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101574-65-6

中文名称 GSK 4716
英文名称 4-HYDROXY-2-[(1E)-[4-(1-METHYLETHYL)PHENYL]METHYLENE]HYDRAZIDE
CAS 101574-65-6
分子式 C17H18N2O2
分子量 282.34
MOL 文件 101574-65-6.mol
更新日期 2024/04/26 20:46:01
101574-65-6 结构式 101574-65-6 结构式

基本信息

中文别名
(E)-4-羟基-N'-(4-异丙基亚苄基)苯并酰肼
4-羟基苯甲酸 2-[[4-(1-甲基乙基)苯基]亚甲基]肼
英文别名
CS-1084
4-hydroxy-N'-(4-isopropylbenzylidene)benzohydrazide
(E)-4-hydroxy-N'-(4-isopropylbenzylidene)benzohydrazide
4-HYDROXY-2-[(1E)-[4-(1-METHYLETHYL)PHENYL]METHYLENE]HYDRAZIDE
2-[[4-(1-Methylethyl)phenyl]methylene]hydrazide 4-hydroxybenzoic acid
4-Hydroxybenzoic acid 2-[[4-(1-methylethyl)phenyl]methylene]hydrazide
Benzoic acid, 4-hydroxy-, 2-[[4-(1-methylethyl)phenyl]methylene]hydrazide

物理化学性质

密度1.12
储存条件Inert atmosphere,2-8°C
溶解度二甲基亚砜:>10mg/mL
酸度系数(pKa)8.48±0.15(Predicted)
形态粉末
颜色白色至灰白色

安全数据

危险性符号(GHS)
GHS07,GHS09
警示词警告
危险性描述H317-H410
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 Germany3
危险等级9

常见问题列表

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.

GSK 4716价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/01/16S0358GSK 4716
GSK-4716
101574-65-65mg4479.93元
2024/01/16S0358GSK 4716
GSK-4716
101574-65-625mg13505.3元
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