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Raloxifene hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Raloxifene hydrochloride图片
CAS NO:82640-04-8
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
盐酸雷洛昔芬
Keoxifene hydrochloride
LY156758
LY139481 hydrochloride
产品介绍
Raloxifene hydrochloride (Keoxifene hydrochloride) 是第二代选择性且具有口服活性的雌激素受体 (estrogen receptor) 调节剂。Raloxifene hydrochloride 对骨脂代谢中,发挥雌激素激动作用,在子宫内膜和乳腺组织中具有雌激素拮抗作用。
生物活性

Raloxifene hydrochloride (Keoxifene hydrochloride) is a second generation selective and orally activeestrogen receptormodulator. Raloxifene hydrochloride produces estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue[1].

IC50& Target

IC50: estrogen receptor[1]

体外研究
(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[1].
Raloxifene is a potent uncompetitive inhibitor of human liver aldehyde oxidase-catalyzed oxidation of phthalazine, vanillin, and nicotine-Delta1'(5')-iminium ion, exhibits Kivalues of 0.87 to 1.4 nM[2].
Raloxifene is also a noncompetitive inhibitor of an aldehyde oxidase-catalyzed reduction reaction of a hydroxamic acid-containing compound, with a Kivalue of 51 nM[2].
Raloxifene (0-80 μM; 48 hours) significantly decreased in mouse mammary carcinoma BJMC3879luc2 cells viability as a concentration manner in BJMC3879luc2 cells[5].

Cell Viability Assay[5]

Cell Line:BJMC3879luc2 cells
Concentration:0 μM, 10 μM, 20 μM, 40 μM, 80 μM
Incubation Time:48 hours
Result:Reduced BJMC3879luc2 cell viability.
体内研究
(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[3].
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 ED50of 0.2 mg/kg in ovariectomized (OVX) rat[4].
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[5].
.

Animal Model:Syngeneic BALB/c mice with BJMC3879luc2 cells[5]
Dosage:18 or 27 mg/kg
Administration:Subcutaneously implanted mini-osmotic pumps
Result:Inhibited tumor growth in mice.
Clinical Trial
分子量

510.04

性状

Solid

Formula

C28H28ClNO4S

CAS 号

82640-04-8

中文名称

盐酸雷洛昔芬

结构分类
  • Alkaloids
  • Piperidine Alkaloids
  • Phenols
  • Polyphenols
来源
  • Plants
  • Rutaceae
  • Tetradium ruticarpum(A. Jussieu) T. G. Hartley
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 33.33 mg/mL(65.35 mM;Need ultrasonic)

H2O : 1 mg/mL(1.96 mM;ultrasonic and warming and heat to 60℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.9606 mL9.8032 mL19.6063 mL
5 mM0.3921 mL1.9606 mL3.9213 mL
10 mM0.1961 mL0.9803 mL1.9606 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;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方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,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.90 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.90 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.90 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。