1. Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Anti-infection
  2. VD/VDR Endogenous Metabolite Bacterial
  3. Vitamin D3

Vitamin D3  (Synonyms: 维生素D3; Cholecalciferol; Colecalciferol)

目录号: HY-15398 纯度: 99.94%
COA 产品使用指南

Vitamin D3 (Cholecalciferol; Colecalciferol) 是维生素 D 的天然存在形式,代谢激活后能诱导细胞分化和癌细胞增殖。

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Vitamin D3 Chemical Structure

Vitamin D3 Chemical Structure

CAS No. : 67-97-0

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Other Forms of Vitamin D3:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Vitamin D3 (Cholecalciferol; Colecalciferol) is a naturally occuring form of vitamin D. Vitamin D3 induces cell differentiation and prevents proliferation of cancer cells.

IC50 & Target

Human Endogenous Metabolite

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
C3H 10T1/2 IC50
2.9 μM
Compound: 3, VD3
Inhibition of Hedgehog signaling in mouse C3H10T1/2 cells assessed as downregulation of Ptch mRNA expression after 24 hrs by RT-PCR analysis
Inhibition of Hedgehog signaling in mouse C3H10T1/2 cells assessed as downregulation of Ptch mRNA expression after 24 hrs by RT-PCR analysis
[PMID: 24900716]
C3H 10T1/2 IC50
2.9 μM
Compound: 3, VD3, Vitamin D3
Inhibition of hedgehog signaling pathway-mediated PTCH mRNA expression in mouse C3H10T1/2 cells after 24 hrs by RT-PCR analysis
Inhibition of hedgehog signaling pathway-mediated PTCH mRNA expression in mouse C3H10T1/2 cells after 24 hrs by RT-PCR analysis
[PMID: 24730984]
C3H 10T1/2 IC50
4.1 μM
Compound: 3, VD3
Inhibition of Hedgehog signaling in mouse C3H10T1/2 cells assessed as downregulation of Gli1 mRNA expression after 24 hrs by RT-PCR analysis
Inhibition of Hedgehog signaling in mouse C3H10T1/2 cells assessed as downregulation of Gli1 mRNA expression after 24 hrs by RT-PCR analysis
[PMID: 24900716]
C3H 10T1/2 IC50
4.1 μM
Compound: 3, VD3, Vitamin D3
Inhibition of hedgehog signaling pathway-mediated GLI1 mRNA expression in mouse C3H10T1/2 cells after 24 hrs by RT-PCR analysis
Inhibition of hedgehog signaling pathway-mediated GLI1 mRNA expression in mouse C3H10T1/2 cells after 24 hrs by RT-PCR analysis
[PMID: 24730984]
C3H 10T1/2 IC50
4.1 μM
Compound: 2, VD3, vitamin D3
Inhibition of hedgehog signaling in mouse C3H10T1/2 cells assessed as reduction in Gli1 mRNA level after 24 hrs by quantitative PCR analysis
Inhibition of hedgehog signaling in mouse C3H10T1/2 cells assessed as reduction in Gli1 mRNA level after 24 hrs by quantitative PCR analysis
[PMID: 25676864]
Daoy IC50
> 10 μM
Compound: 3, VD3, Vitamin D3
Inhibition of hedgehog signaling pathway-mediated GLI1 mRNA expression in human DaOY cells after 24 hrs by RT-PCR analysis
Inhibition of hedgehog signaling pathway-mediated GLI1 mRNA expression in human DaOY cells after 24 hrs by RT-PCR analysis
[PMID: 24730984]
Daoy IC50
> 10 μM
Compound: 3, VD3, Vitamin D3
Inhibition of hedgehog signaling pathway-mediated PTCH mRNA expression in human DaOY cells after 24 hrs by RT-PCR analysis
Inhibition of hedgehog signaling pathway-mediated PTCH mRNA expression in human DaOY cells after 24 hrs by RT-PCR analysis
[PMID: 24730984]
Daoy IC50
> 10 μM
Compound: 3, VD3
Inhibition of Hedgehog signaling in human DaOY cells assessed as downregulation of Gli1 mRNA expression after 48 hrs by RT-PCR analysis
Inhibition of Hedgehog signaling in human DaOY cells assessed as downregulation of Gli1 mRNA expression after 48 hrs by RT-PCR analysis
[PMID: 24900716]
HEK293 EC50
0.21 nM
Compound: VitD3
Agonist activity at human VDR expressed in HEK293 cells by luciferase reporter gene assay
Agonist activity at human VDR expressed in HEK293 cells by luciferase reporter gene assay
[PMID: 25305688]
HT-29 GI50
53.8 μM
Compound: 2, VD3
Growth inhibition of human HT-29 cells after 72 hrs by MTS-PMS assay
Growth inhibition of human HT-29 cells after 72 hrs by MTS-PMS assay
[PMID: 23972439]
HT-29 GI50
68.5 μM
Compound: VD3
Growth inhibition of human HT-29 cells overexpressing VDR gene after 72 hrs by MTS assay
Growth inhibition of human HT-29 cells overexpressing VDR gene after 72 hrs by MTS assay
[PMID: 22687748]
Medulloblastoma cell GI50
5.8 μM
Compound: 1; VD3
Antiproliferative activity against medulloblastoma cells derived from conditional patched knockout mouse after 48 hrs by [3H]-thymidine incorporation assay
Antiproliferative activity against medulloblastoma cells derived from conditional patched knockout mouse after 48 hrs by [3H]-thymidine incorporation assay
[PMID: 30471551]
U-87MG ATCC GI50
23.2 μM
Compound: VD3
Growth inhibition of human U87MG cells after 72 hrs by MTS assay
Growth inhibition of human U87MG cells after 72 hrs by MTS assay
[PMID: 22687748]
U-87MG ATCC IC50
29.7 μM
Compound: VD3
Antiproliferative activity against human U87MG cells after 72 hrs by MTS assay
Antiproliferative activity against human U87MG cells after 72 hrs by MTS assay
[PMID: 22226657]
体外研究
(In Vitro)

Vitamin D3 是一种在体内无活性的维生素 D 分子。Vitamin D3 需要经历两次羟基化过程才能被激活。Vitamin D3 首先在肝脏中被羟基化,形成循环激素原 25-羟基维生素 D3 [25(OH)D3],其作用机理是酶 25-羟化酶 (CYP27A1),也可能是其他酶(例如 CYP2R1)[1]
第二次羟基化发生在肾脏中,通过酶 1-α-羟化酶,生成 1,25-二羟基胆钙化醇(骨化三醇),这是 Vitamin D3 的生物活性形式[1]
Vitamin D3(2-10 μM;24-48 小时)表现出剂量和时间依赖性的抗增殖作用。用 10 μM Vitamin D3 处理 72 小时后,细胞活力最大降低 62% (IK)、52% (RL-95-2) 和 55% (Hec-1A)。但 24 小时的暴露并未显著减少活细胞[2]
Vitamin D3 (10 μM;24-48 小时) 显示核 VDR 染色显著增加,并在 IK 细胞中产生局部 VDR 活化[1]

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

Cell Viability Assay[2]

Cell Line: EC cell lines from EEC, Ishikawa 3-H-12(IK), RL-95/2, and HEC-1-A cells
Concentration: 2-10 μM
Incubation Time: 24-72 hours
Result: Reduced viability in response to VD3 in a dose- and time-dependent manner.
Indicated that the conversion of VD3 to 25(OH)D is an essential step for the reduced cell viability effect.

Cell Viability Assay[2]

Cell Line: EC cell lines from EEC, Ishikawa 3-H-12(IK) cells
Concentration: 10 μM
Incubation Time: 24-48 hours
Result: Improved nuclear VDR content in IK cells.
体内研究
(In Vivo)

Vitamin D3(口服管饲;5 mg/kg;7 天)仅增强肝脏中的 CCl4 毒性,如血浆 ALT 和 AST 水平(肝损伤的生化标志物)所示。它显著增加小鼠的肾钙水平,但小鼠之间的肾钙含量没有显著差异[3]

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

Animal Model: Male ddY mice on CCl4 toxicity[3]
Dosage: 5 mg/kg
Administration: Oral gavage; 5 mg/kg; 7 days
Result: Potentiated CCl4-induced hepatotoxicity and enhanced mouse mortality, without increasing renal toxicity and generation of liver fibrosis.
Clinical Trial
分子量

384.64

Formula

C27H44O

CAS 号
性状

固体

颜色

White to off-white

中文名称

维生素D3;胆骨化醇

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°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 : 10 mg/mL (26.00 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)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5998 mL 12.9992 mL 25.9983 mL
5 mM 0.5200 mL 2.5998 mL 5.1997 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    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (5.41 mM); 悬浊液; 超声助溶

    此方案可获得 2.08 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    1 mL 工作液为例,取 100 μL 20.8 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。

    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。
  • 方案 二

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

    Solubility: ≥ 1 mg/mL (2.60 mM); 澄清溶液

    此方案可获得 ≥ 1 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 10.0 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。
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: 99.94%

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
DMSO 1 mM 2.5998 mL 12.9992 mL 25.9983 mL 64.9958 mL
5 mM 0.5200 mL 2.5998 mL 5.1997 mL 12.9992 mL
10 mM 0.2600 mL 1.2999 mL 2.5998 mL 6.4996 mL
15 mM 0.1733 mL 0.8666 mL 1.7332 mL 4.3331 mL
20 mM 0.1300 mL 0.6500 mL 1.2999 mL 3.2498 mL
25 mM 0.1040 mL 0.5200 mL 1.0399 mL 2.5998 mL
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    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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