추천 제품
Quality Level
분석
≥98% (HPLC)
양식
powder
solubility
DMSO: >20 mg/mL
주관자
Novartis
저장 온도
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
생화학적/생리학적 작용
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.
특징 및 장점
This compound was developed by Novartis. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
신호어
Danger
유해 및 위험 성명서
Hazard Classifications
Acute Tox. 3 Oral - Repr. 2
Storage Class Code
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
개인 보호 장비
dust mask type N95 (US), Eyeshields, Faceshields, Gloves
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시험 성적서(COA)
Lot/Batch Number
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
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
Sarah A Heimovics et al.
Endocrinology, 153(3), 1364-1376 (2012-02-02)
Across vertebrate species, 17β-estradiol (E(2)) acts on the brain via both genomic and nongenomic mechanisms to influence neuronal physiology and behavior. Nongenomic E(2) signaling is typically initiated by membrane-associated estrogen receptors that modulate intracellular signaling cascades, including rapid phosphorylation of
문서
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