Arzoxifene-hydrochloride-(LY-353381-HCl)-Estrogen-Receptor-ERR-Modulator-MedChemExpress

Arzoxifene hydrochloride Cat. No.:

HY-13556A CAS No.:

182133-27-3分?式:

C??H??ClNO?S 分?量:

512.06作?靶点:

Estrogen Receptor/ERR 作?通路:

Others 储存?式:Please store the product under the recommended conditions in the COA.BIOLOGICAL ACTIVITY

?物活性Arzoxifene hydrocloride 是?种选择性的雌激素受体 (estrogen receptor ) 调节剂，它是乳腺和?宫组织中有效的雌激素

拮抗剂，同时作为维持?密度和降低?清胆固醇的雌激素激动剂。

IC?? & Target

Estrogen receptor [1]体外研究Arzoxifene inhibits cell growth as effectively as the antiestrogen tamoxifen. Northern analysis reveals that arzoxifene

exerts a statistically significant inhibition of pS2 and progesterone receptor B mRNA expression. Significant agonistic effect is observed on the antitrypsin mRNA expression. In contrast to estradiol and tamoxifen, arzoxifene does not

upregulate cathepsin D mRNA and protein expression [1].

体内研究Arzoxifene prevents the ovariectomy-induced increase in body weight and serum cholesterol levels of treated rats

and lowers them to below sham levels in a dose dependent manner, with maximum efficacy similar to estrogen or

raloxifene. Arzoxifene (LY353381.HCl) prevents loss of bone due to ovariectomy with an ED 50 of about 0.01 mg/kg

with maximal efficacy observed at 0.1-1 mg/kg/day. Arzoxifene (LY353381.HCl) antagonizes the estrogen-induced

elevation in uterine weight down to vehicle-dosed control levels with ED 50 of 0.03 mg/kg/day [2].

PROTOCOL

Cell Assay For growth experiments, MCF-7 and MDA-MB-231 cells are treated with Arzoxifene HCl (LY353381.HCl) (0.1, 1, 10,

100, 1000 nM). Medium is renewed at days 3 and 5. At day 6, four wells are used for each cell-number determination by counting in a hemocytometer [1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Rats [2]

Antiestrogen activity is evaluated in 21-day old Sprague Dawley rats.17α-Ethynyl estradiol at 0.1 mg/kg/day is used as the estrogenic stimulus to increase uterine weight in these rats. Arzoxifene HCl (LY353381.HCl)LY353381.HCl

(0.001-10 mg/kg) or raloxifene (1 mg/kg) are administered by oral gavage in a volume of 0.2 mL, 15 min prior to the EE2 gavage. Dosing with test compounds is continued for 3 consecutive days. Animals are fasted over night,

following the final dose [2].

Animal

Administration [2]Product Data Sheet

Inhibitors ?Agonists ?Screening Libraries

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

REFERENCES

[1]. Suh N, et al. Arzoxifene, a new selective estrogen receptor modulator for chemoprevention of experimental breast cancer. Cancer Res. 2001 Dec 1;61(23):8412-5.

McePdfHeight

Caution: Product has not been fully validated for medical applications. For research use only.

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