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F3806

Sigma-Aldrich

Fadrozole hydrochloride

≥98% (HPLC)

Sinónimos:

4-(5,6,7,8-Tetrahydroimidazo[1,5-a]pyridin-5-yl)-benzonitrile, Afema, CGS 16949A

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10 MG
US$ 164,00
50 MG
US$ 655,00

US$ 164,00

Fecha estimada de envío26 de mayo de 2025

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10 MG
US$ 164,00
50 MG
US$ 655,00

About This Item

Fórmula empírica (notación de Hill):
C14H13N3·HCl
Número de CAS:
102676-31-3
Peso molecular:
259.73
Número MDL:
MFCD00866239
Código UNSPSC:
51111800
ID de la sustancia en PubChem:
329799706
NACRES:
NA.77

US$ 164,00

Fecha estimada de envío26 de mayo de 2025

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Nivel de calidad

100

Ensayo

≥98% (HPLC)

Formulario

powder

solubilidad

DMSO: >20 mg/mL

emisor

Novartis

temp. de almacenamiento

room temp

cadena SMILES

Cl.N#Cc1ccc(cc1)C2CCCc3cncn23

InChI

1S/C14H13N3.ClH/c15-8-11-4-6-12(7-5-11)14-3-1-2-13-9-16-10-17(13)14;/h4-7,9-10,14H,1-3H2;1H

Clave InChI

UKCVAQGKEOJTSR-UHFFFAOYSA-N

Acciones bioquímicas o fisiológicas

Fadrozole is a nonsteroidal aromatase inhibitor.
Fadrozole is a nonsteroidal aromatase inhibitor. Fadrozole is a very potent and highly selective inhibitor of the aromatase enzyme system in vitro and estrogen biosynthesis in vivo. It inhibited the conversion of [4-14C]androstenedione to [4-14C]estrone by human placental microsomes in a competitive manner (Ki = 1.6 nM). At a substrate concentration 3-fold the Km, Fadrozole was 180 times more potent, as an inhibitor, than aminoglutethimide (Cat. No. A9657), exhibiting half-maximal inhibition at 1.7 nM as compared to 0.3 μM. In vivo, Fadrozole lowered ovarian estrogen synthesis by gonadotropin-primed, androstenedione treated, immature rats by 90% at a dose of 260 μg/kg (PO). In vivo, Fadrozole leads to sequelae of estrogen deprivation (e.g. regression of DMBA-induced mammary tumors) without causing adrenal hypertrophy in adult rats. It blocked aromatase by 50% in human breast cancer homogenates, live breast cancer cells, human placental microsomes, and porcine ovarian microsomes at concentrations of 0.008 to 0.02 μM.

Características y beneficios

This compound was developed by Novartis. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Pictogramas

Skull and crossbonesHealth hazard
GHS06,GHS08

Palabra de señalización

Danger

Frases de peligro

H301,H361

Clasificaciones de peligro

Acute Tox. 3 Oral - Repr. 2

Código de clase de almacenamiento

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

Clase de riesgo para el agua (WGK)

WGK 2

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable

Equipo de protección personal

dust mask type N95 (US), Eyeshields, Faceshields, Gloves

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Certificados de análisis (COA)

Lot/Batch Number
0000325376
0000325376
0000109981
0000109981
0000063098

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M Gust et al.
Chemosphere, 79(1), 47-53 (2010-02-16)
The freshwater prosobranch Potamopyrgus antipodarum (Molluska, Hydrobiidea, Smith 1889) has been proposed as a suitable species to assess the impact of endocrine disrupting compounds (EDC) in aquatic ecosystems. Steroid hormone biosynthesis pathway is potentially an important target for EDC, and
K J Ralston-Hooper et al.
Environmental science & technology, 47(2), 1091-1100 (2012-11-28)
Although two-dimensional electrophoresis (2D-GE) remains the basis for many ecotoxicoproteomic analyses, newer non-gel-based methods are beginning to be applied to overcome throughput and coverage limitations of 2D-GE. The overall objective of our research was to apply a comprehensive, liquid chromatography-tandem
Dapeng Zhang et al.
Comparative biochemistry and physiology. Toxicology & pharmacology : CBP, 152(2), 202-206 (2010-04-15)
It has been extensively documented that exposure of amphibians and teleost fish to exogenous steroid hormones like estrogen, androgen, xenoestrogen or steroid biosynthesis inhibitors can impair their gonadal development or induce sex reversal against genotypic sex. However, the molecular pathways
Luke Remage-Healey et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 32(24), 8231-8241 (2012-06-16)
The activity of sensory circuits is shaped by neuromodulators, which can have downstream consequences for both sensorimotor integration and behavioral output. Recent evidence indicates that brain-derived estrogens ("neuroestrogens") can act as local circuit modulators in the songbird auditory forebrain. Specifically
Bing S Huang et al.
American journal of physiology. Heart and circulatory physiology, 299(2), H422-H430 (2010-06-01)
An increase in plasma ANG II causes neuronal activation in hypothalamic nuclei and a slow pressor response, presumably by increasing sympathetic drive. We evaluated whether the activation of a neuromodulatory pathway, involving aldosterone and "ouabain," is involved in these responses.
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