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)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
5MG 34 In Stock
10MG 52 In Stock
25MG 118 In Stock
50MG 227 In Stock
100MG 422 In Stock
200MG Get Quote In Stock
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Biological Information

  • Product Name
    GSK-4716
  • Note
    Research use only, not for human use.
  • Brief Description
    GSK4716 is an ERRβ/γ agonist (IC50 = 2 μM) that can activate the receptor with similar potency as the protein ligand.
  • Description
    GSK4716 is an ERRβ/γ agonist (IC50 = 2 μM) that can activate the receptor with similar potency as the protein ligand.
  • In Vitro
    Treatment 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.
  • In Vivo
    ——
  • Synonyms
    ——
  • Pathway
    Endocrinology/Hormones
  • Target
    Estrogen Receptor/ERR
  • Recptor
    ERRβ/γ
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    101574-65-6
  • Formula Weight
    282.34
  • Molecular Formula
    C17H18N2O2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:100 mg/mL?(354.18 mM)
  • SMILES
    CC(C)c1ccc(cc1)\C=N\NC(=O)c1ccc(O)cc1
  • Chemical Name
    4-hydroxy-N-[(4-propan-2-ylphenyl)methylideneamino]benzamide

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • 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.
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