鹽酸雷洛昔芬作用機制 - Medchemexpress - MCE中國

1、Product Data SheetRaloxifene hydrochlorideCat. No.: HY-13738ACAS No.: 82640-04-8分式: CHClNOS分量: 510.04作靶點: Estrogen Receptor/ERR; Autophagy作通路: Others; Autophagy儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 33.33 mg/mL (65.35 mM; Need ultrasonic)SolventMass1 m

2、g 5 mg 10 mgConcentration制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都請先?/p>

3、照 In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.90 mM); Clear solution此案可獲得 2.5 mg/mL (4.90 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100

4、L 25.0 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (4.90 mM); Clear solution此案可獲得 2.5 mg/mL (4.90 mM，飽和度未知) 的澄清溶液。Page 1 of 2 www.MedChemE以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄均勻。DMSO 儲備液加到

5、900 L 20% 的 SBE-CD 理鹽溶液中，混合3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.90 mM); Clear solution此案可獲得 2.5 mg/mL (4.90 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Raloxifene hydrochloride (LY156758 hydrochloride; LY

6、139481 hydrochloride) 第代選擇性且具有服活性的雌激 素受體 (estrogen receptor) 調(diào)節(jié)劑。Raloxifene hydrochloride 對脂代謝中，發(fā)揮雌激素激動作，在宮內(nèi)膜和乳腺組織中具有雌激素拮抗作。IC & Target IC50: estrogen receptor1體外研究 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.體內(nèi)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.戶使本產(chǎn)品發(fā)表的科研獻 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