GSK-4716

SKU: orb1220987

Description

GSK4716 is an ERRβ/γ agonist (IC50 = 2 μM) that can activate the receptor with similar potency as the protein ligand.

Key Properties

• CAS Number: 101574-65-6
• MW: 282.34
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₈N₂O₂
• SMILES: CC(C)c1ccc(cc1)\C=N\NC(=O)c1ccc(O)cc1
• Target: Estrogen Receptor/ERR
• Solubility: DMSO:100 mg/mL (354.18 mM)

Bioactivity

• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Estrogen Receptor/ERR