Raloxifene hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

RaloxifeneHcl(LY156758 Hcl)是第二代选择性雌激素受体拮抗剂。

RaloxifeneHcl(LY156758 Hcl) is a second generation selective estrogen receptor antagonist.(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 Ki 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 Ki 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. .

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 Ki values of0.87 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 Ki 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. Cell Viability Assay Cell Line:BJMC3879luc2 cells?Concentration:0 μM, 10 μM, 20 μM, 40 μM, 80 μM Incubation Time:48 hours Result:Reduced BJMC3879luc2 cell viability.

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.. Animal Model:Syngeneic BALB/c mice with BJMC3879luc2 cells Dosage:18 or 27 mg/kg Administration:Subcutaneously implanted mini-osmotic pumps Result:Inhibited tumor growth in mice.

Keoxifene | LY156758

Endocrinology/Hormones

Estrogen Receptor/ERR

ER| AO| SERM

Endocrinology

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82640-04-8

510.04

C28H28ClNO4S

>98% (HPLC)

DMSO: 102 mg/mL (199.98 mM)

[H+].[Cl-].OC1=CC=C(C=C1)C1=C(C(=O)C2=CC=C(OCCN3CCCCC3)C=C2)C2=CC=C(O)C=C2S1

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(-20℃)

With Ice Pack

≥ 2 years