盐酸雷洛昔芬作用机制 - Medchemexpress - MCE中国

1、Product Data SheetRaloxifene hydrochlorideCat. No.: HY-13738ACAS No.: 82640-04-8分式: CHClNOS分量: 510.04作靶点: Estrogen Receptor/ERR; Autophagy作通路: Others; Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 33.33 mg/mL (65.35 mM; Need ultrasonic)SolventMass1 m

2、g 5 mg 10 mgConcentration制备储备液1 mM 1.9606 mL 9.8032 mL 19.6063 mL5 mM 0.3921 mL 1.9606 mL 3.9213 mL10 mM 0.1961 mL 0.9803 mL 1.9606 mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按

3、照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.90 mM); Clear solution此案可获得 2.5 mg/mL (4.90 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100

4、L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (4.90 mM); Clear solution此案可获得 2.5 mg/mL (4.90 mM，饱和度未知) 的澄清溶液。Page 1 of 2 www.MedChemE以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄均匀。DMSO 储备液加到

5、900 L 20% 的 SBE-CD 理盐溶液中，混合3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.90 mM); Clear solution此案可获得 2.5 mg/mL (4.90 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Raloxifene hydrochloride (LY156758 hydrochloride; LY

6、139481 hydrochloride) 第代选择性且具有服活性的雌激 素受体 (estrogen receptor) 调节剂。Raloxifene hydrochloride 对脂代谢中，发挥雌激素激动作，在宫内膜和乳腺组织中具有雌激素拮抗作。IC & Target IC50: estrogen receptor1体外研究 Raloxifene activates TGF beta 3 promoter as a full agonist at nanomolar concentrations, and raloxifene inhibits theestrogen response el

7、ement-containing vitellogenin promoter expression as a pure estrogen antagonist in transienttransfection assays1.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

8、to 1.4 nM2.Raloxifene is also a noncompetitive inhibitor of an aldehyde oxidase-catalyzed reduction reaction of a hydroxamicacid-containing compound, with a Ki value of 51 nM2.Raloxifene (0-80 M; 48 hours) significantly decreased in mouse mammary carcinoma BJMC3879luc2 cells viability asa concentrat

9、ion manner in BJMC3879luc2 cells5.Cell Viability Assay5Cell Line: BJMC3879luc2 cellsConcentration: 0 M, 10 M, 20 M, 40 M, 80 MIncubation Time: 48 hoursResult: Reduced BJMC3879luc2 cell viability.体内研究Raloxifene (3 mg/kg; once daily) has potent estrogenic activity on bone resorption and serum choleste

10、rol, a lessereffect on bone formation, and minimal activity on uterine wet weight in ovariectomized (OVX) ximal tibia. It reduces serum cholesteroloral with ED50 of 0.2 mg/kg in ovariectomized (OVX) rat4.Raloxifene (subcutaneously implanted mini-osmotic pumps; 18 or 27 mg/kg; once daily; 6

11、weeks) significantlysuppresses tumor volumes in mice, in addition, the multiplicity of lymph node metastasis is also significantlydecreased5.Raloxifene (oral administration; 0.1 mg/kg-10 mg/kg; 5 weeks) increases bone mineral density in the distal femur andAnimal Model: Syngeneic BALB/c mice with BJ

12、MC3879luc2 cells5Dosage: 18 or 27 mg/kgAdministration: Subcutaneously implanted mini-osmotic pumpsPage 2 of 3 www.MedChemEResult: Inhibited tumor growth in mice.户使本产品发表的科研献 Free Radic Biol Med. 2017 Apr 10;108:404-417. PLoS Negl Trop Dis. 2019 Aug 20;13(8):e0007681. Med Sci Monit. 2019 Apr 29;25:314

13、6-3153.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Yang, N.N., et al., Estrogen and raloxifene stimulate transforming growth factor-beta 3 gene expression in rat bone: a potential mechanism for estrogen-or raloxifene-mediated bone maintenance. Endocrinology, 1996

14、. 137(5): p. 2075-84.2. Obach, R.S., Potent inhibition of human liver aldehyde oxidase by raloxifene. Drug Metab Dispos, 2004. 32(1): p. 89-97.3. Sato, M., M.K. Rippy, and H.U. Bryant, Raloxifene, tamoxifen, nafoxidine, or estrogen effects on reproductive and nonreproductive tissues inovariectomized

15、 rats. FASEB J, 1996. 10(8): p. 905-12.4. Black, L.J., et al., Raloxifene (LY139481 HCI) prevents bone loss and reduces serum cholesterol without causing uterine hypertrophy in ovariectomizedrats. J Clin Invest, 1994. 93(1): p. 63-9.5. Shibata MA, et al. Raloxifene inhibits tumor growth and lymph node metastasis in a xenograft model of metastatic mammary cancer.BMCCancer. 2010Oct 19