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Calcifediol

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Chemical Structure| 19356-17-3 同义名 : 25-羟基维生素 D3 ;25-hydroxy Vitamin D3;25-hydroxy Cholecalciferol;U 32070E;Rovimix Hy-D;RO 8-8892;Hidroferol;Didrogyl;Calcidiol
CAS号 : 19356-17-3
货号 : A154275
分子式 : C27H44O2
纯度 : 99%+
分子量 : 400.637
MDL号 : MFCD00867077
存储条件:

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(262.08 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:

2% DMSO+30% PEG 300+5% Tween+water 5 mg/mL

生物活性
描述 Vitamin D3 receptor is a member of the nuclear hormone receptor superfamily of ligand-inducible transcription factors. It is the nuclear receptor for calcitriol which is the active form of vitamin D3 which mediates the action of this vitamin on cells. Vitamin D3 receptor enters the nucleus upon vitamin D3 binding where it forms heterodimers with the retinoid X receptor/RXR. The VDR-RXR heterodimers bind to specific response elements on DNA and activate the transcription of vitamin D3-responsive target genes[4]. Downstream targets of vitamin D3 receptor are principally involved in mineral metabolism and vitamin D3 receptor plays a central role in calcium homeostasis. Calcifediol, also known as calcidiol, is a prehormone that is produced in the liver by hydroxylation of vitamin D3. Calcifediol is further hydroxylated by CYP27B1 to form the active metabolite, calcitriol[5]. Calcitriol is a vitamin D3 receptor (VDR) agonist. According to a report, neonatal rat cardiomyocytes were treated with the prehormone calcidiol in the presence of aldo (1 μM). Calcidiol induced VDR expression in the presence of aldo with EC50 at 7952 nM. Calcidiol also stimulated CYP24A1 with EC50 at 992 nM and suppressed NPPB expression with IC50 at 210 nM in the presence of 1 μM aldo[5]. In another study, calcifediol was encapsulated in liposomes to enable aerosolisation, and tested for the ability to prevent pulmonary infection by Pseudomonas aeruginosa. Treatment of infected, human bronchial 16-HBE cells with liposomes containing 40 ng calcifediol resulted in a significant reduction in bacterial survival[6].In vivo, the active metabolite, calcitriol was injected at the dose of 50 ng daily for 3 days to SHR or WKY rats. Calcitriol increased total cell and brush border calbindin-D9K in both strains but had no effect on calmodulin in either strain[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.50mL

0.50mL

0.25mL

12.48mL

2.50mL

1.25mL

24.96mL

4.99mL

2.50mL

参考文献

[1]Fedirko V, Bostick RM, et al. Blood 25-hydroxyvitamin D3 concentrations and incident sporadic colorectal adenoma risk: a pooled case-control study. Am J Epidemiol. 2010 Sep 1;172(5):489-500.

[2]Rowling MJ, Kemmis CM, et al. Megalin-mediated endocytosis of vitamin D binding protein correlates with 25-hydroxycholecalciferol actions in human mammary cells. J Nutr. 2006 Nov;136(11):2754-9.

[3]RAYALDEE

[4]Tamura M, Ishizawa M, Isojima T, Özen S, Oka A, Makishima M, Kitanaka S. Functional analyses of a novel missense and other mutations of the vitamin D receptor in association with alopecia. Sci Rep. 2017 Jul 11;7(1):5102. doi: 10.1038/s41598-017-05081-x. PMID: 28698609; PMCID: PMC5505967.

[5]Wu-Wong JR, Chen YW, Nakane M, Wolf M. Differential effects of vitamin d receptor agonists on gene expression in neonatal rat cardiomyocytes. Cardiovasc Drugs Ther. 2011 Jun;25(3):215-22. doi: 10.1007/s10557-011-6287-7. PMID: 21424825.

[6]Castoldi A, Herr C, Niederstraßer J, Labouta HI, Melero A, Gordon S, Schneider-Daum N, Bals R, Lehr CM. 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.

[7]Roullet CM, Roullet JB, Martin AS, McCarron DA. In vivo effect of calcitriol on calcium transport and calcium binding proteins in the spontaneously hypertensive rat. Hypertension. 1994 Aug;24(2):176-82. doi: 10.1161/01.hyp.24.2.176. PMID: 8039841.