Chemical Name |
Arzoxifene hydrochloride |
CAS Number |
182133-27-3 |
MDL Number |
MFCD00954651 |
Molecular Formula |
C28H30ClNO4S |
Molecular Weight |
512.06 |
Synonyms |
LY 353381 HCl; SERM 3 |
Introduction of 182133-27-3 :
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. IC50 & 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].
Purity |
NLT 98% |
Storage |
at 20ºC 2 years |
*The above information is for reference only.