VDR

对于假单胞菌感染的上皮细胞，促炎细胞因子 KC 不受骨化二醇或骨化二醇乙醇溶液的影响。骨化二醇或骨化二醇乙醇溶液感染人支气管炎16-HBE细胞的致死率显着降低[1]。

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维生素D降低MCF-7细胞的存活率并促进其凋亡。维生素D增强VDR表达并诱导DNA损伤。当CD133+干细胞与MCF-7细胞分离时，三苯氧胺对干细胞的IC50明显高于亲本MCF-7细胞，表明MCF-7干细胞对三苯氧铵的耐药性更高。CD133+细胞中VDR表达和Wnt/β-catenin信号传导水平分别显著低于和高于CD133-细胞。与对照细胞相比，转染VDR过表达质粒的干细胞显示出他莫昔芬IC50值、存活率、球体形成以及Wnt和β-catenin蛋白表达的降低。转染VDR过表达质粒可增加细胞凋亡。最后，VDR过表达诱导的抑制作用可以被VDR抑制剂骨化三醇逆转。结论：干细胞参与了MCF-7细胞对三苯氧胺的耐药性。维生素D诱导的VDR表达通过抑制Wnt/β-catenin信号传导增加了MCF-7干细胞对他莫昔芬的敏感性[2]。

三天内，将 50 ng/d 的骨化二醇或单独的载体注射到自发性高血压大鼠和正常血压 Wistar-Kyoto (WKY) 大鼠中。在对照 SHR 中，发现细胞 Ca2+ 通量和钙结合蛋白-D9K 减少。骨化二醇升高刷状缘和总细胞钙结合蛋白-D9K。另一方面，对于与 WKY 大鼠相当的血浆骨化三醇水平，在 vit-D 动物中升高的 Ca2+ 通量在 SHR 中保持较低。

用1,25（OH）2D3处理MCF-7细胞，检测其VDR表达、存活率和凋亡水平。鉴定CD133+MCF-7干细胞，并用VDR过表达质粒转染。测定了将MCF-7细胞存活率降低50%的他莫昔芬浓度（IC50）。还研究了Wnt/β-catenin信号传导的激活[2]。

50 ng/d; injection
Rats

Absorption, Distribution and Excretion
Readily absorbed.

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Metabolism / Metabolites
Calcidiol undergoes hydroxylation in the mitochondria of kidney tissue, and this reaction is activated by the renal 25-hydroxyvitamin D3-1-(alpha)-hydroxylase to produce calcitriol (1,25- dihydroxycholecalciferol), the active form of vitamin D3.

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Biological Half-Life
288 hours

[1]. Calcifediol-loaded liposomes for local treatment of pulmonary bacterial infections. Eur J Pharm Biopharm. 2016 Nov 22.

[2]. Vitamin D-induced vitamin D receptor expression induces tamoxifen sensitivity in MCF-7 stem cells via suppression of Wnt/β-catenin signaling. Biosci Rep. 2018 Dec 7;38(6):BSR20180595.

Calcifediol monohydrate is a vitamin D.
The major circulating metabolite of vitamin D3 (cholecalciferol). It is produced in the liver and is the best indicator of the body's vitamin D stores. It is effective in the treatment of rickets and osteomalacia, both in azotemic and non-azotemic patients. Calcifediol also has mineralizing properties.
Calcifediol is an orally available synthetic form of the calcitriol prohormone calcifediol (25-hydroxyvitamin D), which can be used for vitamin D supplementation, and with potential immunomodulating activity. Upon oral administration, calcifediol is taken up by the body and converted, in the kidneys, to the active form calcitriol (1,25-dihydroxyvitamin D or 1,25(OH)2D). This form increases and normalizes vitamin D plasma levels, which, in turn, regulates calcium plasma levels, and normalizes elevated parathyroid hormone (PTH) levels by suppressing both PTH synthesis, and secretion. Vitamin D modulates and enhances the innate and adaptive immune responses. This may improve unregulated inflammation and prevents the production of pro-inflammatory cytokines. Specifically, vitamin D binds to its receptor vitamin D receptor (VDR) which is widely expressed on immune cells and epithelial cells. This stimulates neutrophils, macrophages, and natural killer (NK) cells, and activates epithelial cells to produce antimicrobial peptides (AMPs). In addition, upon infection, vitamin D promotes the migration of myeloid dendritic cells (mDCs) to lymphoid organs where they activate B- and T-lymphocytes.
The major circulating metabolite of VITAMIN D3. It is produced in the LIVER and is the best indicator of the body's vitamin D stores. It is effective in the treatment of RICKETS and OSTEOMALACIA, both in azotemic and non-azotemic patients. Calcifediol also has mineralizing properties.

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Drug Indication
Used to treat vitamin D deficiency or insufficiency, refractory rickets (vitamin D resistant rickets), familial hypophosphatemia and hypoparathyroidism, and in the management of hypocalcemia and renal osteodystrophy in patients with chronic renal failure undergoing dialysis. Also used in conjunction with calcium in the management and prevention of primary or corticosteroid-induced osteoporosis.
Treatment of secondary hyperparathyroidism (SHPT)

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Mechanism of Action
Calcidiol is transformed in the kidney by 25-hydroxyvitamin D3-1-(alpha)-hydroxylase to calcitriol, the active form of vitamin D3. Calcitriol binds to intracellular receptors that then function as transcription factors to modulate gene expression. Like the receptors for other steroid hormones and thyroid hormones, the vitamin D receptor has hormone-binding and DNA-binding domains. The vitamin D receptor forms a complex with another intracellular receptor, the retinoid-X receptor, and that heterodimer is what binds to DNA. In most cases studied, the effect is to activate transcription, but situations are also known in which vitamin D suppresses transcription. Calcitriol increases the serum calcium concentrations by: increasing GI absorption of phosphorus and calcium, increasing osteoclastic resorption, and increasing distal renal tubular reabsorption of calcium. Calcitriol appears to promote intestinal absorption of calcium through binding to the vitamin D receptor in the mucosal cytoplasm of the intestine. Subsequently, calcium is absorbed through formation of a calcium-binding protein.

C27H46O3

418.66

418.344

C, 77.46; H, 11.08; O, 11.46

63283-36-3

Calcifediol;19356-17-3;Calcifediol-d6 monohydrate;2483831-70-3;Calcifediol-13C5 monohydrate

6441383

White to off-white solid powder

529.2ºC at 760 mmHg

221.4ºC

2.07E-13mmHg at 25°C

6.733

40.46

3

3

6

30

655

5

C[C@H](CCCC(C)(C)O)[C@H]1CC[C@@H]\2[C@@]1(CCC/C2=C\C=C/3\C[C@H](CCC3=C)O)C.O

WRLFSJXJGJBFJQ-WPUCQFJDSA-N

InChI=1S/C27H44O2.H2O/c1-19-10-13-23(28)18-22(19)12-11-21-9-7-17-27(5)24(14-15-25(21)27)20(2)8-6-16-26(3,4)29/h11-12,20,23-25,28-29H,1,6-10,13-18H2,2-5H31H2/b21-11+,22-12-/t20-,23+,24-,25+,27-/m1./s1

(S,Z)-3-(2-((1R,3aS,7aR,E)-1-((R)-6-hydroxy-6-methylheptan-2-yl)-7a-methyloctahydro-4H-inden-4-ylidene)ethylidene)-4-methylenecyclohexan-1-ol hydrate

U 32070E; U-32070E; 63283-36-3; Calcifediol (monohydrate); Calderol; Calcifediol hydrate; Hidroferol; Didrogyl; U32070E; 2,5-Hydroxyvitamin D3 monohydrate; Calderol Dedrogyl Rayaldee

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage.  (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture.

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

DMSO : ~50 mg/mL (~119.43 mM)

配方 1 中的溶解度: ≥ 2.5 mg/mL (5.97 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.5 mg/mL (5.97 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液添加到 900 μL 玉米油中并混合均匀。

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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。