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[CAS NO. 104121-92-8] Eldecalcitol
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-A0020 |
| Brand: | MCE |
| CAS: | 104121-92-8 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 490.72 |
| Molecular Formula | C30H50O5 |
| 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 |
Summary
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. |
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT05433207 | Chugai Pharmaceutical |
Postmenopausal Osteoporosis
|
August 1, 2022 | |
| NCT05406050 | The Affiliated Hospital of Qingdao University|Wenzhou Haihe Pharmaceutical Co., Ltd. |
Healthy
|
October 20, 2020 | Phase 1 |
| NCT01974167 | e-GLORIA trial Protocol Review Committee |
Osteoporosis
|
December 2013 | Not Applicable |
| NCT00144456 | Chugai Pharmaceutical |
Osteoporosis
|
September 2004 | Phase 3 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
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)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.0378 mL | 10.1891 mL | 20.3782 mL |
| 5 mM | 0.4076 mL | 2.0378 mL | 4.0756 mL |
| 10 mM | 0.2038 mL | 1.0189 mL | 2.0378 mL |
References
- [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.
- [3] Lu Y, et al. Eldecalcitol inhibits the progression of oral cancer by suppressing the expression of GPx-1. Oral Dis. 2021 Aug 24.
- [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.
Synonyms
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