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Eldecalcitol
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。
Eldecalcitol图片
CAS NO:104121-92-8
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品名称
艾地骨化醇
ED-71
2-(3-hydroxypropoxy)-1,25-dihydroxyvitamin D3
产品介绍
Eldecalcitol (ED-71) 是一种具有口服活性维生素 D3 类似物,可抑制骨吸收并增加骨密度。Eldecalcitol 具有抗肿瘤作用,抑制细胞增殖、迁移,并通过抑制 GPx-1 来诱导细胞凋亡 (apoptosis)。
生物活性

Eldecalcitol (ED-71) is an orally active vitamin D3 analogue, inhibits bone resorption and increases bone mineral density. Eldecalcitol (ED-71) displays anti-tumor effect and inhibits cell proliferation, migration and inducesapoptosisby suppressing GPx-1[1][2][3][4].

体外研究
(In Vitro)

Eldecalcitol (0-50 nM; 24 h) displays no cytotoxicity, and (0.5-50 nM; 24 h) reduces cell death induced by LPS (5 μg/mL)[2].
Eldecalcitol (5 nM; 24 h) inhibits the LPS-induced pyroptosis by activating Nrf2 and its effector molecule HO-1[2].
Eldecalcitol (0.5-50 nM; 24 h) exhibits anti-pyroptotic ability, and decreases NLRP3, caspase-1, and IL-1β expression dose-dependently[3].
Eldecalcitol (0.04-40 nM; 0-48 h) inhibits the proliferation and migration of SCC-15 and CAL-27 cells[3].
Eldecalcitol (0.4 nM; 48 h) arrests cell cycle at G0/G1 phase and induces apoptosis by suppressing the expression of GPx-1 (glutathione peroxidase) in OSCC cells[3].

Western Blot Analysis[2]

Cell Line:Human gingival fibroblasts (HGFs)
Concentration:0, 0.5, 5, and 50 nM
Incubation Time:24 hours
Result:Decreased TLR4, NLRP3, caspase-1 p20, ASC, and GSDMD-N level in a dose-dependent manner compared with the group treated with LPS.
Reduced the release of IL-1β and IL-18 induced by LPS to normal levels.

Cell Proliferation Assay[3]

Cell Line:SCC-15 and CAL-27 cells
Concentration:0, 0.04, 0.4, 4, and 40 nM
Incubation Time:6, 8, 12, 24, 48 hours
Result:Inhibited the cell viability of the OSCC cells to reach 50% at 24 h with 0.4 nM.

Cell Proliferation Assay[3]

Cell Line:OSCC cells
Concentration:0.4 nM
Incubation Time:48 hours
Result:Increased the proportion of cells at the late phases of apoptosis from 7.1% to 16.1%.
Upregulated Bax and caspase-3, downregulated Bcl-2.
Significantly triggered apoptosis in SCC- 15 and CAL- 27 cells.
体内研究
(In Vivo)

Eldecalcitol (0.5 μg/kg; p.o.; twice a week for 4 weeks) displays anti-cancer effect by GPx-1 (glutathione peroxidase) inhibition[3].
Eldecalcitol (10, 30, or 90 ng/kg; p.o.; 5-times per week for 12 weeks), as a more potent vitamin D3 analog, stimulates focal bone formation (minimodeling) and suppresses bone resorption more strongly than does calcitriol[4].

Animal Model:Xenograft tumor model in mice (male athymic nude BALB/c mice)[3]
Dosage:0.5 μg/kg
Administration:Oral gavage; twice a week for 4 weeks
Result:Reduced the growth rate of tumors, and downregulated the expression levels of PCNA and MMP- 2 and upregulated the expression of Bax in the tumors.
Resulted in decrease of proliferation, the inhibition of migration, and the promotion of apoptosis.
Animal Model:Ovariectomized (OVX) rat model[4]
Dosage:10, 30, or 90 ng/kg
Administration:Oral gavage; 5-times per week for 12 weeks
Result:Increased the lumbar and femoral BMD in a dose dependent manner. Stimulated focal bone formation that started without prior bone resorption, a process known as bone minimodeling.
Clinical Trial
分子量

490.72

性状

Solid

Formula

C30H50O5

CAS 号

104121-92-8

中文名称

艾尔骨化醇;艾地骨化醇

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据
In Vitro: 

Methanol : 8.33 mg/mL(16.98 mM;Need ultrasonic)

DMSO : 3.33 mg/mL(6.79 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 mM2.0378 mL10.1891 mL20.3782 mL
5 mM0.4076 mL2.0378 mL4.0756 mL
10 mM0.2038 mL1.0189 mL2.0378 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 (protect from light, stored under nitrogen)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。