, 78, 116-130 (2019-01-27)
The orphan nuclear receptors REV-ERBα and REV-ERBβ (REV-ERBs) are crucial in the regulation of inflammatory-related gene transcription in astroglioma cells, but their role in nociceptive transduction has yet to be elaborated. Spinal dorsal horn astrocytes contribute to the maintenance of
Na-Lee Ka et al.
Molecular and cellular endocrinology, 454, 87-92 (2017-06-11)
Cancer cells exhibit an elevated intracellular level of reactive oxygen species (ROS) because of their accelerated metabolism, mitochondrial dysfunction, and antioxidant deficit. The oxidative stress in cancer cells may provide clinical benefits, which can be associated with a better response
Kayoko Ishimaru et al.
International journal of molecular sciences, 20(24) (2019-12-19)
The cell-autonomous circadian clock regulates IgE- and IL-33-mediated mast cell activation, both of which are key events in the development of allergic diseases. Accordingly, clock modifiers could be used to treat allergic diseases, as well as many other circadian-related diseases
Dong-Kai Guo et al.
Acta pharmacologica Sinica, 40(1), 26-34 (2018-06-29)
REV-ERBα, the NR1D1 (nuclear receptor subfamily 1, group D, member 1) gene product, is a dominant transcriptional silencer that represses the expression of genes involved in numerous physiological functions, including circadian rhythm, inflammation, and metabolism, and plays a crucial role
Rev-erbα Inhibits Proliferation and Promotes Apoptosis of Preadipocytes through the Agonist GSK4112.
Guiyan Chu et al.
International journal of molecular sciences, 20(18) (2019-09-25)
Proliferation and apoptosis are important physiological processes of preadipocytes. Rev-erbα is a circadian clock gene, and its activity contributes to several physiological processes in various cells. Previous studies demonstrated that Rev-erbα promotes preadipocyte differentiation, but a role of Rev-erbα on
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