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Raloxifene HCl(LY-139481)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Raloxifene HCl(LY-139481)图片
CAS NO:82640-04-8
规格:≥98%
包装与价格:
包装价格(元)
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
10g电议

产品介绍
Raloxifene HCl (also known as LY-156758; LY-139481; trade names: Evista; Keoxifene; RALOX), the hydrochloride salt of Raloxifene, is a selective estrogen antagonist or estrogen strogen receptor modulator (SERM) that has been approved as a medication to prevent and treat osteoporosis in postmenopausal women. It inhibits human cytosolic aldehyde oxidase-catalyzed phthalazine oxidation activity with an IC50 of 5.7 nM. Raloxifene belongs to the benzothiophene class of estrogen strogen receptor modulator (SERM). Raloxifene binds to estrogen receptors as a mixed estrogen agonist/antagonist; it displays both an ER-α-selective partial agonist/antagonist effect and a pure ER-ss-selective antagonist effect.
理化性质和储存条件
Molecular Weight (MW)510.04
FormulaC28H27NO4S.HCl
CAS No.82640-04-8
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 100 mg/mL (196.1 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)1% methylcellulose: 30mg/mL
SynonymsLY-156758; LY-139481; LY 156758; LY139481; LY156758 (Keoxifene) HCl; LY 139481; trade names: Evista; Keoxifene; RALOX
实验参考方法
In Vitro

In vitro activity: Raloxifene, has been demonstrated as a potent uncompetitive inhibitor of human liver aldehyde oxidase-catalyzed oxidation of phthalazine, vanillin, and nicotine-Delta1'(5')-iminium ion, with Ki values of 0.87 nM, 1.2 nM and 1.4 nM. Raloxifene has also been shown to be a noncompetitive inhibitor of an aldehyde oxidase-catalyzed reduction reaction of a hydroxamic acid-containing compound, with a Ki of 51 nM. Raloxifene activates TGF beta 3 promoter as a full agonist at nanomolar concentrations, and raloxifene inhibits the estrogen response element-containing vitellogenin promoter expression as a pure estrogen antagonist in transient transfection assays.

In VivoRaloxifene restores both bone mineral density and TGF beta 3 messenger RNA expression in the femur to levels measured in intact rats. Raloxifene (0.1 mg/kg-10 mg/kg, orally for 5 weeks) increases bone mineral density in the distal femur and proximal tibia in ovariectomized (OVX) rat. Raloxifene reduces serum cholesteroloral with ED50 of 0.2 mg/kg in ovariectomized (OVX) rat. Raloxifene diverges dramatically from estrogen in its lack of significant estrogenic effects on uterine tissue. Raloxifene prevents cancellous osteopenia as well as the changes in radial bone growth, bone resorption, and blood cholesterol, but is less effective in reducing cancellous bone formation and does not prevent uterine atrophy in ovariectomized (OVX) rats. Raloxifene (3 mg/kg/day) has potent estrogenic activity on bone resorption and serum cholesterol, a lesser effect on bone formation, and minimal activity on uterine wet weight in ovariectomized (OVX) rats.
Animal modelOvariectomized (OVX) rat
Formulation & DosageDissolved in 1.5% carboxymethylcellulose; 10 mg/kg; Oral gavage
References

Drug Metab Dispos. 2004 Jan;32(1):89-97; Endocrinology. 1996 May;137(5):2075-84.