Estrogen receptor antagonist 8

Names

[ CAS No. ]:
2889370-92-5

[ Name ]:
Estrogen receptor antagonist 8

Biological Activity

[Description]:

Estrogen receptor antagonist 8 is a potent ER-antagonist with in vivo?anti-uterotrophic potential (EC50?=?4.160?μM)[1].

[Related Catalog]:

Signaling Pathways >> Others >> Estrogen Receptor/ERR

Research Areas >> Metabolic Disease

[Target]

Estrogen receptor

[In Vivo]

在体内抗子宫营养试验中，通过测量未成熟雌性大鼠子宫重量与对照组相比的减少，建立了剂量-反应曲线。 Estrogen receptor antagonist 8 (compound 4) (s.c.; 1、3、10、20、30 mg/Kg/天; 3 d) 表现出比 TMX 更好的抗子宫萎缩潜能 (EC50: 7.625 μM), Estrogen receptor antagonist 8 的 EC50 值为 4.160 μM[1]。

[References]

[1]. Mahmoud A Ragab, et al. Structure-based design and synthesis of conformationally constrained derivatives of methyl-piperidinopyrazole (MPP) with estrogen receptor (ER) antagonist activity. Bioorg Chem. 2022 Feb;119:105554.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₅H₂₁N₃O₄

[ Molecular Weight ]:
427.45

Related Compounds

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