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Raloxifene hydrochloride

CAS No. : 82640-04-8

MCE 站：Raloxifene hydrochloride

产品活性：Raloxifene hydrochloride (Keoxifene hydrochloride) 是第二代选择性且具有口服活性的雌激素受体 (estrogen receptor) 调节剂。Raloxifene hydrochloride 对骨脂代谢中，发挥雌激素激动作用，在子宫内膜和乳腺组织中具有雌激素拮抗作用。

研究领域：Others  |  Autophagy

作用靶点：Estrogen Receptor/ERR  |  Autophagy

In Vitro: 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.
Raloxifene is a potent uncompetitive inhibitor of human liver aldehyde oxidase-catalyzed oxidation of phthalazine, vanillin, and nicotine-Delta1'(5')-iminium ion, exhibits K_i values of 0.87 to 1.4 nM.
Raloxifene is also a noncompetitive inhibitor of an aldehyde oxidase-catalyzed reduction reaction of a hydroxamic acid-containing compound, with a K_i value of 51 nM.
Raloxifene (0-80 μM; 48 hours) significantly decreased in mouse mammary carcinoma BJMC3879luc2 cells viability as a concentration manner in BJMC3879luc2 cells.

In Vivo: Raloxifene (3 mg/kg; once daily) 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.
Raloxifene (oral administration; 0.1 mg/kg-10 mg/kg; 5 weeks) increases bone mineral density in the distal femur and proximal tibia. It reduces serum cholesteroloral with ED₅₀ of 0.2 mg/kg in ovariectomized (OVX) rat.
Raloxifene (subcutaneously implanted mini-osmotic pumps; 18 or 27 mg/kg; once daily; 6 weeks) significantly suppresses tumor volumes in mice, in addition, the multiplicity of lymph node metastasis is also significantly decreased.
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