Eldecalcitol|104121-92-8|(艾地骨化醇; ED-71; 2-(3-hydroxypropoxy)-1,25-dihydroxyvitamin D3)-陌孚医药/Medlife

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Eldecalcitol (Synonyms: 艾地骨化醇; ED-71; 2-(3-hydroxypropoxy)-1,25-dihydroxyvitamin D3)

目录号: PL12564 纯度: ≥99%

CAS No. :104121-92-8

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中文名称	Eldecalcitol
中文别名	1α,25-二羟基-2β-(3-羟基丙氧基)维生素D3;2-(3-羟基丙氧基)-1,25-二羟基维他命 D3;艾地骨化醇;艾尔骨化醇;2-(3-羟基丙氧基)-1,25-二羟基维他命 D3, ED71
英文名称	Eldecalcitol
英文别名	1,3-Cyclohexanediol,2-(3-hydroxypropoxy)-4-methylene-5-[(2E)-2-[(1R,3aS,7aR)-octahydro-1-[(1R)-5-hydroxy-1,5-dimethylhexyl]-7a-methyl-4H-inden-4-ylidene]ethylidene]-,(1R,2R,3R,5Z)-;Eldecalcitol;(1S,2S,3S,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(2R)-6-hydroxy-6-methylheptan-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-2-(3-hydroxypropoxy)-4-methylidenecyclohexane-1,3-diol;1,3-Cyclohexanediol,2-(3-hydroxypropoxy)-4-methylene-5-[(2E)-2-[(1R,3aS,7aR)-octahydro-1-[(1R)-5-hydroxy-1,5-dimethylhexyl]-7;1α,25-dihydroxy-2β-(3-hydroxypropoxy)Vitamin D3;2.beta.-(3-Hydroxypropoxy)-1.alpha.,25-dihydroxyvitamin D3;CS-0363;ED 71;ED-71;HY-A0020;UNII-I2JP8UE90H;2-(3-Hydroxypropoxy)-1,25-dihydroxyvitamin D3;Eldecalcitol(ED-71);1alpha,25-dihydroxy-2beta-(3-hydroxypropoxy)vitamin D3;(1R,Z)-5-((E)-2-((1R,7aR)-1-((R)-6-hydroxy-6-methylheptan-2-yl)-7a-methylhexahydro-1H-inden-4(2H)-ylidene)ethylidene)-2-(3-hydroxypropoxy)-4-methylenecyclohexane-1,3-diol;Edirol;I2JP8UE90H;(1R,2R,3R,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(2R)-6-hydroxy-6-methylheptan-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-2-(3-hydroxypropoxy)-4-methylidenecyclohexane-1,3-diol;1alpha,25-dihydroxy-2beta-(3-hydroxypropoxy
Cas No.	104121-92-8
分子式	C₃₀H₅₀O₅
分子量	490.72
包装储存	4°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

产品详情

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 induces apoptosis by suppressing GPx-1.

性状

Solid

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).
Eldecalcitol (5 nM; 24 h) inhibits the LPS-induced pyroptosis by activating Nrf2 and its effector molecule HO-1.
Eldecalcitol (0.5-50 nM; 24 h) exhibits anti-pyroptotic ability, and decreases NLRP3, caspase-1, and IL-1β expression dose-dependently.
Eldecalcitol (0.04-40 nM; 0-48 h) inhibits the proliferation and migration of SCC-15 and CAL-27 cells.
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.
has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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.
has not independently confirmed the accuracy of these methods. They are for reference only.

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)

ClinicalTrial

参考文献

[1]. Matsumoto T.Osteoporosis Treatment by a New Active Vitamin D3 Compound, Eldecalcitol, in Japan.Curr Osteoporos Rep. 2012 Aug 24.
[2]. Huang C, et al. Eldecalcitol Inhibits LPS-Induced NLRP3 Inflammasome-Dependent Pyroptosis in Human Gingival Fibroblasts by Activating the Nrf2/HO-1 Signaling Pathway. Drug Des Devel Ther. 2020 Nov 13;14:4901-4913.

溶解度数据	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°C)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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