Eldecalcitol

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 326741

CAS#: 104121-92-8

Description: Eldecalcitol is a drug used in Japan for the treatment of osteoporosis. It is an analog of vitamin D. Eldecalcitol is an orally administered drug to patients, which binds to vitamin D receptors and binding protein for the goal of achieving greater specificity to bind calcium for its absorption. This greater affinity is 2.7-fold that of the active vitamin D form of calcitriol. Eldecalcitol is readily absorbed into the body, with a long elimination half-life of over eight hours, reaching maximum absorption in 3.4 hours.


Chemical Structure

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Eldecalcitol
CAS# 104121-92-8

Theoretical Analysis

MedKoo Cat#: 326741
Name: Eldecalcitol
CAS#: 104121-92-8
Chemical Formula: C30H50O5
Exact Mass: 490.37
Molecular Weight: 490.725
Elemental Analysis: C, 73.43; H, 10.27; O, 16.30

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: ED 71; ED-71; ED71; Eldecalcitol; 1,25-dihydroxyvitamin D3; 2-(3-Hydroxypropoxy)calcitriol; Edirol

IUPAC/Chemical Name: (1S,2S,3S,Z)-5-(2-((1R,3aS,7aR,E)-1-((R)-6-hydroxy-6-methylheptan-2-yl)-7a-methyloctahydro-4H-inden-4-ylidene)ethylidene)-2-(3-hydroxypropoxy)-4-methylenecyclohexane-1,3-diol

InChi Key: FZEXGDDBXLBRTD-SJSKTVLPSA-N

InChi Code: InChI=1S/C30H50O5/c1-20(9-6-15-29(3,4)34)24-13-14-25-22(10-7-16-30(24,25)5)11-12-23-19-26(32)28(27(33)21(23)2)35-18-8-17-31/h11-12,20,24-28,31-34H,2,6-10,13-19H2,1,3-5H3/b22-11+,23-12-/t20-,24-,25+,26+,27+,28+,30-/m1/s1

SMILES Code: CC(C)(O)CCC[C@@H](C)[C@H]([C@]1(CCC/2)C)CC[C@@]1([H])C2=C\C=C3C[C@H](O)[C@H](OCCCO)[C@@H](O)C\3=C

Appearance: Solid powder

Purity: >97% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 490.73 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Takada J, Ikeda S, Kusanagi T, Mizuno S, Wada H, Iba K, Yoshizaki T, Yamashita T. Comparison of the effects of eldecalcitol with either raloxifene or bisphosphonate on serum tartrate resistant acid phosphatase-5b, a bone resorption marker, in postmenopausal osteoporosis. Clin Cases Miner Bone Metab. 2016 Jan-Apr;13(1):25-8. doi: 10.11138/ccmbm/2016.13.1.025. Epub 2016 May 11. PubMed PMID: 27252739; PubMed Central PMCID: PMC4869948.

2: Erratum: Treatment of osteoporosis with eldecalcitol, a new vitamin D analog: a comprehensive review and meta-analysis of randomized clinical trials [Corrigendum]. Drug Des Devel Ther. 2016 Feb 15;10:697. doi: 10.2147/DDDT.S105820. eCollection 2016. PubMed PMID: 26929600; PubMed Central PMCID: PMC4760662.

3: Xu Z, Fan C, Zhao X, Tao H. Treatment of osteoporosis with eldecalcitol, a new vitamin D analog: a comprehensive review and meta-analysis of randomized clinical trials. Drug Des Devel Ther. 2016 Jan 28;10:509-17. doi: 10.2147/DDDT.S84264. eCollection 2016. Review. Erratum in: Drug Des Devel Ther. 2016;10:697. PubMed PMID: 26869769; PubMed Central PMCID: PMC4734733.

4: Iba K, Sonoda T, Takada J, Dohke T, Yamashita T. Further significant effects of eldecalcitol on bone resorption markers and bone mineral density in postmenopausal osteoporosis patients having undergone long-term bisphosphonate treatment. J Bone Miner Metab. 2016 Jan 30. [Epub ahead of print] PubMed PMID: 26832388.

5: Mukaiyama K, Uchiyama S, Nakamura Y, Ikegami S, Taguchi A, Kamimura M, Kato H. Eldecalcitol, in Combination with Bisphosphonate, Is Effective for Treatment of Japanese Osteoporotic Patients. Tohoku J Exp Med. 2015;237(4):339-43. doi: 10.1620/tjem.237.339. PubMed PMID: 26639092.

6: Serizawa K, Yogo K, Tashiro Y, Takeda S, Kawasaki R, Aizawa K, Endo K. Eldecalcitol prevents endothelial dysfunction in postmenopausal osteoporosis model rats. J Endocrinol. 2016 Feb;228(2):75-84. doi: 10.1530/JOE-15-0332. Epub 2015 Nov 4. PubMed PMID: 26537128.

7: Shintani T, Rosli SN, Takatsu F, Choon YF, Hayashido Y, Toratani S, Usui E, Okamoto T. Eldecalcitol (ED-71), an analog of 1α,25-dihydroxyvitamin D3 as a potential anti-cancer agent for oral squamous cell carcinomas. J Steroid Biochem Mol Biol. 2015 Oct 9. pii: S0960-0760(15)30102-3. doi: 10.1016/j.jsbmb.2015.09.043. [Epub ahead of print] Review. PubMed PMID: 26444325.

8: Saito M, Marumo K. [Bone Cell Biology Assessed by Microscopic Approach. The effects of active vitamin D3 such as alfacalcidol and eldecalcitol on bone quality]. Clin Calcium. 2015 Oct;25(10):1541-54. doi: CliCa151015411554. Japanese. PubMed PMID: 26412735.

9: Ebina K, Noguchi T, Hirao M, Kaneshiro S, Tsukamoto Y, Yoshikawa H. Comparison of the effects of 12 months of monthly minodronate monotherapy and monthly minodronate combination therapy with vitamin K2 or eldecalcitol in patients with primary osteoporosis. J Bone Miner Metab. 2016 May;34(3):243-50. doi: 10.1007/s00774-015-0710-2. Epub 2015 Aug 25. Review. PubMed PMID: 26303222.

10: Sakai S, Takeda S, Sugimoto M, Shimizu M, Shimonaka Y, Yogo K, Hashimoto J, Bauss F, Endo K. Treatment with the combination of ibandronate plus eldecalcitol has a synergistic effect on inhibition of bone resorption without suppressing bone formation in ovariectomized rats. Bone. 2015 Dec;81:449-58. doi: 10.1016/j.bone.2015.08.004. Epub 2015 Aug 15. PubMed PMID: 26281770.

11: Saito K, Miyakoshi N, Matsunaga T, Hongo M, Kasukawa Y, Shimada Y. Eldecalcitol improves muscle strength and dynamic balance in postmenopausal women with osteoporosis: an open-label randomized controlled study. J Bone Miner Metab. 2015 Jul 25. [Epub ahead of print] PubMed PMID: 26209166.

12: Yamasaki Y, Nagira K, Osaki M, Nagashima H, Hagino H. Effects of eldecalcitol on cortical bone response to mechanical loading in rats. BMC Musculoskelet Disord. 2015 Jun 30;16:158. doi: 10.1186/s12891-015-0613-3. PubMed PMID: 26123128; PubMed Central PMCID: PMC4484892.

13: Yasuda K, Iwanaga Y, Ogawa K, Mano H, Ueno S, Kimoto S, Ohta M, Kamakura M, Ikushiro S, Sakaki T. Human hepatic metabolism of the anti-osteoporosis drug eldecalcitol involves sterol C4-methyl oxidase. Pharmacol Res Perspect. 2015 Mar;3(2):e00120. doi: 10.1002/prp2.120. Epub 2015 Feb 10. PubMed PMID: 26038696; PubMed Central PMCID: PMC4448988.

14: Kinoshita H, Miyakoshi N, Kasukawa Y, Sakai S, Shiraishi A, Segawa T, Ohuchi K, Fujii M, Sato C, Shimada Y. Effects of eldecalcitol on bone and skeletal muscles in glucocorticoid-treated rats. J Bone Miner Metab. 2016 Mar;34(2):171-8. doi: 10.1007/s00774-015-0664-4. Epub 2015 May 6. PubMed PMID: 25944421.

15: Takeuchi Y. [Current Topics on Vitamin D. Treatment of osteoporosis with eldecalcitol: Its therapeutic efficacy and adverse effect on renal function]. Clin Calcium. 2015 Mar;25(3):425-32. doi: CliCa1503425432. Review. Japanese. PubMed PMID: 25716816.

16: Sakai A, Ito M, Tomomitsu T, Tsurukami H, Ikeda S, Fukuda F, Mizunuma H, Inoue T, Saito H, Nakamura T; e-ADVANCED Study Group. Erratum to: efficacy of combined treatment with alendronate (ALN) and eldecalcitol, a new active vitamin D analog, compared to that of concomitant ALN, vitamin D plus calcium treatment in Japanese patients with primary osteoporosis. Osteoporos Int. 2015 Apr;26(4):1453. doi: 10.1007/s00198-015-3049-6. PubMed PMID: 25656519; PubMed Central PMCID: PMC4643555.

17: Kondo S, Takano T, Ono Y, Saito H, Matsumoto T. Eldecalcitol reduces osteoporotic fractures by unique mechanisms. J Steroid Biochem Mol Biol. 2015 Apr;148:232-8. doi: 10.1016/j.jsbmb.2015.01.016. Epub 2015 Jan 24. PubMed PMID: 25625663.

18: Sakai A, Ito M, Tomomitsu T, Tsurukami H, Ikeda S, Fukuda F, Mizunuma H, Inoue T, Saito H, Nakamura T; e-ADVANCED Study Group. Efficacy of combined treatment with alendronate (ALN) and eldecalcitol, a new active vitamin D analog, compared to that of concomitant ALN, vitamin D plus calcium treatment in Japanese patients with primary osteoporosis. Osteoporos Int. 2015 Mar;26(3):1193-202. doi: 10.1007/s00198-014-2991-z. Epub 2015 Jan 16. Erratum in: Osteoporos Int. 2015 Apr;26(4):1453. PubMed PMID: 25592133; PubMed Central PMCID: PMC4331603.

19: Saito M, Grynpas MD, Burr DB, Allen MR, Smith SY, Doyle N, Amizuka N, Hasegawa T, Kida Y, Marumo K, Saito H. Treatment with eldecalcitol positively affects mineralization, microdamage, and collagen crosslinks in primate bone. Bone. 2015 Apr;73:8-15. doi: 10.1016/j.bone.2014.11.025. Epub 2014 Dec 5. PubMed PMID: 25482210.

20: Takeda S, Smith SY, Tamura T, Saito H, Takahashi F, Samadfam R, Haile S, Doyle N, Endo K. Long-term treatment with eldecalcitol (1α, 25-dihydroxy-2β- (3-hydroxypropyloxy) vitamin D3) suppresses bone turnover and leads to prevention of bone loss and bone fragility in ovariectomized rats. Calcif Tissue Int. 2015 Jan;96(1):45-55. doi: 10.1007/s00223-014-9937-5. Epub 2014 Dec 4. PubMed PMID: 25467010.