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Merck
CN

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:
1216744-19-2
分子量:
396.89
NACRES:
NA.77
PubChem Substance ID:
329799818
UNSPSC Code:
12352200
MDL number:
MFCD12912412

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产品名称

GSK4112, ≥98% (HPLC)

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

SMILES string

CC(C)(C)OC(=O)CN(Cc1ccc(Cl)cc1)Cc2ccc(s2)[N+]([O-])=O

InChI key

WYSLOKHVFKLWOU-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

color

off-white to tan

solubility

DMSO: >20 mg/mL

originator

GlaxoSmithKline

storage temp.

2-8°C

Quality Level

100

相关类别

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。

pictograms

Health hazardCorrosion
GHS08,GHS05

signalword

Danger

hcodes

H318,H334

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

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000507071
0000507071
0000135090
0000135091
0000078259

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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
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
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
Dong Dong et al.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, 1020, 142-147 (2016-04-04)
There is a relationship between circadian rhythm and metabolic disorders. The active agent, SR8278, could competitively bind to and inhibit the nuclear receptor, Rev-erb (a major modulator of mammalian circadian clock system), to regulate the metabolism in organisms. However, we
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