94344-54-4

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苏木查耳酮

94344-54-4

编号ABP000973 化学名称苏木查耳酮 英文名称 sappanchalcone MDL: MFCD20274974 分子式C16H14O5 分子量286.282 纯度 >98%

化学名称 : 苏木查耳酮

CAS : 94344-54-4

英文名称: sappanchalcone

英文同义词: 2-Propen-1-one,3-(3,4-dihydroxyphenyl)-1-(4-hydroxy-2-methoxyphenyl)-, (2E)-

溶解度:Soluble in DMSO: >20 mg/mL

储存条件:Store at room temperature

生物活性

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.

参考文献

Van Meeuwen, J., et al., Aromatase inhibition by synthetic lactones and flavonoids in human placental microsomes and breast fibroblasts--a comparative study. Toxicol. Appl. Pharmacol. 228, 269-276, (2008) Minnaard-Huiban, M., et al., Fadrozole reverses cardiac fibrosis in spontaneously hypertensive heart failure rats: discordant enantioselectivity versus reduction of plasma aldosterone. Endocrinology 149, 28-31, (2008) Mikolajczyk, T., et al., The effect of aromatase inhibitor, fadrozole, on sGnRHa stimulated LH secretion in goldfish (Carassius auratus) and common carp (Cyprinus carpio). Reprod. Biol. 6, 195-199, (2006) Merck 14,3927
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