A selective ERRβ/γ agonist (IC50 = 2 µM) that can activate the receptor with similar potency as the protein ligand

GSK4716 – 5 mg

Brand:
Cayman
CAS:
101574-65-6
Storage:
-20
UN-No:
Non-Hazardous - /

The estrogen-related receptors (ERRs) are orphan nuclear receptors with homology to the estrogen receptor family and are expressed in tissues with high metabolic demand. Binding of peroxisome proliferator-activated receptor γ-coactivator 1α (PGC-1α) to this class of receptors is known to potentiate ERR activity.{12071} GSK4716 is an ERRβ/γ agonist (IC50 = 2 µM) that can activate the receptor with similar potency as the protein ligand, PGC-1α.{28181} It is more than 50-fold selective for binding to ERRβ/γ compared with the estrogen receptors.{28181} This compound has been used to demonstrate the contribution of ERR receptor activity to the regulation of mitochondrial activity in skeletal muscle during exercise.{28182}  

 

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Description

A selective ERRβ/γ agonist (IC50 = 2 µM) that can activate the receptor with similar potency as the protein ligand, PGC-1α

Formal name: 4-hydroxy-2-[[4-(1-methylethyl)phenyl]methylene]hydrazide benzoic acid

Synonyms: 

Molecular weight: 282.3

CAS: 101574-65-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Cell Biology|Mitochondrial Biology||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Estrogens & Progestins

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