GSK 4716
|
|
|
- CAS号:
- 101574-65-6
- 英文名:
- 4-HYDROXY-2-[(1E)-[4-(1-METHYLETHYL)PHENYL]METHYLENE]HYDRAZIDE
- 英文别名:
- CS-1084;4-hydroxy-N'-(4-isopropylbenzylidene)benzohydrazide;(E)-4-hydroxy-N'-(4-isopropylbenzylidene)benzohydrazide;4-hydroxy-N'-(4-isopropylphenyl‐
methylidene)-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
- 中文名:
- GSK 4716
- 中文别名:
- 化合物GSK-4716;GSK 4716,ERRΒΓ激动剂;(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
- 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
-
|
GSK 4716性质、用途与生产工艺
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。
GSK-4716 是一种选择性 ERRβ/γ 激动剂。
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
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/16 | S0358 | GSK 4716
GSK-4716 | 101574-65-6 | 5mg | 4479.93元 |
| 2024/01/16 | S0358 | GSK 4716
GSK-4716 | 101574-65-6 | 25mg | 13505.3元 |
101574-65-6, GSK 4716 相关搜索:
- Selective agonist at estrogen-related receptors ERRβ and ERRγ.
- 合成有机化合物配体
- GSK 4716,ERRΒΓ激动剂
- 化合物GSK-4716
- (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
- 101574-65-6
- 4-hydroxy-N'-(4-isopropylphenyl‐
methylidene)-benzohydrazide
- Benzoic acid, 4-hydroxy-, 2-[[4-(1-methylethyl)phenyl]methylene]hydrazide
- CS-1084
- 4-hydroxy-N'-(4-isopropylbenzylidene)benzohydrazide
- 2-[[4-(1-Methylethyl)phenyl]methylene]hydrazide 4-hydroxybenzoic acid
- 4-HYDROXY-2-[(1E)-[4-(1-METHYLETHYL)PHENYL]METHYLENE]HYDRAZIDE
- 4-Hydroxybenzoic acid 2-[[4-(1-methylethyl)phenyl]methylene]hydrazide
- (E)-4-hydroxy-N'-(4-isopropylbenzylidene)benzohydrazide