GSK4716
货号:
17233-5mg 基本售价:
490.0 元 规格:
5 mg
产品信息
概述货号 | 17233-5mg |
描述 | 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.1 GSK4716 is an ERRβ/γ agonist (IC50 = 2 µM) that can activate the receptor with similar potency as the protein ligand, PGC-1α.2 It is more than 50-fold selective for binding to ERRβ/γ compared with the estrogen receptors.2 This compound has been used to demonstrate the contribution of ERR receptor activity to the regulation of mitochondrial activity in skeletal muscle during exercise.3 |
性能供应商 | Cayman |
应用文献 |
1.Schreiber, S.N.,Knutti, D.,Brogli, K., et al. The transcriptional coactivator PGC-1 regulates the expression and activity of the orphan nuclear receptor estrogen-related receptor α (ERRα). The Journal of Biological Chemisty 278(11), 9013-9018 (2003). 2.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). 3.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).
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运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 282.3 |
分子式 | C17H18N2O2 |
CAS号 | 101574-65-6 |
稳定性 | ≥ 2 years |
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