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Calcifediol monohydrate

Catalog No.GC16720

Calcifediol monohydrate (25-hydroxy Vitamin D3 monohydrate; 25(OH)D3) is a potent ligand for the vitamin D receptor (VDR) with gene regulatory and anti-proliferative properties, and functions as a vitamin D supplement and a VDR antagonist.

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Calcifediol monohydrate Chemical Structure

Cas No.: 63283-36-3

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5mg
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25mg
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100mg
$758.00
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500mg
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Sample solution is provided at 25 µL, 10mM.

Description of Calcifediol monohydrate

Calcifediol monohydrate (25-hydroxy Vitamin D3 monohydrate; 25(OH)D3) is a potent ligand for the vitamin D receptor (VDR) with gene regulatory and anti-proliferative properties, and functions as a vitamin D supplement and a VDR antagonist. As a precursor hormone in the vitamin D endocrine system (VDES), calcifediol undergoes hydroxylation in the liver to form the active hormone, calcitriol. This form of vitamin D can rapidly increase serum vitamin D levels [1-3].

Calcifediol monohydrate (100nM; 24h) decreased amyloid-β (Aβ)-production and increased Aβ-degradation in neuroblastoma cells. Effects were mediated by affecting the Aβ-producing enzymes BACE1 and γ-secretase [4]. Calcifediol monohydrate(10−5M) can induce a rapid increase in Ca2+ levels in hADMSCs cells in vitro [5].

Calcifediol monohydrate (5µg/kg, 100µL; 7 times; i.p)significantly protected mice against DNCB-induced AD. Calcifediol monohydrate may reduce inflammatory cell infiltration and chemokines by inhibiting the phosphorylation of STAT3 and may restore skin barrier function through the downregulation of AQP3 protein expression and inhibition of cell proliferation in In AD mouse model [6]. After viral attack, mice supplemented with Calcifediol monohydrate(125mg/kg; p.o; 7 weeks) stimulated the production of both anti-inflammatory and pro-inflammatory cytokines [7].

References:
[1]. Castoldi A, Herr C, et,al. Calcifediol-loaded liposomes for local treatment of pulmonary bacterial infections. Eur J Pharm Biopharm. 2017 Sep;118:62-67. doi: 10.1016/j.ejpb.2016.11.026. Epub 2016 Nov 22. PMID: 27888144.
[2]. Zheng W, Duan B, et,al. 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. doi: 10.1042/BSR20180595. PMID: 30314996; PMCID: PMC6435469.
[3]. Lou YR, Molnár F, Peräkylä M, Qiao S, Kalueff AV, St-Arnaud R, Carlberg C, Tuohimaa P. 25-Hydroxyvitamin D(3) is an agonistic vitamin D receptor ligand. J Steroid Biochem Mol Biol. 2010 Feb 15;118(3):162-70. doi: 10.1016/j.jsbmb.2009.11.011. Epub 2009 Nov 26. PMID: 19944755.
[4]. Grimm MOW, Thiel A, Lauer AA, Winkler J, Lehmann J, Regner L, Nelke C, Janitschke D, Benoist C, Streidenberger O, Stötzel H, Endres K, Herr C, Beisswenger C, Grimm HS, Bals R, Lammert F, Hartmann T. Vitamin D and Its Analogues Decrease Amyloid-β (Aβ) Formation and Increase Aβ-Degradation. Int J Mol Sci. 2017 Dec 19;18(12):2764. doi: 10.3390/ijms18122764. PMID: 29257109; PMCID: PMC5751363.
[5]. Donati S, Palmini G, Romagnoli C, Aurilia C, Miglietta F, Falsetti I, Marini F, Zonefrati R, Galli G, Marcucci G, Iantomasi T, Brandi ML. In Vitro Non-Genomic Effects of Calcifediol on Human Preosteoblastic Cells. Nutrients. 2021 Nov 25;13(12):4227. doi: 10.3390/nu13124227. PMID: 34959778; PMCID: PMC8707877.
[6]. Lu R, Peng Z, Lian P, Wazir J, Gu C, Ma C, Wei L, Li L, Pu W, Liu J, Wang H, Su Z. Vitamin D attenuates DNCB-induced atopic dermatitis-like skin lesions by inhibiting immune response and restoring skin barrier function. Int Immunopharmacol. 2023 Sep;122:110558. doi: 10.1016/j.intimp.2023.110558. Epub 2023 Jun 30. PMID: 37393836.
[7]. Hayashi H, Okamatsu M, et,al. Oral Supplementation of the Vitamin D Metabolite 25(OH)D3 Against Influenza Virus Infection in Mice. Nutrients. 2020 Jul 5;12(7):2000. doi: 10.3390/nu12072000. PMID: 32635656; PMCID: PMC7400405.

Protocol of Calcifediol monohydrate

Cell experiment [1]:

Cell lines

Neuroblastoma cells

Preparation Method

Cells were treated with Calcifediol monohydrate in a final concentration of 100nM or solvent control (EtOH).

Reaction Conditions

100nM; 24h

Applications

Calcifediol monohydrate decreased amyloid-β (Aβ)-production and increased Aβ-degradation in neuroblastoma cells.
Animal experiment [2]:

Animal models

Atopic dermatitis (AD) mice model (Female BALB/c mice)

Preparation Method

The AD mice model was induced by using DNCB. 1% DNCB was applied once a day to the ears (5μL) of AD-induced mice on days 6, 10, 14, and 18. The treatment was started on the day of challenge (day 6) with an intraperitoneal injection of 100µL Calcifediol monohydrate(5µg/kg). Each dose was given once every two days for a total of seven doses.

Dosage form

5µg/kg, 100µL; 7 times; i.p

Applications

Calcifediol monohydrate treatment reduces inflammatory infiltration and edema in the ears of AD mice.

References:
[1]. Grimm MOW, Thiel A, et,al. Vitamin D and Its Analogues Decrease Amyloid-β (Aβ) Formation and Increase Aβ-Degradation. Int J Mol Sci. 2017 Dec 19;18(12):2764. doi: 10.3390/ijms18122764. PMID: 29257109; PMCID: PMC5751363.
[2]. Lu R, Peng Z, et,al. Vitamin D attenuates DNCB-induced atopic dermatitis-like skin lesions by inhibiting immune response and restoring skin barrier function. Int Immunopharmacol. 2023 Sep;122:110558. doi: 10.1016/j.intimp.2023.110558. Epub 2023 Jun 30. PMID: 37393836.

Chemical Properties of Calcifediol monohydrate

Cas No. 63283-36-3 SDF
Chemical Name (1S,3Z)-3-[(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]-4-methylidenecyclohexan-1-ol;hydrate
Canonical SMILES CC(CCCC(C)(C)O)C1CCC2C1(CCCC2=CC=C3CC(CCC3=C)O)C.O
Formula C27H46O3 M.Wt 418.65
Solubility DMSO : 50 mg/mL (119.43 mM);Soluble in Chloroform Storage Store at -20°C, protect from light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Calcifediol monohydrate

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1 mg 5 mg 10 mg
1 mM 2.3886 mL 11.9432 mL 23.8863 mL
5 mM 0.4777 mL 2.3886 mL 4.7773 mL
10 mM 0.2389 mL 1.1943 mL 2.3886 mL
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