Eldecalcitol   中文名称: 艾地骨化醇

艾德骨化醇无细胞毒性，可减少 LPS (5 μg/mL) 诱导的细胞死亡（0.5–50 nM；24 小时）[2]。通过激活 Eldecalcitol (0.5-50 nM; 24 h)，Eldecalcitol (5 nM; 24 h) 表现出抗焦亡能力，并诱导 NLRP3、caspase-1 和 IL 的剂量减少。 LPS 诱导的焦亡被 Nrf2 及其效应分子 HO-1 抑制[2]。 Eldecalcitol（0.04–40 nM；0-48 小时）可防止 SCC-15 和 CAL-27 细胞增殖和迁移 [3]。 -1β 处的细胞周期曲线表达由依德骨化醇（0.4 nM；48 小时）诱导[3]。 G0/G1 期，以及通过阻止细胞表达谷胱甘肽过氧化物酶或 GPx-1 [3]。

通过抑制 GPx-1（谷胱甘肽过氧化物酶），艾德骨化醇（0.5 μg/kg；通道；每周两次，持续 4 周）具有抗癌作用 [3]。 Eldecalcitol，一种更有效的维生素 D3 类似物，可促进局灶性骨（微型模型），并且在抑制骨吸收方面比骨 Chetriol 更有效（10、30 或 90 ng/kg；侧向；每周 5 次，持续 12 周）。

蛋白质印迹分析 [2]
细胞类型：人类牙龈成纤维细胞 (HGF)
测试浓度：0、0.5、5 和 50 nM
孵育持续时间：24小时
实验结果：与LPS治疗组相比，TLR4、NLRP3、caspase-1 p20、ASC和GSDMD-N水平以剂量依赖性方式降低。 LPS 诱导的 IL-1β 和 IL-18 释放减少至正常水平。

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细胞增殖测定 [3]
细胞类型： SCC-15 和 CAL-27 细胞
测试浓度： 0、0.04、 0.4、4 和 40 nM
孵育时间：6、8、12、24、48 小时
实验结果：使用 0.4 nM 的细胞活力，OSCC 细胞在 24 小时内达到 50%。

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细胞增殖分析 [3]
细胞类型： OSCC 细胞
测试浓度： 0.4 nM
孵育时间：48小时
实验结果：晚期凋亡细胞比例从7.1%增加到16.1%。 Bax 和 caspase-3 上调，Bcl-2 下调。显着引发 SCC-15 和 CAL-27 细胞凋亡。

Animal/Disease Models: Mouse xenograft tumor model (male athymic nude BALB/c mouse) [3]
Doses: 0.5 μg/kg
Route of Administration: po (oral gavage); [4]. Twice a week for 4 weeks.
Experimental Results: diminished tumor growth rate, down-regulated the expression levels of PCNA and MMP-2 in tumors, and up-regulated Bax expression. Resulting in diminished proliferation, inhibition of migration, and promotion of apoptosis.

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Animal/Disease Models: Ovariectomized (OVX) rat model [4]
Doses: 10, 30 or 90 ng/kg
Route of Administration: po (oral gavage); 5 times per week for 12 weeks
Experimental Results: Lumbar spine and femur BMD in a dose-dependent manner way increased. The stimulation of local bone formation begins without prior bone resorption, a process called bone micromodelling.

[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.

C30H50O5

490.725

490.3658

C, 73.43; H, 10.27; O, 16.30

104121-92-8

Eldecalcitol-d6

Solid powder

C[C@H](CCCC(C)(C)O)[C@H]1CC[C@@H]\2[C@@]1(CCC/C2=C\C=C/3\C[C@H]([C@H]([C@@H](C3=C)O)OCCCO)O)C

FZEXGDDBXLBRTD-AYIMTCTASA-N

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

(1R,2R,3R,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(2R)-6-hydroxy-6-methylheptan-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-2-(3-hydroxypropoxy)-4-methylidenecyclohexane-1,3-diol

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

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Methanol: ~8.3 mg/mL (~17 mM)
DMSO: ~3.3 mg/mL (~6.8 mM)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。