X4753
XCT790
≥98% (HPLC), ERRα agonist, solid
别名:
3-[4-（2,4-双-三氟甲基苄氧基）-3-甲氧基苯基]-2-氰基-N-（5-三氟甲基-1,3,4-噻二唑-2-基）丙烯酰胺
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关于此项目
经验公式（希尔记法）:
C23H13F9N4O3S
化学文摘社编号:
分子量:
596.42
MDL编号:
UNSPSC代码:
12352202
PubChem化学物质编号:
NACRES:
NA.77
产品名称
XCT790, ≥98% (HPLC), solid
质量水平
方案
≥98% (HPLC)
表单
solid
颜色
yellow
溶解性
DMSO: ≥10 mg/mL
储存温度
2-8°C
SMILES字符串
COc1cc(ccc1OCc2ccc(cc2C(F)(F)F)C(F)(F)F)\C=C(/C#N)C(=O)Nc3nnc(s3)C(F)(F)F
InChI
1S/C23H13F9N4O3S/c1-38-17-7-11(6-13(9-33)18(37)34-20-36-35-19(40-20)23(30,31)32)2-5-16(17)39-10-12-3-4-14(21(24,25)26)8-15(12)22(27,28)29/h2-8H,10H2,1H3,(H,34,36,37)/b13-6+
InChI key
HQFNFOOGGLSBBT-AWNIVKPZSA-N
应用
XCT790已被用于：
- 在C2C12肌管中作为雌激素相关受体（ERR）α 的反向激动剂
- 作为雌激素相关受体（ERR）α 反向激动剂以阐明ERR的蜕膜功能α 子宫内膜胚胎干细胞中
- 作为人类神经母细胞瘤SH-SY5Y和HeLa细胞系中的自噬诱导剂。
生化/生理作用
XCT 790是一种5′腺苷单磷酸激活蛋白激酶（AMPK）激活剂。它还可充当线粒体中的质子离子载体和氧化磷酸化的解偶联剂。XCT790会破坏血管内皮生长因子（VEGF）和血管生成素2（Ang-2）的表达，并通过雌激素相关受体（ERRα）抑制表现出对子宫内膜肿瘤的抑制作用。XCT790可介导细胞周期停滞并促进三阴性乳腺癌（TNBC）的凋亡。
XCT790 是一种强效、特异性的 ERRα 反向激动剂。XCT790 具有选择性，在浓度低于 10 μM 时，对相关核受体（如 ERRγ 或 ERα）无明显拮抗活性。在使用 GAL4-ERR LBD 或全长 ERR 和 mSHP 启动子的瞬时转染试验中，IC 50 值为 300-500 nM。
XCT790 是一种强效、特异性的 ERRα 反向激动剂。选择性；在 10 μM 以下浓度时，对相关核受体，如 ERRγ 或 ERα 显示无明显拮抗活性。
危险声明
预防措施声明
危险分类
Aquatic Chronic 4
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
Eyeshields, Gloves, type N95 (US)
Rasmus J O Sjögren et al.
Diabetologia, 64(9), 2077-2091 (2021-06-17)
Increased levels of branched-chain amino acids (BCAAs) are associated with type 2 diabetes pathogenesis. However, most metabolomic studies are limited to an analysis of plasma metabolites under fasting conditions, rather than the dynamic shift in response to a metabolic challenge.
Ying-Min Wu et al.
Oncotarget, 7(11), 12568-12581 (2016-02-13)
There is an urgent clinical need for targeted therapy approaches for triple-negative breast cancer (TNBC) patients. Increasing evidences suggested that the expression of estrogen-related receptor alpha (ERRα) was correlate with unfavorable clinical outcomes of breast cancer patients. We here show
J Z Hu et al.
Neuroscience, 290, 570-580 (2015-02-11)
Estrogen receptor-related receptor-α (ERRα) is an orphan member of the nuclear receptor superfamily that interacts with peroxisome proliferator-activated receptor γ coactivator-1α (PGC-1α) to stimulate vascular endothelial growth factor (VEGF) expression and angiogenesis in a hypoxia-inducible factor-1α-independent pathway. Although it is
W F Theeuwes et al.
Biochimica et biophysica acta. Molecular cell research, 1867(2), 118610-118610 (2019-11-19)
In muscle cells, the peroxisome proliferator-activated receptor γ co-activator 1 (PGC-1) signaling network, which has been shown to be disturbed in the skeletal muscle in several chronic diseases, tightly controls mitochondrial biogenesis and oxidative substrate metabolism. Previously, we showed that
G Vargas et al.
Oncogene, 38(7), 950-964 (2018-11-28)
Bone is the most common metastatic site for breast cancer. Estrogen-related-receptor alpha (ERRα) has been implicated in cancer cell invasiveness. Here, we established that ERRα promotes spontaneous metastatic dissemination of breast cancer cells from primary mammary tumors to the skeleton.
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