F3806
法倔唑 盐酸盐
≥98% (HPLC), nonsteroidal aromatase inhibitor, powder
别名:
4-(5,6,7,8-Tetrahydroimidazo[1,5-a]pyridin-5-yl)-benzonitrile, Afema, CGS 16949A
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关于此项目
经验公式（希尔记法）:
C14H13N3·HCl
化学文摘社编号:
分子量:
259.73
UNSPSC Code:
51111800
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
法倔唑 盐酸盐, ≥98% (HPLC)
SMILES string
Cl.N#Cc1ccc(cc1)C2CCCc3cncn23
InChI key
UKCVAQGKEOJTSR-UHFFFAOYSA-N
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
assay
≥98% (HPLC)
form
powder
solubility
DMSO: >20 mg/mL
originator
Novartis
storage temp.
room temp
Quality Level
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
存储类别
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
法规信息
新产品
此项目有
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
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
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
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
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
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