Eldecalcitol
(Synonyms: 艾地骨化醇; ED-71; 2-(3-hydroxypropoxy)-1,25-dihydroxyvitamin D3) 目录号 : GC35971
Eldecalcitol (ED-71) 是1,25-二羟基维生素D3的类似物。
Cas No.:104121-92-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Eldecalcitol (ED-71) is an analog of 1,25-dihydroxyvitamin D3 that improves bone mineral density. IC50 value:Target: Vd analogEldecalcitol (ED-71) is more efficacious than alfacalcidol in preventing vertebral and wrist fractures in osteoporotic patients with vitamin D sufficiency, with a safety profile similar to alfacalcidol.
[1]. Matsumoto T.Osteoporosis Treatment by a New Active Vitamin D3 Compound, Eldecalcitol, in Japan.Curr Osteoporos Rep. 2012 Aug 24. [2]. Shiraki M, et al. Eldecalcitol normalizes bone turnover markers regardless of their pre-treatment levels.Curr Med Res Opin. 2012 Aug 23. [3]. Matsumoto T, Endo I.Eldecalcitol for the treatment of osteoporosis.Drugs Today (Barc). 2012 Mar;48(3):189-96. [4]. Sakai S, et al.Combination therapy with eldecalcitol and alendronate has therapeutic advantages over monotherapy by improving bone strength.Bone. 2012 May;50(5):1054-63. Epub 2012 Feb 17. [5]. Sanford M, McCormack PL.Spotlight on eldecalcitol in osteoporosis.Drugs Aging. 2012 Jan 1;29(1):69-71.
| Cas No. | 104121-92-8 | SDF | |
| 别名 | 艾地骨化醇; ED-71; 2-(3-hydroxypropoxy)-1,25-dihydroxyvitamin D3 | ||
| Canonical 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 | ||
| 分子式 | C30H50O5 | 分子量 | 490.72 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Eldecalcitol for the treatment of osteoporosis
Drugs Today (Barc) 2012 Mar;48(3):189-96.PMID:22462038DOI:10.1358/dot.2012.48.3.1745223.
Eldecalcitol [1α,25-dihydroxy-2β-(3-hydroxypropyloxy)-vitamin D₃] is an analogue of 1α,25-dihydroxyvitamin D₃ [1,25(OH)₂D₃], bearing a hydroxypropyloxy residue at the 2β position. Eldecalcitol shows stronger effects than alfacalcidol to increase bone mineral density and reduce bone resorption markers in osteoporotic patients, and oral once-daily 0.75 μg Eldecalcitol reduced vertebral fracture incidence by 26% compared to 1.0 μg alfacalcidol in a 3-year randomized, double-blind, active-comparator clinical trial. The effect of Eldecalcitol on vertebral fracture incidence was sustained throughout the 3-year study period, and the annual incidence of vertebral fracture during the third year was significantly lower with Eldecalcitol rather than with alfacalcidol treatment (3.9% vs 7.0%, respectively). Eldecalcitol also reduced the incidence of wrist fractures by 71% compared to alfacalcidol. Eldecalcitol is well tolerated and is not associated with serious side effects including sustained hypercalcemia. Eldecalcitol was approved for the treatment of osteoporosis in Japan in 2011.
Eldecalcitol for the treatment of osteoporosis
Clin Interv Aging 2013;8:1313-21.PMID:24101867DOI:10.2147/CIA.S49825.
Eldecalcitol (1α, 25-dihydroxy-2β-[3-hydroxypropyloxy] vitamin D3; ED-71) is a new analog of the active form of vitamin D. Eldecalcitol has recently been approved for the treatment of osteoporosis in Japan. In addition to regulation of calcium metabolism carried out by conventional vitamin D analogs, Eldecalcitol possesses a strong inhibitory effect on bone resorption and causes a significant increase in bone mineral density. A Phase III clinical trial on osteoporosis showed that Eldecalcitol reduced the incidence of new vertebral fractures over 3 years by 26% compared with alfacalcidol. Although the overall risk of nonvertebral fractures was not reduced by Eldecalcitol, the risk of wrist fracture was decreased significantly in the Eldecalcitol group (71%) compared with the alfacalcidol group. The serum level of 25-hydroxyvitamin D (25[OH]D) was normalized by supplementation of native vitamin D in this trial, so the desirable effects on bone by Eldecalcitol were considered to be derived from its distinctive pharmacological action. Increased blood calcium was observed in 21% of patients treated with Eldecalcitol, and hypercalcemia (>11.5 mg/dL) occurred in 0.4% of Eldecalcitol recipients, so serum calcium concentration should be monitored after starting Eldecalcitol treatment. Eldecalcitol has dual effects on the metabolism of bone and calcium and is useful for the treatment of osteoporosis, especially for elderly patients (who frequently suffer from vitamin D deficiency). This article reviews the clinical efficacy and safety of Eldecalcitol in the treatment of osteoporosis.
Eldecalcitol: a review of its use in the treatment of osteoporosis
Drugs 2011 Sep 10;71(13):1755-70.PMID:21902297DOI:10.2165/11206790-000000000-00000.
Eldecalcitol (1α,25[OH](2)-2β-(3-hydroxypropyloxy)vitamin D(3); ED-71; Edirol®) is an orally administered analogue of active vitamin D (calcitriol) that is available in Japan for the treatment of osteoporosis. Two randomized, double-blind, multicentre trials were conducted in patients with osteoporosis. In a placebo-controlled, dose-ranging trial, Eldecalcitol significantly reduced serum bone-specific alkaline phosphatase (BALP) and serum osteocalcin, markers of bone formation, more than placebo. Eldecalcitol at a 1.0 μg/day dosage, but not at lower dosages, also significantly reduced urinary type I collagen N-telopeptide (NTX), a marker of bone resorption, more than placebo. In a comparison with alfacalcidol (a prodrug of calcitriol), Eldecalcitol produced significantly greater reductions in serum BALP and urinary NTX, and had a positive effect on CT markers of femoral biomechanical properties. In the comparison with alfacalcidol, Eldecalcitol 0.75 μg/day significantly reduced the 3-year incidence of vertebral fractures, with an absolute risk reduction of 4.1% over this period, representing a relative risk reduction of 26%. There was no significant difference in the rate of non-vertebral fractures. In both trials, Eldecalcitol treatment was also associated with an increase in bone mineral density, whereas patients who received the comparators generally had a reduction in bone mineral density. Increases in blood calcium (to >2.6 mmol/L) and urinary calcium (to >0.1 mmol/L glomerular filtrate) were the most clinically important treatment-emergent adverse events. In the placebo-controlled, dose-ranging trial, 23% and 25% of patients in the Eldecalcitol 1 μg/day group had increased blood and urinary calcium compared with 7% and 7%, 6% [corrected] and 9%, and 0% and 1.9% in the Eldecalcitol 0.5 and 0.75 μg/day, and placebo groups, respectively. In the comparison with alfacalcidol, 21.0% and 13.5% of Eldecalcitol 0.75 μg/day and alfacalcidol 1.0 μg/day recipients had increased blood calcium, whereas hypercalcaemia (defined as a serum calcium >2.9 mmol/L) occurred in 0.4% and urolithiasis in 1.3% of Eldecalcitol recipients over 36 months of treatment. Eldecalcitol is an efficacious treatment for patients with osteoporosis that should be further investigated in head-to-head trials with other recommended first-line pharmacological treatments.
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.PMID:33223823DOI:10.2147/DDDT.S269223.
Purpose: Periodontitis is a major chronic oral disease that is accelerated by activation of the NLRP3 inflammasome and the resulting pyroptosis. According to recent studies, active vitamin D and its analogs have been reported to have great anti-inflammatory effects. However, the anti-inflammatory mechanism of a newly found vitamin D analog, Eldecalcitol (ED-71), is still unclear. This study investigates whether ED-71 could protect human gingival fibroblasts (HGFs) from LPS-induced pyroptosis and, if so, determine its underlying mechanism. Methods: After HGFs were treated with LPS alone or with LPS and ED-71, their viability was measured by CCK8 assay. The degrees of inflammation and pyroptosis were measured via LDH assay, H2O2 assay, fluorescent staining, flow cytometry, and Western blots. Intracellular ROS, Hoechst 33,342, and PI stains were assessed with a fluorescence microscope. ROS inhibitor NAC, NLRP3 inhibitor MCC950, and Nrf2 inhibitor ML385 were added to further clarify the mechanism. Results: LPS induced cytotoxicity in HGFs, as shown by CCK8 assay. LPS also increased intracellular ROS, H2O2 levels, release of LDH, and expression of the pyroptosis-related proteins NLRP3, caspase-1, and IL-1β. NAC and MCC950 reduced LPS-induced NLRP3, caspase-1, and IL-1β. Pretreatment with ED-71 effectively inhibited the LPS-induced pyroptosis and was associated with activation of the Nrf2/HO-1 signaling pathway. This beneficial effect of ED-71 was suppressed by ML385. Conclusion: This study demonstrates the therapeutic effect of ED-71 on LPS-induced NLRP3 inflammasome-dependent pyroptosis in HGFs and further reveals that ED-71 can inhibit pyroptosis by activating the Nrf2/HO-1 pathway. Our results thus suggest that ED-71 is a potential candidate for the treatment of periodontitis.
[Eldecalcitol (ED-71)]
Clin Calcium 2011 Jan;21(1):53-8.PMID:21187594doi
ED-71 is a new vitamin D receptor ligand, bearing a hydroxypropoxy substituent at the 2β-position of 1α, 25 (OH) (2)D(3). In ovariectomized rats, ED-71 increased vertebral bone mass and bone strength by inhibiting bone resorption and maintaining bone formation. In randomized, placebo-controlled, double-blinded clinical trial for osteoporotic subjects, ED-71 increased lumber vertebral and hip bone mineral density independently vitamin D status. Furthermore, ED-71 may have a better osteoprotective effect than alfacalcidol and suggest that ED-71 may serve as a new generation of active vitamin D with anti-fracture efficacy in osteiporotic subjects.