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Calcifediol (Synonyms: 25hydroxy Cholecalciferol, RO 88892, Rovimix HyD, U 32070E)

Catalog No.GC16066 Copy One-Click Copy Product Info

Major circulating form of vitamin D3

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Calcifediol Chemical Structure

Cas No.: 19356-17-3

Size Price Stock Qty
10mM (in 1mL DMSO)
$103.00
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5mg
$67.00
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25mg
$250.00
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100mg
$711.00
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500mg
$1,192.00
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1g
$2,080.00
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Sample solution is provided at 25 µL, 10mM.



Description of Calcifediol

Vitamin D receptor (VDR) activation is associated with cardiovascular and survival benefits in chronic kidney disease patients. Calcifediol, also known as calcidiol, is a prehormone that is produced in the liver by hydroxylation of vitamin D3.

In vitro: Calcifediol induced CYP24A1 expression with EC50 at 70 nM. Calcifediol stimulated the expression of thrombomodulin with EC50 at 10-100 nM. Confocal microscopy revealed that calcifediol at 0.1 - 10 μM induced VDR translocation into the nucleus dose-dependently; the VDR localization pattern was similar in cells treated with calcitriol [1].

In vivo: Spontaneously hypertensive rats and normotensive Wistar-Kyoto (WKY) rats were injected with either 50 ng/d calcifediol or vehicle alone for 3 days. Decreased calbindin-D9K and cellular Ca2+ flux were observed in control SHR. Calcifediol increased total cell and brush border calbindin-D9K. In contrast, Ca2+ flux, which increased in vit-D animals, remained lower in SHR for plasma calcitriol levels similar to those in WKY rats [2].

Clinical trial: Calcifediol given daily, weekly, or as a single bolus is about 2-3 times more potent in increasing plasma 25(OH)D3 concentrations than vitamin D3. Plasma 25(OH)D3 concentrations of 30 ng/mL were reached more rapidly and reliably with calcifediol [3].

Reference:
[1] 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.
[2] 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.
[3] Jetter A, Egli A, Dawson-Hughes B, Staehelin HB, Stoecklin E, Goessl R, Henschkowski J, Bischoff-Ferrari HA.  Pharmacokinetics of oral vitamin D(3) and calcifediol. Bone. 2014 Feb;59:14-9.

Protocol of Calcifediol

Cell experiment [1,2]:

Cell lines

Neonatal rat cardiomyocytes, plasmacyoid dendritic cells (pDCs) and conventional DCs

Preparation method

The solubility of this compound in DMSO is >13.65mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0.1-10 μM, 2 hours

Applications

Calcifediol induced CYP24A1 expression with EC50 of 70 nM. Calcifediol stimulated the expression of thrombomodulin with EC50 at 10-100 nM. Calcifediol (0.1-10 μM) dose-dependently induced VDR translocation into the nucleus. Calcifediol led to significant expression of Cyp24A1 in moDCs after 16 hours.

Animal experiment [2]:

Animal models

Wistar-Kyoto rats

Dosage form

50 ng/d calcifediol for 3 days

Application

In spontaneously hypertensive rats and normotensive Wistar-Kyoto (WKY) rats, calcifediol (50 ng/d for 3 days), calcifediol increased total cell and brush border calbindin-D9K.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Wu-Wong J R, Chen Y W, Nakane M, et al. Differential effects of vitamin d receptor agonists on gene expression in neonatal rat cardiomyocytes[J]. Cardiovascular drugs and therapy, 2011, 25(3): 215-222.

[2]. Karthaus N, Van Spriel A B, Looman M W G, et al. Vitamin D controls murine and human plasmacytoid dendritic cell function[J]. Journal of Investigative Dermatology, 2014, 134(5): 1255-1264.

[3]. Roullet C M, Roullet J B, Martin A S, et al. In vivo effect of calcitriol on calcium transport and calcium binding proteins in the spontaneously hypertensive rat[J]. Hypertension, 1994, 24(2): 176-182.

Chemical Properties of Calcifediol

Cas No. 19356-17-3 SDF
Synonyms 25hydroxy Cholecalciferol, RO 88892, Rovimix HyD, U 32070E
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
Canonical SMILES CC(CCCC(C)(C)O)C1CCC2C1(CCCC2=CC=C3CC(CCC3=C)O)C
Formula C27H44O2 M.Wt 400.64
Solubility ≥ 13.65mg/mL in DMSO 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

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.496 mL 12.48 mL 24.9601 mL
5 mM 499.2 μL 2.496 mL 4.992 mL
10 mM 249.6 μL 1.248 mL 2.496 mL
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In vivo Formulation Calculator (Clear solution) of Calcifediol

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Product Documents

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Average Rating: 5 ★★★★★ (Based on Reviews and 28 reference(s) in Google Scholar.)

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