An ERRβ/γ agonist
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GSK4716

Item No. 17233

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-hydroxy-2-[[4-(1-methylethyl)phenyl]methylene]hydrazide benzoic acid
CAS Number
101574-65-6
Molecular Formula
C17H18N2O2
Formula Weight
282.3
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 16 mg/mlEthanol: 20 mg/mlEthanol:PBS (pH 7.2) (1:6): 0.14 mg/ml
λmax
220, 309 nm
SMILES
OC1=CC=C(C(N/N=C/C2=CC=C(C(C)C)C=C2)=O)C=C1
InChi Code
InChI=1S/C17H18N2O2/c1-12(2)14-5-3-13(4-6-14)11-18-19-17(21)15-7-9-16(20)10-8-15/h3-12,20H,1-2H3,(H,19,21)/b18-11+
InChi Key
IKPPIUNQWSRCOZ-WOJGMQOQSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $44

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    10 mg

    $71

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    50 mg

    $304

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    Product Description

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

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wang, L., Zuercher, W.J., Consler, T.G., et al. X-ray crystal structures of the estrogen-related receptor-gamma ligand binding domain in three functional states reveal the molecular basis of small molecule regulation. The Journal of Biological Chemisty 281(49), 37773-37781 (2006).

    2. Rangwala, S.M., Wang, X., Calvo, J.A., et al. Estrogen-related receptor γ is a key regulator of muscle mitochondrial activity and oxidative capacity. The Journal of Biological Chemisty 285(29), 22619-22629 (2010).