GSK 4716

简介生物活性靶点体外研究 GSK 4716 试剂级价格

GSK 4716

CAS号:101574-65-6
英文名:4-HYDROXY-2-[(1E)-[4-(1-METHYLETHYL)PHENYL]METHYLENE]HYDRAZIDE
中文名:GSK 4716
CBNumber:CB02446303
分子式:C17H18N2O2
分子量:282.34
MOL File:101574-65-6.mol

GSK 4716化学性质

密度 :1.12
储存条件 :Inert atmosphere,2-8°C
溶解度 :DMSO: >10mg/mL
形态 :powder
酸度系数(pKa) :8.48±0.15(Predicted)
颜色 :white to off-white

安全信息

危险品标志 :Xi,N
危险类别码 :43-50/53
安全说明 :36/37-60-61
危险品运输编号 :UN 3077 9 / PGIII
WGK Germany :3
危险等级 :9

GSK 4716性质、用途与生产工艺

简介雌激素相关受体 (ERR) 是与雌激素受体家族同源的孤儿核受体，在具有高代谢需求的组织中表达。已知过氧化物酶体增殖物激活受体 γ-共激活因子 1α (PGC-1α) 与这类受体的结合会增强 ERR 活性。GSK4716 是一种 ERRβ/γ 激动剂 (IC50 = 2 μM)，可以激活受体，其效力与蛋白质配体 PGC-1α 相似。与雌激素受体相比，它与 ERRβ/γ 结合的选择性超过 50 倍。该化合物已被用于证明 ERR 受体活性对运动期间骨骼肌中线粒体活性的调节的贡献。
生物活性 GSK-4716 是一种选择性 ERRβ/γ 激动剂。
靶点

ERRβ/γ
体外研究

Treatment of differentiated C2C12 cells with the ERRβ/γ agonist (relative to vehicle) over a 2 to 4 h time period reveals a reproducible and robust increase in the immunoreactivity of the GRα-D isoform. It is observed that MAO-A mRNA expression is significantly increased by treatment with the ERRβ/γ agonist, GSK4716. Furthermore, it is observed that GSK4716 induces the expression of the mRNAs encoding peroxisome proliferator-activated receptor-γcoactivator 1α (PGC-1α) and PGC-1β (key regulator of many metabolic genes) identified as direct coactivators for the ERR family. GSK4716 induces the expression of PGC-1 and genes involved in fatty acid oxidation in concordance with the characterized role of ERRγ in cardiac metabolism. Treatment of primary mouse myotubes with GSK4716, an ERRβ/γ agonist, results in a concerted increase in the expression levels of Ppargc1a , Ppargc1b , and the Esrr genes. Furthermore, Cpt1b , Atp5b , and Idh3 , genes in key mitochondrial pathways, are also induced by GSK4716. Additionally, GSK4716 increases citrate synthase activity and cytochrome c protein levels.