F3806
Fadrozole hydrochloride
≥98% (HPLC), nonsteroidal aromatase inhibitor, powder
Sinónimos:
4-(5,6,7,8-Tetrahydroimidazo[1,5-a]pyridin-5-yl)-benzonitrile, Afema, CGS 16949A
Iniciar sesión para ver los precios por organización y contrato.
Seleccione un Tamaño
Cambiar Vistas
Acerca de este artículo
Fórmula empírica (notación de Hill):
C14H13N3·HCl
Número CAS:
Peso molecular:
259.73
UNSPSC Code:
51111800
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Servicio técnico
¿Necesita ayuda? Nuestro equipo de científicos experimentados está aquí para ayudarle.
Permítanos ayudarleNombre del producto
Fadrozole hydrochloride, ≥98% (HPLC)
Quality Level
assay
≥98% (HPLC)
form
powder
solubility
DMSO: >20 mg/mL
originator
Novartis
storage temp.
room temp
SMILES string
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
InChI key
UKCVAQGKEOJTSR-UHFFFAOYSA-N
Biochem/physiol Actions
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.
Features and Benefits
This compound was developed by Novartis. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
signalword
Danger
hcodes
Hazard Classifications
Acute Tox. 3 Oral - Repr. 2
Clase de almacenamiento
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
dust mask type N95 (US), Eyeshields, Faceshields, Gloves
Elija entre una de las versiones más recientes:
¿Ya tiene este producto?
Encuentre la documentación para los productos que ha comprado recientemente en la Biblioteca de documentos.
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
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
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