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
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Quality Level
assay
≥98% (HPLC)
form
powder
color
off-white to tan
solubility
DMSO: >20 mg/mL
originator
GlaxoSmithKline
storage temp.
2-8°C
SMILES string
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
Biochem/physiol Actions
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。
Features and Benefits
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。
signalword
Danger
hcodes
Hazard Classifications
Eye Dam. 1 - Resp. Sens. 1
存储类别
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
商品
We offer a variety of small molecule research tools, such as transcription factor modulators, inhibitors of chromatin modifying enzymes, and agonists/antagonists for target identification and validation in gene regulation research; a selection of these research tools is shown below.
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
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
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
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| G0673-5MG | 04061833024188 |
| G0673-25MG | 04061833024171 |