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Purity: ≥98%
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.
| ln Vitro |
At nanomolar concentrations, raloxifene fully agonistically activates the TGF beta 3 promoter. In transient transfection studies, raloxifene acts as a pure estrogen antagonist to suppress the expression of the vitellogenin promoter, which contains the estrogen response element[1]. With Ki values ranging from 0.87 to 1.4 nM, raloxifene is a strong uncompetitive inhibitor of the oxidation of phthalazine, vanillin, and nicotine by human liver aldehyde oxidase[2]. Raloxifene has a Ki value of 51 nM and is also a noncompetitive inhibitor of an aldehyde oxidase-catalyzed reduction process of a molecule containing hydroxamic acid[2]. Raloxifene (0-80 μM; 48 hours) dramatically reduced the viability of mouse mmmary carcinoma BJMC3879luc2 cells in a concentration-dependent manner[5].
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| ln Vivo |
In ovariectomized (OVX) rats, raloxifene (3 mg/kg; once daily) has a limited effect on uterine wet weight and low estrogenic activity on bone resorption and serum cholesterol[3]. In the proximal tibia and distal femur, raloxifene (oral dosage; 0.1 mg/kg–10 mg/kg; 5 weeks) enhances bone mineral density. In ovariectomized (OVX) rats, it lowers serum cholesteroloral with an ED50 of 0.2 mg/kg[4]. Raloxifene (subcutaneously implanted mini-osmotic pumps; 18 or 27 mg/kg; once daily; 6 weeks) dramatically reduces the number of lymph node metastases in addition to dramatically suppressing tumor sizes in mice[5].
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| Cell Assay |
Cell Viability Assay[5]
Cell Types: BJMC3879luc2 cells Tested Concentrations: 0 μM, 10 μM, 20 μM, 40 μM, 80 μM Incubation Duration: 48 hrs (hours) Experimental Results: decreased BJMC3879luc2 cell viability. |
| Animal Protocol |
Animal/Disease Models: Syngeneic balb/c (Bagg ALBino) mouse with BJMC3879luc2 cells[5]
Doses: 18 or 27 mg/kg Route of Administration: subcutaneously (sc) implanted mini-osmotic pumps Experimental Results: Inhibited tumor growth in mice. |
| References |
[1]. 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. 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 in ovariectomized 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 ovariectomized rats. 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.BMC Cancer. 2010 Oct 19;10:566. |
| Molecular Formula |
C28H27NO4S.HCL
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|---|---|
| Molecular Weight |
510.04
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| CAS # |
82640-04-8
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| Related CAS # |
Raloxifene;84449-90-1
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| SMILES |
O=C(C1=C(C2=CC=C(O)C=C2)SC3=CC(O)=CC=C31)C4=CC=C(OCCN5CCCCC5)C=C4.Cl
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| Synonyms |
LY-156758; LY-139481; LY 156758; LY139481; LY156758 (Keoxifene) HCl; LY 139481; trade names: Evista; Keoxifene; RALOX
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9606 mL | 9.8032 mL | 19.6063 mL | |
| 5 mM | 0.3921 mL | 1.9606 mL | 3.9213 mL | |
| 10 mM | 0.1961 mL | 0.9803 mL | 1.9606 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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