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F3806

Sigma-Aldrich

Fadrozole hydrochloride

≥98% (HPLC)

Sinônimo(s):

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

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10 MG
R$ 860,00
50 MG
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About This Item

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

R$ 860,00

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Nível de qualidade

100

Ensaio

≥98% (HPLC)

Formulário

powder

solubilidade

DMSO: >20 mg/mL

originador

Novartis

temperatura de armazenamento

room temp

cadeia de caracteres 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

chave InChI

UKCVAQGKEOJTSR-UHFFFAOYSA-N

Ações bioquímicas/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 e benefícios

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

Palavra indicadora

Danger

Frases de perigo

H301,H361

Classificações de perigo

Acute Tox. 3 Oral - Repr. 2

Código de classe de armazenamento

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

Classe de risco de água (WGK)

WGK 2

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable

Equipamento de proteção individual

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

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Certificados de análise (COA)

Lot/Batch Number
0000325376
0000325376
0000109981
0000109981
012M4719V

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Thierry D Charlier et al.
General and comparative endocrinology, 167(1), 18-26 (2010-02-11)
Local aromatization of testosterone into 17beta-estradiol (E(2)) is often required for the physiological and behavioral actions of testosterone. In most vertebrates, aromatase is expressed in a few discrete brain regions. While many studies have measured brain aromatase mRNA or activity
Aviva Gamliel-Lazarovich et al.
Journal of hypertension, 28(9), 1900-1907 (2010-08-12)
Aldosterone is known to be involved in atherosclerosis and cardiovascular disease and blockade of its receptor was shown to improve cardiovascular function. It was, therefore, hypothesized that inhibition of aldosterone synthesis would also reduce atherosclerosis development. To test this hypothesis
Elizabeth Adkins-Regan
Frontiers in neuroendocrinology, 32(2), 155-163 (2011-02-01)
A majority of birds are socially monogamous, providing exceptional opportunities to discover neuroendocrine mechanisms underlying preferences for opposite-sex partners where the sexes form extended affiliative relationships. Zebra finches have been the focus of the most systematic program of research to
Devy Deliyanti et al.
Hypertension (Dallas, Tex. : 1979), 59(3), 607-613 (2012-01-26)
Neovascularization is a hallmark feature of retinopathy of prematurity and diabetic retinopathy. Type 1 angiotensin receptor blockade reduces neovascularization in experimental retinopathy of prematurity, known as oxygen-induced retinopathy (OIR). We investigated in OIR whether inhibiting aldosterone with the aldosterone synthase
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
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