
GSK-4716
CAS No. 101574-65-6
GSK-4716( —— )
Catalog No. M20159 CAS No. 101574-65-6
GSK4716 is an ERRβ/γ agonist (IC50 = 2 μM) that can activate the receptor with similar potency as the protein ligand.
Purity : >98% (HPLC)






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Biological Information
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Product NameGSK-4716
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NoteResearch use only, not for human use.
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Brief DescriptionGSK4716 is an ERRβ/γ agonist (IC50 = 2 μM) that can activate the receptor with similar potency as the protein ligand.
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DescriptionGSK4716 is an ERRβ/γ agonist (IC50 = 2 μM) that can activate the receptor with similar potency as the protein ligand.
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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. 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.
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In Vivo——
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Synonyms——
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PathwayEndocrinology/Hormones
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TargetEstrogen Receptor/ERR
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RecptorERRβ/γ
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Research Area——
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Indication——
Chemical Information
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CAS Number101574-65-6
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Formula Weight282.34
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Molecular FormulaC17H18N2O2
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Purity>98% (HPLC)
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SolubilityDMSO:100 mg/mL?(354.18 mM)
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SMILESCC(C)c1ccc(cc1)\C=N\NC(=O)c1ccc(O)cc1
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Chemical Name4-hydroxy-N-[(4-propan-2-ylphenyl)methylideneamino]benzamide
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Wang L Zuercher W J Consler T G et al. X-ray Crystal Structures of the Estrogen-related Receptor-? Ligand Binding Domain in Three Functional States Reveal the Molecular Basis of Small Molecule Regulation[J]. Journal of Biological Chemistry 2006 281(49):37773-37781.
molnova catalog



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