FERb 033

• 常用名: FERb 033
• 英文名: FERb 033
• CAS号: 1111084-78-6
• 分子量: 281.66700
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₃H₉ClFNO₃
• 熔点: N/A
• 闪点: N/A

FERb 033用途

FERB033是一种选择性和有效的ERβ激动剂(Ki=7.1nM,EC50=4.8nM)。FERB033的选择性是ERα[1]的62倍。

FERb 033名称

• 英文名: 2-Chloro-3'-fluoro-4-[(E)-(hydroxyimino)methyl]-3,4'-biphenyldiol

FERb 033生物活性

• 描述: FERB033是一种选择性和有效的ERβ激动剂(Ki=7.1nM,EC50=4.8nM)。FERB033的选择性是ERα[1]的62倍。
• 相关类别:
  信号通路 >> 其他 >> 雌激素受体/ERR
  研究领域 >> 内分泌
• 靶点实验:

  ERβ:4.8 nM (EC50)

  ERβ:7.1 nM (Ki)

• 体外研究: FERb 033(0-100μM)对反式激活中的雌激素受体(ESR)全长具有特异性[2]。FERb 033(10 nM,2 h)治疗轻度降低气道平滑肌(ASM)细胞中的Ca2+反应[3]。细胞活力测定[2]细胞系：HEK293细胞浓度：0-100μM孵育时间：结果：通过ERE上的全长受体诱导转录活性,ESR1和ESR2的EC50值分别为0.253和0.053μM。细胞存活率测定[3]细胞系：ASM细胞浓度：10nM孵育时间：2小时结果：在非稳态人ASM细胞中,组胺诱导的Ca2+反应趋于减少,但与对照组相比无显著性差异。
• 参考文献:

  [1]. Filippo Minutolo, et al. Structural evolutions of salicylaldoximes as selective agonists for estrogen receptor beta. J Med Chem. 2009 Feb 12;52(3):858-67.

  [2]. Satomi Kohno, et al. Estrogen receptor 1 (ESR1; ERα), not ESR2 (ERβ), modulates estrogen-induced sex reversal in the American alligator, a species with temperature-dependent sex determination. Endocrinology. 2015 May;156(5):1887-99.

  [3]. Sangeeta Bhallamudi, et al. Estrogen receptors differentially regulate intracellular calcium handling in human nonasthmatic and asthmatic airway smooth muscle cells. Am J Physiol Lung Cell Mol Physiol. 2020 Jan 1;318(1):L112-L124.

FERb 033物理化学性质

• 分子式: C₁₃H₉ClFNO₃
• 分子量: 281.66700
• 精确质量: 281.02500
• PSA: 73.05000
• LogP: 3.36540
• InChIKey: LRRMQNGSYOUANY-OMCISZLKSA-N
• SMILES: C1=CC(=C(C=C1C2=C(C(=C(C=C2)/C=N/O)O)Cl)F)O

FERb 033靶点实验

查看更多实验

实验名称：Discovery of Small Molecules to Inhibit Human Cytomegalovirus Nuclear Egress 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：HCMV UL50 External Id：HMS1262

实验名称：Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VER... 来源：ChEMBL 靶标：Severe acute respiratory syndrome coronavirus 2 External Id：CHEMBL4513082

实验名称：Rescue cell viability in cybrid cells with a genetic mutation in complex 1 of the mit... 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：N/A External Id：HMS1315

实验名称：Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Cac... 来源：ChEMBL 靶标：Severe acute respiratory syndrome coronavirus 2 External Id：CHEMBL4303805

实验名称：SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response f... 来源：ChEMBL 靶标：Replicase polyprotein 1ab External Id：CHEMBL4495582

实验名称：Tocris HTS for Inhibitors of Aerobactin Synthetase lucA 来源：23265 External Id：IucA Pilot Assay Tocris Library

实验名称：Ratio of relative binding affinity for full-length human estrogen receptor beta to ra... 来源：ChEMBL 靶标：N/A External Id：CHEMBL993944

实验名称：Displacement of [3H]estradiol from full-length human estrogen receptor beta by radiom... 来源：ChEMBL 靶标：Estrogen receptor beta External Id：CHEMBL993943

实验名称：Agonist activity at full-length human estrogen receptor beta expressed in human HEC1 ... 来源：ChEMBL 靶标：Estrogen receptor beta External Id：CHEMBL993946

实验名称：Enzymatic assay of human HDAC6 with commercial peptide substrate 来源：ChEMBL 靶标：Histone deacetylase 6 External Id：CHEMBL4808149

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FERb 033英文别名

• DMPQ dihydrochloride
• 2-Pentenoic acid,3-(chlorocarbonyl)-4-methyl-,methyl ester,(E)
• (E)-3-carbomethoxy-2-(1-methylethyl)prop-2-enoyl chloride
• (E)-3-chloro-4-(3-fluoro-4-hydroxyphenyl)salicylaldoxime