Arzoxifene hydrochloride
Modify Date: 2024-01-10 09:32:57
Arzoxifene hydrochloride structure
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Common Name | Arzoxifene hydrochloride | ||
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| CAS Number | 182133-27-3 | Molecular Weight | 512.060 | |
| Density | N/A | Boiling Point | 656.4ºC at 760mmHg | |
| Molecular Formula | C28H30ClNO4S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 350.8ºC | |
Use of Arzoxifene hydrochlorideArzoxifene hydrocloride is a selective estrogen receptor modulator that is a potent estrogen antagonist in mammary and uterine tissue while acting as an estrogen agonist to maintain bone density and lower serum cholesterol. |
| Name | 2-(4-methoxyphenyl)-3-[4-(2-piperidin-1-ylethoxy)phenoxy]-1-benzothiophen-6-ol,hydrochloride |
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| Synonym | More Synonyms |
| Description | Arzoxifene hydrocloride is a selective estrogen receptor modulator that is a potent estrogen antagonist in mammary and uterine tissue while acting as an estrogen agonist to maintain bone density and lower serum cholesterol. |
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| Related Catalog | |
| Target |
Estrogen receptor[1] |
| In Vitro | 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]. |
| In Vivo | 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 ED50 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 ED50 of 0.03 mg/kg/day[2]. |
| 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]. |
| Animal Admin | 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]. |
| References |
| Boiling Point | 656.4ºC at 760mmHg |
|---|---|
| Molecular Formula | C28H30ClNO4S |
| Molecular Weight | 512.060 |
| Flash Point | 350.8ºC |
| Exact Mass | 511.158417 |
| PSA | 79.40000 |
| LogP | 7.67940 |
| Vapour Pressure | 7.85E-18mmHg at 25°C |
| 2-(4-Methoxyphenyl)-3-{4-[2-(1-piperidinyl)ethoxy]phenoxy}-1-benzothiophene-6-ol hydrochloride (1:1) |
| Benzo[b]thiophene-6-ol, 2-(4-methoxyphenyl)-3-[4-[2-(1-piperidinyl)ethoxy]phenoxy]-, hydrochloride (1:1) |
| UNII:FU88PI0433 |
| SERM 3 |
| ARZOXIFENE HCL |
| Arzoxifene hydrochloride |