Introduction：Basic information about CAS 182133-27-3|Arzoxifene hydrochloride, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Arzoxifene hydrochloride |
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| CAS Number | 182133-27-3 | Molecular Weight | 512.060 |
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| Density | / | Boiling Point | 656.4ºC at 760mmHg |
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| Molecular Formula | C28H30ClNO4S | Melting Point | / |
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| MSDS | / | Flash Point | 350.8ºC |
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Names
| Name | 2-(4-methoxyphenyl)-3-[4-(2-piperidin-1-ylethoxy)phenoxy]-1-benzothiophen-6-ol,hydrochloride |
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| Synonym | More Synonyms |
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Arzoxifene hydrochloride BiologicalActivity
| 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 | Signaling Pathways >>Others >>Estrogen Receptor/ERRResearch Areas >>Cancer |
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| Target | Estrogen receptor[1] |
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| 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]. |
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| 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]. |
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| 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]. |
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| 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]. |
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| 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. |
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Chemical & Physical Properties
| Boiling Point | 656.4ºC at 760mmHg |
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| Molecular Formula | C28H30ClNO4S |
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| Molecular Weight | 512.060 |
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| Flash Point | 350.8ºC |
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| Exact Mass | 511.158417 |
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| PSA | 79.40000 |
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| LogP | 7.67940 |
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| Vapour Pressure | 7.85E-18mmHg at 25°C |
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| InChIKey | NHSNLUIMAQQXGR-UHFFFAOYSA-N |
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| SMILES | COc1ccc(-c2sc3cc(O)ccc3c2Oc2ccc(OCCN3CCCCC3)cc2)cc1.Cl |
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Synonyms
| 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 |
