CAS 101574-65-6|GSK 4716

Introduction:Basic information about CAS 101574-65-6|GSK 4716, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameGSK 4716
CAS Number101574-65-6Molecular Weight282.33700
Density1.12g/cm3Boiling Point/
Molecular FormulaC17H18N2O2Melting Point/
MSDSChineseUSAFlash Point/
Symbol
GHS07, GHS09
Signal WordWarning

Names

Name4-hydroxy-N-[(E)-(4-propan-2-ylphenyl)methylideneamino]benzamide
SynonymMore Synonyms

GSK 4716 BiologicalActivity

DescriptionGSK-4716 is a selective ERRβ/γ agonist.
Related CatalogSignaling Pathways >>Others >>Estrogen Receptor/ERRResearch Areas >>Cancer
Target

ERRβ/γ[1]

In VitroTreatment of differentiated C2C12 cells with the ERRβ/γ agonist (relative to vehicle) over a 2 to 4 h time period reveals a reproducible and robust increase in the immunoreactivity of the GRα-D isoform. It is observed that MAO-A mRNA expression is significantly increased by treatment with the ERRβ/γ agonist, GSK4716. Furthermore, it is observed that GSK4716 induces the expression of the mRNAs encoding peroxisome proliferator-activated receptor-γcoactivator 1α (PGC-1α) and PGC-1β (key regulator of many metabolic genes) identified as direct coactivators for the ERR family. GSK4716 induces the expression of PGC-1 and genes involved in fatty acid oxidation in concordance with the characterized role of ERRγ in cardiac metabolism[1]. Treatment of primary mouse myotubes with GSK4716, an ERRβ/γ agonist, results in a concerted increase in the expression levels of Ppargc1a, Ppargc1b, and the Esrr genes. Furthermore,Cpt1b, Atp5b, and Idh3, genes in key mitochondrial pathways, are also induced by GSK4716. Additionally, GSK4716 increases citrate synthase activity and cytochrome c protein levels[2].
Cell AssayProliferating mouse C2C12 myoblast are cultured and maintained in DMEM supplemented with 10% heat-inactivated serum supreme. Differentiation of myoblasts into post-mitotic, multi-nucleated myotubes are induced by mitogen withdrawal (DMEM supplemented with 2% horse serum) for 4 days. C2C12 myotubes are treated with either vehicle (DMSO) or ERRβ/γ agonist GSK4716 for 1 day and RNA collected and processed[1].
References

[1]. Wang SC, et al. An ERRbeta/gamma agonist modulates GRalpha expression, and glucocorticoid responsive gene expression in skeletal muscle cells. Mol Cell Endocrinol. 2010 Feb 5;315(1-2):146-52.

[2]. Rangwala SM, et al. Estrogen-related receptor gamma is a key regulator of muscle mitochondrial activity and oxidative capacity. J Biol Chem. 2010 Jul 16;285(29):22619-29.

Chemical & Physical Properties

Density1.12g/cm3
Molecular FormulaC17H18N2O2
Molecular Weight282.33700
Exact Mass282.13700
PSA61.69000
LogP3.67040
Index of Refraction1.576
InChIKeyIKPPIUNQWSRCOZ-WOJGMQOQSA-N
SMILESCC(C)c1ccc(C=NNC(=O)c2ccc(O)cc2)cc1
Storage condition2-8℃

Safety Information

Symbol
GHS07, GHS09
Signal WordWarning
Hazard StatementsH317-H410
Precautionary StatementsP273-P280-P501
RIDADRUN 3077 9 / PGIII

Synonyms

GSK 4716
2gpp
QCR-163
GSK-4716
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