[CAS NO. 104121-92-8] Eldecalcitol

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PRODUCTS SPECIFICATIONS [104121-92-8]

Catalog

HY-A0020

Brand

MCE

CAS

104121-92-8

DESCRIPTION [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

For research use only. We do not sell to patients.

Summary

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 ^[1] ^[2] ^[3] ^[4] .

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

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)

Preparing
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

* Please refer to the solubility information to select the appropriate solvent.

References

Synonyms

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)-

9,10-Secocholesta-5,7,10(19)-triene-1,3,25-triol, 2-(3-hydroxypropoxy)-, (1α,2β,3β,5Z,7E)-

(1R,2R,3R,5Z)-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]-1,3-cyclohexanediol

ED 71

2β-(3-Hydroxypropoxy)-1α,25-dihydroxyvitamin D₃

Eldecalcitol

Edirol

2-(3-Hydroxypropoxy)calcitriol