1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAnastrozoleCat. No.: HY-14274CAS No.: 120511-73-1Synonyms: ZD1033分式: CHN分量: 293.37作靶點: Aromatase作通路: Others儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 150 mg/mL (511.30 mM)* means solub

2、le, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.4087 mL 17.0433 mL 34.0866 mL5 mM 0.6817 mL 3.4087 mL 6.8173 mL10 mM 0.3409 mL 1.7043 mL 3.4087 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Anastrozole種選擇性的芳酶 (aromatase) 抑制劑，抑制胎盤芳化酶，IC50 為 15 nM

3、。IC50 & Target IC50: 15 nM (human aromatase) 1體外研究Anastrozole is a comparatively simple, achiral benzyltriazole derivative, that inhibits human placental1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEaromatase with an IC50 of 15 nM. In the same assay it is 200 times as potent as aminoglutethimide

4、(AG),twice as potent as 4-OHA and one third as potent as Fadrozole 1.體內(nèi)研究 Groups of eight immature (22-day-old) female rats are given androstenedione (AD) (30 mg/kg) in arachis oils.c. daily for3 days with or without various doses of Anastrozole p.o. on day 4 the uteri are dissected, blottedand weig

5、hed. An oral dose of 0.1 mg/kg of Anastrozole given on day 2 or day 3 of the cycle completelyblocked ovulation. At the same daily dosage (0.1 mg/kg), Anastrozole completely extinguished theuterotrophic activity of exogenous AD in immature rats. In male pigtailed monkeys, twice-daily oral treatmentwi

6、th 0.1 mg/kg and above of Anastrozole reduced circulating oestradiol concentrations by 50-60% 1.PROTOCOLKinase Assay 1 Aromatase inhibition is measured using human placental microsomes and the method of Thompson andSiiteri with Testosterone (0.5 M) as substrate. 11-hydroxylase inhibition is determin

7、ed by measuring theconversion of 1,2,6,7-3H-ll-deoxy- cortisol to cortisol using freshly prepared mitochondria from guinea pig,dog and cow adrenal glands. Reaction products areextracted into chloroform and separated by thin layerchromatography 1.MCE has not independently confirmed the accuracy of th

8、ese methods. They are for reference only.Animal Mice 1Administration 1 Groups of at least eight adult female rats, housed in controlled lighting (on 06.00-20.00 h) and temperature(242C) and undergoing 4-day oestrous cycles, are treated p.o. with a single dose of Anastrozole (0.01-0.1mg/kg), Fadrozol

9、e (0.01-0.1 mg/kg) or AG (5-20 mg/kg) on day 2 at 16.00 h or day 3 at 12.00 h. Thepresence or absence of eggs in the oviducts on day 1 of the next cycle is then determined. Ovulation isconsidered blocked when no eggs are found.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Dukes M, et al. The preclinical pharmacology of Arimidex (anastrozole; ZD1033)-a potent, selective aromatase inhibitor. J SteroidBiochem Mol Biol. 1996 Jul;58(4):439-45.McePdfHeightCaution: Product has not been fully validated