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Merck
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Key Documents

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G0673

Sigma-Aldrich

GSK4112

≥98% (HPLC)

Sinónimos:

1,1-Dimethylethyl N-[(4-chlorophenyl)methyl]-N-[(5-nitro-2-thienyl)methyl])glycinate, SR6452

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About This Item

Fórmula empírica (notación de Hill):
C18H21ClN2O4S
Número de CAS:
1216744-19-2
Peso molecular:
396.89
Número MDL:
MFCD12912412
Código UNSPSC:
12352200
ID de la sustancia en PubChem:
329799818
NACRES:
NA.77

Análisis

≥98% (HPLC)

formulario

powder

color

off-white to tan

solubilidad

DMSO: >20 mg/mL

emisor

GlaxoSmithKline

temp. de almacenamiento

2-8°C

cadena SMILES

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

Clave InChI

WYSLOKHVFKLWOU-UHFFFAOYSA-N

Acciones bioquímicas o fisiológicas

GSK4112 is a rev-erbα, (orphan nuclear receptor NR1D1) agonist, the first agent able to reset the circadian clock in a phase-dependent manner. Rev-erbα impacts the precision of the circadian clock by repressing target gene activities with the help of a nuclear receptor co-repressor complex (NCoR) and HDAC3. GSK4112 competes with heme (rev-erb′s natural ligand) and enhances co-repressor complex recruitment and thus, repression of transcription. suggests that pharmacological modulation through Rev-erb may provide new routes to treat metabolic diseases, especially disorders of adipogenesis regulated by rev-erba.

Características y beneficios

This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Pictogramas

Health hazardCorrosion
GHS08,GHS05

Palabra de señalización

Danger

Frases de peligro

H318,H334

Clasificaciones de peligro

Eye Dam. 1 - Resp. Sens. 1

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 1

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable

Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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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
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
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 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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