4-HYDROXY-2-[(1E)-[4-(1-METHYLETHYL)PHENYL]METHYLENE]HYDRAZIDE Chemical Properties

Density 

1.12

storage temp. 

Inert atmosphere,2-8°C

solubility 

DMSO: >10mg/mL

form 

powder

pka

8.48±0.15(Predicted)

color 

white to off-white

Safety Information

Hazard Codes 

Xi,N

Risk Statements 

43-50/53

Safety Statements 

36/37-60-61

RIDADR 

UN 3077 9 / PGIII

WGK Germany 

3

HazardClass 

9

4-HYDROXY-2-[(1E)-[4-(1-METHYLETHYL)PHENYL]METHYLENE]HYDRAZIDE Usage And Synthesis

Description

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. GSK4716 is an ERRβ/γ agonist (IC₅₀ = 2 μM) that can activate the receptor with similar potency as the protein ligand, PGC-1α. It is more than 50-fold selective for binding to ERRβ/γ compared with the estrogen receptors. This compound has been used to demonstrate the contribution of ERR receptor activity to the regulation of mitochondrial activity in skeletal muscle during exercise.

Uses

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. GSK4716 is an ERRβ/γ agonist (IC50 = 2 μM) that can activate the receptor with similar potency as the protein ligand, PGC-1α. It is more than 50-fold selective for binding to ERRβ/γ compared with the estrogen receptors. This compound has been used to demonstrate the contribution of ERR receptor activity to the regulation of mitochondrial activity in skeletal muscle during exercise.[Cayman Chemical]

Uses

Selective agonist at estrogen-related receptors ERR and ERR

Definition

ChEBI: GSK 4716 is a monoterpenoid.

Biological Activity

Selective agonist at estrogen-related receptors ERR β and ERR γ . Displays selectivity over ERR α and the classical estrogen receptors.

storage

Store at +4°C

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