Drug intelligence / Profile preview

methyl-piperidino-pyrazole

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral (investigational/research Use), Intraperitoneal (preclinical/research Use)
01

Overview

**Methyl-piperidino-pyrazole (MPP)** is a highly selective estrogen receptor alpha (**ERα**) antagonist in the triarylpyrazole class. It demonstrates strong selectivity for ERα over ERβ (K_i = 5.6 nM for ERα, 2.3 μM for ERβ), and inhibits the transcriptional activation of ERα (IC_50 ranging from 20–80 nM). Developed as a research tool and potential lead compound for selective estrogen receptor modulation, MPP is used to study estrogen signaling, tissue selectivity, and mechanisms in models of estrogen-responsive cancers and metabolic diseases. It acts as a selective estrogen receptor modulator (SERM) with antagonist activity in systems driven by ERα, and has enabled dissection of ERα function apart from ERβ and off-target effects common to less selective agents[1][2][5][7].

Other names
methyl-piperidino-pyrazoleMPP4-[1-(4-hydroxyphenyl)-4-methyl-5-[4-[2-(1-piperidinyl)ethoxy]phenyl]-1H-pyrazol-3-yl]-phenolCAS 289726-02-9CAS289726-02-9CAS-289726-02-9methylpiperidinopyrazole
02

Targets

ESR2 (ERβ)ESR1 (ERα)

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