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  3. Kaempferide

Kaempferide  (Synonyms: 山奈素; Kaempferol 4'-O-methyl ether)

目录号: HY-15449 纯度: 99.35%
COA 产品使用指南

Kaempferide 是具有口服活性的可以从 Hippophae rhamnoides L 中分离得到的黄酮醇。Kaempferide 有抗癌、抗炎症、抗氧化、抗糖尿病、抗肥胖、抗高血压和神经保护等活性。Kaempferide 可以诱导细胞凋亡 (apoptosis)。Kaempferide 通过抗氧化来促进成骨,可以用于骨质疏松的研究。

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Kaempferide Chemical Structure

Kaempferide Chemical Structure

CAS No. : 491-54-3

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Other Forms of Kaempferide:

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Kaempferide is an orally active flavonol isolated from Hippophae rhamnoides L. Kaempferide has anticancer, anti-inflammatory, antioxidant, antidiabetic, antiobesity, antihypertensive, and neuroprotective activities. Kaempferide induces apoptosis. Kaempferide promotes osteogenesis through antioxidants and can be used in osteoporosis research[1][2][3][4][5][6].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
2.2 x 10-5 M
Compound: 13
Cytotoxicity against human A549 cells after 72 hrs by XTT assay
Cytotoxicity against human A549 cells after 72 hrs by XTT assay
[PMID: 20619940]
B16 IC50
16 μM
Compound: 5
Inhibition of melanogenesis in theophylline-stimulated mouse B16-4A5 cells after 72 hrs
Inhibition of melanogenesis in theophylline-stimulated mouse B16-4A5 cells after 72 hrs
[PMID: 19615910]
B16-4A5 IC50
> 100 μM
Compound: 5
Inhibition of theophylline-stimulated mouse B16-4A5 cell proliferation assessed as cell viability after 68 hrs by WST8 assay
Inhibition of theophylline-stimulated mouse B16-4A5 cell proliferation assessed as cell viability after 68 hrs by WST8 assay
[PMID: 19615910]
HeLa IC50
2 μg/mL
Compound: 7
Antiallergic activity in Ca(2+)-stimulated differentiated human HeLa cells assessed as inhibition of cys-leukotriene release after 6 days by ELISA
Antiallergic activity in Ca(2+)-stimulated differentiated human HeLa cells assessed as inhibition of cys-leukotriene release after 6 days by ELISA
[PMID: 19942440]
HeLa IC50
2.3 x 10-5 M
Compound: 13
Cytotoxicity against human HeLa cells after 72 hrs by XTT assay
Cytotoxicity against human HeLa cells after 72 hrs by XTT assay
[PMID: 20619940]
HT-1080 ED50
< 8 μg/mL
Compound: Kaempferide
Cytotoxicity against human HT1080 cells by MTT assay
Cytotoxicity against human HT1080 cells by MTT assay
[PMID: 11000036]
HT-1080 ED50
2.91 μg/mL
Compound: 20
Cytotoxicity against human HT1080 cells after 24 hrs by MTT assay
Cytotoxicity against human HT1080 cells after 24 hrs by MTT assay
[PMID: 9677271]
HT-29 IC50
3.2 x 10-5 M
Compound: 13
Cytotoxicity against human HT-29 cells after 72 hrs by XTT assay
Cytotoxicity against human HT-29 cells after 72 hrs by XTT assay
[PMID: 20619940]
Huh-7 CC50
> 50 μM
Compound: 30
Cytotoxicity against human Huh7.5.1 cells by MTT assay
Cytotoxicity against human Huh7.5.1 cells by MTT assay
[PMID: 22445328]
L929 EC50
129 μM
Compound: kaempferide
Inhibition of recombinant human TNF-alpha-induced cytotoxicity of mouse L929 cells assessed as survivality preincubated for 15 mins before TNFalpha addition measured after 24 hrs by crystal violet staining
Inhibition of recombinant human TNF-alpha-induced cytotoxicity of mouse L929 cells assessed as survivality preincubated for 15 mins before TNFalpha addition measured after 24 hrs by crystal violet staining
[PMID: 9287415]
L929 EC50
140 μM
Compound: kaempferide
Inhibition of recombinant human TNF-alpha-induced cytotoxicity of mouse L929 cells assessed as survivality preincubated for 15 mins before TNFalpha addition measured after 24 hrs by [methyl-3H]thymidine incorporation assay
Inhibition of recombinant human TNF-alpha-induced cytotoxicity of mouse L929 cells assessed as survivality preincubated for 15 mins before TNFalpha addition measured after 24 hrs by [methyl-3H]thymidine incorporation assay
[PMID: 9287415]
Monocyte IC50
5.7 μM
Compound: kaempferide
Inhibition of procoagulant activity in monocyte from human blood assessed as counteraction of IL1-induced tissue factor expression after 18 hrs
Inhibition of procoagulant activity in monocyte from human blood assessed as counteraction of IL1-induced tissue factor expression after 18 hrs
[PMID: 8882428]
体外研究
(In Vitro)

Kaempferid 在 HCC 细胞系中具有细胞毒性 (HepG2:IC50 = 27.94 µM; Huh7: IC50 = 25.65  µM; N1S1: IC50 = 15.18  µM)[1]
Kaempferid (5, 20 μM; 48 h) 在 HepG2 细胞中减轻 oral acid (OA) (0.5 mM) (HY-N1446) 诱导的细胞脂质积累和氧化应激[2]
Kaempferide 通过 FoxO1/β-catenin 信号通路来促进成骨[3]
Kaempferide (10-15 μM; 24 h) 在 HeLa 细胞中具有细胞毒性 IC50 为 16 μM,且可以诱导细胞凋亡[6]

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

Western Blot Analysis[2]

Cell Line: HepG2
Concentration: 5 μM, 10 μM, 20 μM . Before treatment with OA (HY-N1446) (0.5 mM; 48 h)
Incubation Time: 48 h
Result: Lowered the expression of proteins related to fat production, including sterol regulatory element-binding protein 1 (SREBP1), fatty acid synthase (FAS), and stearoyl-CoA desaturase 1 (SCD-1).
Reduced the expression of two adipogenic transcription factors, peroxisome proliferator-activated receptor gamma (PPARγ) and CCAAT enhancer-binding protein β (C/EBPβ).
Enhanced the expression of heme oxygenase-1 (HO-1) and nuclear factor erythroid 2-related factor 2 (Nrf2).
体内研究
(In Vivo)

Kaempferid (25 mg/kg; 静脉注射; 一周三次) 在 SD (Sprague Dawley) 大鼠中具有抗癌活性[1]
Kaempferide (10 mg/kg; 日食喂养,一天一次连续 16 周) 在肥胖 C57BL/6J 小鼠中通过抑制 TLR4/i-κBα/NF-κB 通路来改善氧化应激和炎症,并且可以缓解小鼠的肥胖和糖脂代谢紊乱[4]
Kaempferide (0.1-0.3 mg/kg; 注射; 单剂量) 在缺血/再灌注 (I/R) 诱导的 SD (Sprague Dawley) 大鼠中通过激活 PI3K/Akt/GSK-3β 通路来缓解心肌缺血/再灌注损伤[5]

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

Animal Model: High-fat diet male C57BL/6J mice model[4]
Dosage: 10 mg/kg
Administration: Supplemented in daily diet, once daily for16 weeks
Result: Reduced the weight, organ weight, and index of mice.
Lowered the levels of glycolipids in mouse serum.
Decreased the expression levels of inflammatory-related genes, including NF-κB, IL-6, ICAM-1, VCAM-1, and TNF-α.
Animal Model: Ischemia/Reperfusion (I/R) SD rat model[5].
Dosage: 0.1 mg/kg, 0.3 mg/kg, 3 mg/kg
Administration: Injection, Single dose. Before the I/R injury induced by Coronary Artery Ligation (CAL) in SD rats.
Result: Significantly improved heart function, reduced myocardial injury by reducing myocardial enzyme levels, and dose-dependently reduced the area of myocardial infarction in rats.
Significantly decreased serum levels of TNF-α, IL-6, C-reactive protein (CRP), MDA, and ROS, while increasing serum levels of SOD.
Downregulated the expression levels of nuclear factor erythroid 2-related factor 2 (Nrf2) and cleaved caspase-3, and upregulated the phosphorylation expression levels of phospho-Akt (p-Akt) and phospho-glycogen synthase kinase-3β (p-GSK-3β).
分子量

300.26

Formula

C16H12O6

CAS 号
性状

固体

颜色

Light yellow to yellow

中文名称

山奈素;莰非醇

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 20 mg/mL (66.61 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 3.3304 mL 16.6522 mL 33.3045 mL
5 mM 0.6661 mL 3.3304 mL 6.6609 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;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 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 mg/mL (6.66 mM); 悬浊液; 超声助溶

    此方案可获得 2 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 20.0 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)。
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: 99.35%

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;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3304 mL 16.6522 mL 33.3045 mL 83.2612 mL
5 mM 0.6661 mL 3.3304 mL 6.6609 mL 16.6522 mL
10 mM 0.3330 mL 1.6652 mL 3.3304 mL 8.3261 mL
15 mM 0.2220 mL 1.1101 mL 2.2203 mL 5.5507 mL
20 mM 0.1665 mL 0.8326 mL 1.6652 mL 4.1631 mL
25 mM 0.1332 mL 0.6661 mL 1.3322 mL 3.3304 mL
30 mM 0.1110 mL 0.5551 mL 1.1101 mL 2.7754 mL
40 mM 0.0833 mL 0.4163 mL 0.8326 mL 2.0815 mL
50 mM 0.0666 mL 0.3330 mL 0.6661 mL 1.6652 mL
60 mM 0.0555 mL 0.2775 mL 0.5551 mL 1.3877 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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