Raloxifene HCl

製品コードS1227 バッチS122701

化学情報

	Synonyms	LY156758 (Keoxifene) HCl	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₈H₂₇NO₄S.HCl
	分子量	510.04	CAS No.	82640-04-8
Solubility (25°C)*	体外	DMSO	102 mg/mL (199.98 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Raloxifene (LY156758, Keoxifene) HCl is a selective and orally active estrogen receptor modulator (SERM), which inhibits human cytosolic aldehyde oxidase-catalyzed phthalazine oxidation activity with IC50 of 5.7 nM.
in vitro	Raloxifene, has been demonstrated as a potent uncompetitive inhibitor of human liver aldehyde oxidase-catalyzed oxidation of phthalazine, vanillin, and nicotine-Delta1'(5')-iminium ion, with Ki values of 0.87 nM, 1.2 nM and 1.4 nM. Raloxifene has also been shown to be a noncompetitive inhibitor of an aldehyde oxidase-catalyzed reduction reaction of a hydroxamic acid-containing compound, with a Ki of 51 nM. ^[1] 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. ^[2]
in vivo	Raloxifene restores both bone mineral density and TGF beta 3 messenger RNA expression in the femur to levels measured in intact rats. ^[2] Raloxifene (0.1 mg/kg-10 mg/kg, orally for 5 weeks) increases bone mineral density in the distal femur and proximal tibia in ovariectomized (OVX) rat. Raloxifene reduces serum cholesteroloral with ED50 of 0.2 mg/kg in ovariectomized (OVX) rat. Raloxifene diverges dramatically from estrogen in its lack of significant estrogenic effects on uterine tissue. ^[3] Raloxifene prevents cancellous osteopenia as well as the changes in radial bone growth, bone resorption, and blood cholesterol, but is less effective in reducing cancellous bone formation and does not prevent uterine atrophy in ovariectomized (OVX) rats. ^[4] Raloxifene (3 mg/kg/day) 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. ^[5]
特徴	Raloxifene is as effective as tamoxifen in reducing the incidence of breast cancer in postmenopausal women at increased risk.

プロトコル(参考用のみ)

キナーゼアッセイ	Phthalazine Oxidase Assay
キナーゼアッセイ	Phthalazine is incubated with human liver cytosol (0.05 mg/mL) in a total volume of 0.2 mL of 25 mM KH₂PO4, pH 7.4, containing 0.1 mM EDTA, in the presence and absence of Raloxifene. Raloxifene is added in dimethyl sulfoxide such that the final concentration of solvent is 1% (v/v). Incubations are conducted open to the air for 2.5 min in a water bath set at 37℃. Initial time course experiments establish the linearity of reaction velocity versus protein concentration and incubation time. In preincubation experiments, Raloxifene is incubated with cytosol for 30 min at 37℃ before addition of phthalazine. The incubations are terminated by the addition of 0.05 mL of formic acid (1 M) containing 4-methyl-1-phthalazinone (25 ng) as an internal standard. Terminated incubation mixtures are subjected to filtration through a 0.45-μm mixed cellulose ester 96-well membrane vacuum filtration module into 96-well plates.
動物実験	動物モデル	ovariectomized (OVX) rat
	投薬量	10 mg/kg
	投与方法	Orally

参考

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カスタマーフィードバック

: Data from [J Med Chem, 2014, 57(3), 632-41]

: Data from [Data independently produced by , , Nature, 2018, 560(7718):372-376]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Establishment and Characterization of NCC-PMP1-C1: A Novel Patient-Derived Cell Line of Metastatic Pseudomyxoma Peritonei [ J Pers Med, 2022, 12(2)258]	PubMed: 35207746
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A compendium of kinetic modulatory profiles identifies ferroptosis regulators [ Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4]	PubMed: 33686292
Establishment and characterization of the NCC-GCTB4-C1 cell line: a novel patient-derived cell line from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00639-4]	PubMed: 34731453
Establishment and characterization of novel patient-derived cell lines from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00579-z]	PubMed: 34304386
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Identification of Estrogen Receptor Modulators as Inhibitors of Flavivirus Infection [ Antimicrob Agents Chemother, 2020, 1;AAC.00289-20]	PubMed: 32482672
Estrogen-Related Hormones Induce Apoptosis by Stabilizing Schlafen-12 Protein Turnover. [ Mol Cell, 2019, 75(6):1103-1116.e9]	PubMed: 31420216
Controlling distinct signaling states in cultured cancer cells provides a new platform for drug discovery [ FASEB J, 2019, 10.1096/fj.201802603RR]	PubMed: 31145643
Accumulation of 8,9-unsaturated sterols drives oligodendrocyte formation and remyelination [Hubler Z, et al. Nature, 2018, 560(7718):372-376]	PubMed: 30046109

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