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

CAS NO.：101574-65-6
Empirical Formula: C17H18N2O2
Molecular Weight: 282.34
MDL number: MFCD00567155
SAFETY DATA SHEET (SDS)
Update Date: 2024-11-19 23:02:33

What is 4-HYDROXY-2-[(1E)-[4-(1-METHYLETHYL)PHENYL]METHYLENE]HYDRAZIDE?

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.

The Uses of 4-HYDROXY-2-[(1E)-[4-(1-METHYLETHYL)PHENYL]METHYLENE]HYDRAZIDE

Selective agonist at estrogen-related receptors ERR and ERR

The Uses of 4-HYDROXY-2-[(1E)-[4-(1-METHYLETHYL)PHENYL]METHYLENE]HYDRAZIDE

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]

Definition

ChEBI: GSK 4716 is a monoterpenoid.

What are the applications of Application

GSK 4716 is a selective agonist with estrogen-related receptors ERRβ and ERRγ

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

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

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

Signal word	Warning
Pictogram(s)	Exclamation Mark Irritant GHS07 Environment GHS09
GHS Hazard Statements	H317:Sensitisation, Skin H410:Hazardous to the aquatic environment, long-term hazard
Precautionary Statement Codes	P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P272:Contaminated work clothing should not be allowed out of the workplace. P273:Avoid release to the environment. P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of soap and water. P333+P313:IF SKIN irritation or rash occurs: Get medical advice/attention.