Eldecalcitol
Based on 5 publication(s) in Google Scholar
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.
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- 純度: 99.91%
- CAS 番号: 104121-92-8
- 分子式: C30H50O5
- 分子量:490.72
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保管条件:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
MedChemExpress(MCE)の使用を引用している文献 Eldecalcitol
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生物活性
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human gingival fibroblasts (HGFs)
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Concentration:0, 0.5, 5, and 50 nM
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Incubation Time:24 hours
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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.
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Cell Line:SCC-15 and CAL-27 cells
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Concentration:0, 0.04, 0.4, 4, and 40 nM
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Incubation Time:6, 8, 12, 24, 48 hours
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Result:Inhibited the cell viability of the OSCC cells to reach 50% at 24 h with 0.4 nM.
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Cell Line:OSCC cells
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Concentration:0.4 nM
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Incubation Time:48 hours
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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.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Xenograft tumor model in mice (male athymic nude BALB/c mice)[3]
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Dosage:0.5 μg/kg
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Administration:Oral gavage; twice a week for 4 weeks
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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.
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Animal Model:Ovariectomized (OVX) rat model[4]
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Dosage:10, 30, or 90 ng/kg
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Administration:Oral gavage; 5-times per week for 12 weeks
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 104121-92-8
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性状 Solid
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分子量 490.72
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分子式 C30H50O5
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Color White to off-white
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SMILES
O[C@H]1[C@@H](OCCCO)[C@H](O)C(/C(C1)=C\C=C2[C@]3([H])CC[C@H]([C@H](C)CCCC(C)(O)C)[C@@]3(C)CCC\2)=C
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別名
ED-71; 2-(3-hydroxypropoxy)-1,25-dihydroxyvitamin D3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Publications (5)
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Journal Impact Factor
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Most Recent
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Cell Prolif
Glutaminase-1 Mediated Glutaminolysis to Glutathione Synthesis Maintains Redox Homeostasis and Modulates Ferroptosis Sensitivity in Cancer Cells. [Abstract]2025 Apr 21:e70036. PMID: 40259435 -
Eur J Pharmacol
ED-71 ameliorates bone regeneration in type 2 diabetes by reducing ferroptosis in osteoblasts via the HIF1α pathway. [Abstract]2024 Apr 15:969:176303. PMID: 38211715 -
Virol Sin
Antiviral activity of vitamin D derivatives against severe fever with thrombocytopenia syndrome virus in vitro and in vivo. [Abstract]2024 Aug 19:S1995-820X(24)00134-2. PMID: 39168248 -
Bone
Sympathetic overactivity-induced type H endothelial cell senescence contributes to the impairment of vascularized osteogenesis by PKM2-mediated glycolysis in preclinical stages of Alzheimer's mice. [Abstract]2026 Jun:207:117859. PMID: 41833832 -
Tissue Cell
Eldecalcitol enhances osteo/odontogenic differentiation and mineralized matrix formation via redox modulation in human dental pulp stem cells. [Abstract]2026 May 2:102:103565. PMID: 42096965
溶剤 & 溶解度
DMSO : 3.33 mg/mL (6.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (280 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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取扱説明書 (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[3]. Lu Y, et al. Eldecalcitol inhibits the progression of oral cancer by suppressing the expression of GPx-1. Oral Dis. 2021 Aug 24. [Content Brief]
[4]. Saito H, et al. Eldecalcitol and calcitriol stimulates 'bone minimodeling,' focal bone formation without prior bone resorption, in rat trabecular bone. J Steroid Biochem Mol Biol. 2013 Jul;136:178-82. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0378 mL | 10.1891 mL | 20.3782 mL | 50.9455 mL |
| 5 mM | 0.4076 mL | 2.0378 mL | 4.0756 mL | 10.1891 mL |
- Eldecalcitol
- 104121-92-8
- ED-71
- 2-(3-hydroxypropoxy)-1,25-dihydroxyvitamin D3
- ED71
- ED 71
- VD/VDR
- Apoptosis
- bone
- resorption
- mineral
- density
- periodontitis
- NLRP3 inflammasome
- human gingival fibroblasts
- HGFs
- LPS-induced
- pyroptosis
- Nrf2/HO-1
- osteoporosis
- anti-tumor
- proliferation
- migration
- GPx-1
- arrest cell cycle
- Inhibitor
- inhibitor
- inhibit