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Calcipotriol monohydrate (Synonyms: Calcipotriene)

Catalog No.GC35584

A vitamin D3 analog

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Calcipotriol monohydrate Chemical Structure

Cas No.: 147657-22-5

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment:

Normal human epidermal keratinocytes (NHEK) are grown in serum-free keratinocyte growth medium Epilife and used at third passage in all experiments. Growth supplement is omitted 48 h before experiments. As a control, IL-17A and IL-22 are either added or not added to the cells. Cultured NHEK cells are stimulated with IL-17A (200 ng/mL) and/or IL-22 (200 ng/mL) followed by co-incubation in the presence or absence of Calcipotriol at 0.2-40 nM to test its modulatory effect. Cells are harvested 3 days later and subjected to real-time quantitative PCR (qPCR). Culture supernatants are also collected and frozen at -80°C until use for ELISA[1].

Animal experiment:

Mice[3]The 160 female SKH-1 hairless mice (6-7 weeks of age) are used. After UV treatment, mice without tumors are randomly divided into five groups, four chemoprevention groups (Diclofenac plus DFMO; Diclofenac plus Calcipotriol; DFMO plus calcitriol; and Diclofenac plus DFMO plus Calcipotriol) and one placebo group (skin lotion). The placebo group used in this study is the same as the one used in an earlier study. The mice are treated with test mixtures once a day, five days a week, for a total of 17 weeks. The test mixtures are applied topically on the dorsal surface of the mice. Ten microliters are applied by a pipette after which the mixture is rubbed onto the skin. This corresponded to the following doses of each active substance in the treatments: 100 μg/week for Diclofenac (30 mg/g undiluted), 0.166 μg/week for Calcitriol (50 μg/g undiluted), and 463.3 μg/week for difluoromethylornithine (DFMO) (139 mg/g undiluted).

References:

[1]. Sakabe JI, et al. Calcipotriol Increases hCAP18 mRNA Expression but Inhibits Extracellular LL37 Peptide Production in IL-17/IL-22-stimulated Normal Human Epidermal Keratinocytes. Acta Derm Venereol. 2014 Sep;94(5):512-6.
[2]. Al-Jaderi Z, et al. Effects of vitamin D3, calcipotriol and FTY720 on the expression of surface molecules and cytolytic activities of human natural killer cells and dendritic cells. Toxins (Basel). 2013 Oct 28;5(11):1932-47.
[3]. Pommergaard HC, et al. Combination chemoprevention with diclofenac, calcipotriol and difluoromethylornithine inhibits development of non-melanoma skin cancer in mice. Anticancer Res. 2013 Aug;33(8):3033-9.

Background

Calcipotriol monohydrate is a synthetic VitD3 analogue with a high affinity for the vitamin D receptor. vitamin D receptor[1]

When NHEK cells are not stimulated with IL-17A or IL-22, Calcipotriol slightly enhances (0.2 nM) IL-8 mRNA expression or has no effect (2-20 nM). The addition of IL-17A and IL-22 markedly increased the mRNA expression of IL-8, confirming our previous study. This enhanced IL-8 mRNA expression is suppressed by Calcipotriol at 2, 20 and 40 nM in a dose dependent manner[1]. Treatment of natural killer (NK) cells with drugs modulates their expression of NK cytotoxicity receptors or KIR. Human NK cells are pre-treated with 100, 10 or 1 ng/mL of 1,25(OH)2D3, Calcipotriol or FTY720 for 4 h. All three concentrations of 1,25(OH)2D3, Calcipotriol and FTY720 significantly up-regulate the expression of NKp30 on the surface of NK cells after 4 h incubation[2].

One out of the 32 animals in each of the groups has died, except for the Diclofenac plus DFMO plus Calcipotriol group, where all animals survived. Survival is equally distributed between the groups. The weight gain is significantly smaller in the groups treated with Diclofenac plus Calcipotriol (p=0.018) and Diclofenac plus DFMO plus Calcipotriol (p=0.002) compare with placebo (linear regression model)[3].

[1]. Sakabe JI, et al. Calcipotriol Increases hCAP18 mRNA Expression but Inhibits Extracellular LL37 Peptide Production in IL-17/IL-22-stimulated Normal Human Epidermal Keratinocytes. Acta Derm Venereol. 2014 Sep;94(5):512-6. [2]. Al-Jaderi Z, et al. Effects of vitamin D3, calcipotriol and FTY720 on the expression of surface molecules and cytolytic activities of human natural killer cells and dendritic cells. Toxins (Basel). 2013 Oct 28;5(11):1932-47. [3]. Pommergaard HC, et al. Combination chemoprevention with diclofenac, calcipotriol and difluoromethylornithine inhibits development of non-melanoma skin cancer in mice. Anticancer Res. 2013 Aug;33(8):3033-9.

Chemical Properties

Cas No. 147657-22-5 SDF
Synonyms Calcipotriene
Canonical SMILES O[C@H](C/1=C)C[C@H](O)CC1=C\C=C2[C@@](CC[C@@H]3[C@@H](/C=C/[C@@H](O)C4CC4)C)([H])[C@]3(C)CCC\2.[H]O
Formula C27H42O4 M.Wt 430.62
Solubility DMSO: 100 mg/mL (232.22 mM) Storage 4°C, protect from light, stored under nitrogen,unstable in solution, ready to use.
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

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1 mg 5 mg 10 mg
1 mM 2.3222 mL 11.6112 mL 23.2223 mL
5 mM 0.4644 mL 2.3222 mL 4.6445 mL
10 mM 0.2322 mL 1.1611 mL 2.3222 mL
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