1. Vitamin D Related/Nuclear Receptor
  2. VD/VDR
  3. Calcipotriol

Calcipotriol  (Synonyms: 卡泊三醇; MC 903; Calcipotriene)

目录号: HY-10001 纯度: 99.90%
COA 产品使用指南

Calcipotriol 是一种合成的 VitD3 类似物,对 vitamin D 受体具有高亲和力。

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Calcipotriol Chemical Structure

Calcipotriol Chemical Structure

CAS No. : 112965-21-6

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Customer Review

Other Forms of Calcipotriol:

    Calcipotriol purchased from MCE. Usage Cited in: J Allergy Clin Immunol. 2022.

    A significant number of infiltrating cells express both IL-31 (green) and MOMA-2 (red) in Calcipotriol (MC903)-treated mice.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Calcipotriol is a synthetic VitD3 analogue with a high affinity for the vitamin D receptor.

    IC50 & Target

    Vitamin D receptor[1]

    体外研究
    (In Vitro)

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    分子量

    412.60

    Formula

    C27H40O3

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    卡泊三醇;钙泊三醇;卡泊三烯

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    -20°C, protect from light, stored under nitrogen

    *该产品在溶液状态不稳定,建议您现用现配,即刻使用。

    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : 100 mg/mL (242.37 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    Ethanol 中的溶解度 : 50 mg/mL (121.18 mM; 超声助溶)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.4237 mL 12.1183 mL 24.2365 mL
    5 mM 0.4847 mL 2.4237 mL 4.8473 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液;该产品在溶液状态不稳定,建议您现用现配,即刻使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.06 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.06 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

    *该产品在溶液状态不稳定,建议您现用现配,即刻使用。

    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.90%

    参考文献
    Cell Assay
    [1]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    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).

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液;该产品在溶液状态不稳定,建议您现用现配,即刻使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    Ethanol / DMSO 1 mM 2.4237 mL 12.1183 mL 24.2365 mL 60.5914 mL
    5 mM 0.4847 mL 2.4237 mL 4.8473 mL 12.1183 mL
    10 mM 0.2424 mL 1.2118 mL 2.4237 mL 6.0591 mL
    15 mM 0.1616 mL 0.8079 mL 1.6158 mL 4.0394 mL
    20 mM 0.1212 mL 0.6059 mL 1.2118 mL 3.0296 mL
    25 mM 0.0969 mL 0.4847 mL 0.9695 mL 2.4237 mL
    30 mM 0.0808 mL 0.4039 mL 0.8079 mL 2.0197 mL
    40 mM 0.0606 mL 0.3030 mL 0.6059 mL 1.5148 mL
    50 mM 0.0485 mL 0.2424 mL 0.4847 mL 1.2118 mL
    60 mM 0.0404 mL 0.2020 mL 0.4039 mL 1.0099 mL
    80 mM 0.0303 mL 0.1515 mL 0.3030 mL 0.7574 mL
    100 mM 0.0242 mL 0.1212 mL 0.2424 mL 0.6059 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    产品名称:
    Calcipotriol
    目录号:
    HY-10001
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