1. Anti-infection Metabolic Enzyme/Protease NF-κB Cell Cycle/DNA Damage
  2. Parasite Tyrosinase NF-κB CDK
  3. Kojic acid

Kojic acid  (Synonyms: 曲酸)

目录号: HY-W050154 纯度: 99.99%
COA 产品使用指南

Kojic acid 是由 Aspergillus oryzae 产生的物质,具有口服有效性,也可被透皮吸收。Kojic acid 具有抗衰老、抗线虫、抗菌、抗氧化、抗炎等多种生物活性。Kojic acid 是Tyrosinase抑制剂,对 Mushroon Tyrosinase IC50 为 182.7 μM。Kojic acid 通过捕获与酪氨酸酶活性位点结合的铜离子防止其激活来阻止黑色素产生。Kojic acid 对人角质形成细胞中 NF-κBp21 信号通路具有抑制作用。Kojic acid 衍生物具有抗肿瘤活性。

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Kojic acid Chemical Structure

Kojic acid Chemical Structure

CAS No. : 501-30-4

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Other Forms of Kojic acid:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Kojic acid is a substance produced by Aspergillus oryzae that is orally effective and can also be absorbed transdermally. Kojic acid exhibits various biological activities, including anti-aging, anti-nematode, antimicrobial, antioxidant, and anti-inflammatory effects. Kojic acid is a Tyrosinase inhibitor with an Mushroom Tyrosinase IC50 of 182.7 μM. Kojic acid prevents melanin production by capturing copper ions that bind to the tyrosinase active site, thus inhibiting its activation. Kojic acid also suppresses the NF-κB and p21 signaling pathways in human keratinocytes. Kojic acid derivatives have anticancer activity[1][2][3][4][5][6][7][8].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A-375 GI50
> 100 μM
Compound: 1; KA
Cytotoxicity against human A-375 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human A-375 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 35114540]
B16 IC50
> 50 μM
Compound: Kojic acid
Inhibition of alpha-MSH-induced melanin production in mouse B16 cells after 48 hrs
Inhibition of alpha-MSH-induced melanin production in mouse B16 cells after 48 hrs
[PMID: 20149498]
B16 IC50
> 500 μM
Compound: Kojic acid
Inhibition of alpha-MSH-stimulated melanin production in mouse B16 cells after 72 hrs by microplate reader analysis
Inhibition of alpha-MSH-stimulated melanin production in mouse B16 cells after 72 hrs by microplate reader analysis
[PMID: 26706112]
B16 IC50
111 μM
Compound: Kojic acid
Antimelanogenic activity in mouse B16 cells assessed as inhibition of intracellular melanin accumulation after 2 days
Antimelanogenic activity in mouse B16 cells assessed as inhibition of intracellular melanin accumulation after 2 days
[PMID: 19524439]
B16 IC50
15.8 μM
Compound: Kojic acid
Inhibition of alpha-MSH -stimulated melanogenesis in mouse B16 cells assessed as melanin release after 72 hrs by spectrometric analysis
Inhibition of alpha-MSH -stimulated melanogenesis in mouse B16 cells assessed as melanin release after 72 hrs by spectrometric analysis
[PMID: 21978680]
B16 IC50
39 μM
Compound: Kojic acid
Inhibition of melanin production in alpha-MSH stimulated mouse B16 cells after 72 hrs by spectrophotometry
Inhibition of melanin production in alpha-MSH stimulated mouse B16 cells after 72 hrs by spectrophotometry
[PMID: 23623417]
B16 IC50
5.5 μg/mL
Compound: Kojic acid
Inhibition of alpha-MSH-stimulated melanogenesis in mouse B16 cells assessed as melanin release after 72 hrs
Inhibition of alpha-MSH-stimulated melanogenesis in mouse B16 cells assessed as melanin release after 72 hrs
[PMID: 22450129]
B16 IC50
70 μM
Compound: Kojic acid
Antimelanogenic activity at alpha-MSH-stimulated mouse melanoma B16 cells after 3 days by spectrophotometry
Antimelanogenic activity at alpha-MSH-stimulated mouse melanoma B16 cells after 3 days by spectrophotometry
[PMID: 22217872]
B16 IC50
70 μM
Compound: Kojic acid
Inhibition of alpha-MSH-induced melanin production in mouse B16 cells after 3 days
Inhibition of alpha-MSH-induced melanin production in mouse B16 cells after 3 days
[PMID: 21601449]
B16 IC50
70 μM
Compound: kojic acid
Inhibition of alpha-MSH-induced melanin production in mouse B16 cells after 72 hrs
Inhibition of alpha-MSH-induced melanin production in mouse B16 cells after 72 hrs
[PMID: 20097083]
B16 IC50
70 μM
Compound: Kojic acid
Inhibition of alpha-MSH-induced melanin production in mouse B16 cells after 72 hrs
Inhibition of alpha-MSH-induced melanin production in mouse B16 cells after 72 hrs
[PMID: 20044259]
B16-F10 IC50
144.4 μM
Compound: 1a; KA
Cytotoxicity against mouse B16-F10 cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against mouse B16-F10 cells assessed as reduction in cell viability by MTT assay
[PMID: 32652434]
B16-F10 IC50
500 μM
Compound: Kojic acid
Antimelanogenic activity in mouse B16F10 cells assessed as inhibition of melanin production after 4 days
Antimelanogenic activity in mouse B16F10 cells assessed as inhibition of melanin production after 4 days
[PMID: 25597012]
B16-F10 IC50
84.54 μM
Compound: Kojic acid
Inhibition of alpha-MSH-induced melanogenesis in mouse B16F10 cells after 3 days by spectrophotometric analysis
Inhibition of alpha-MSH-induced melanogenesis in mouse B16F10 cells after 3 days by spectrophotometric analysis
[PMID: 23063404]
BV-2 IC50
> 500 μM
Compound: KA
Cytotoxicity against mouse BV-2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytotoxicity against mouse BV-2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
[PMID: 36846369]
G-361 IC50
571.17 μM
Compound: Kojic acid
Competitive inhibition of tyrosinase in human G-361 cells incubated for 10 mins measured for 2 hrs by MBTH-based spectrophotometry
Competitive inhibition of tyrosinase in human G-361 cells incubated for 10 mins measured for 2 hrs by MBTH-based spectrophotometry
[PMID: 25288494]
H9c2 IC50
> 500 μM
Compound: KA
Cytotoxicity against rat H9c2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytotoxicity against rat H9c2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
[PMID: 36846369]
HEK293 IC50
2 μM
Compound: 6a, Kojic acid
Inhibition of human recombinant DAAO expressed in HEK293 cell lysate assessed as D-Serine conversion to H2O2 after 20 mins by spectrophotometric analysis
Inhibition of human recombinant DAAO expressed in HEK293 cell lysate assessed as D-Serine conversion to H2O2 after 20 mins by spectrophotometric analysis
[PMID: 23683589]
HFF IC50
> 150 μM
Compound: 1a; KA
Cytotoxicity against human HFF cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against human HFF cells assessed as reduction in cell viability by MTT assay
[PMID: 32652434]
HT-22 IC50
> 500 μM
Compound: KA
Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
[PMID: 36846369]
L02 IC50
> 500 μM
Compound: KA
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
[PMID: 36846369]
Melan-a IC50
1.6 mM
Compound: 1
Depigmentation activity in mouse Melan-a cells assessed as inhibition of melanin formation after 4 days
Depigmentation activity in mouse Melan-a cells assessed as inhibition of melanin formation after 4 days
[PMID: 22071299]
Melan-a IC50
1.64 mM
Compound: 1, Kojic acid
Depigmentation activity in mouse Melan-a cells after 4 days by spectrophotometry
Depigmentation activity in mouse Melan-a cells after 4 days by spectrophotometry
[PMID: 22579419]
Melan-a IC50
3.5 mM
Compound: 1
Cytotoxicity against mouse Melan-a cells by modified crystal voilet assay
Cytotoxicity against mouse Melan-a cells by modified crystal voilet assay
[PMID: 22071299]
Melan-a IC50
3.53 mM
Compound: 1, Kojic acid
Cytotoxicity against mouse Melan-a cells after 4 days by crystal voilet method
Cytotoxicity against mouse Melan-a cells after 4 days by crystal voilet method
[PMID: 22579419]
RAW264.7 IC50
> 100 μM
Compound: 1
Cytotoxicity against mouse RAW264.7 cells after 24 hrs by MTT assay
Cytotoxicity against mouse RAW264.7 cells after 24 hrs by MTT assay
[PMID: 20934336]
RAW264.7 IC50
89.41 μM
Compound: 1
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production treated for 30 mins before LPS challenge measured after 24 hrs by Griess reagent method
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production treated for 30 mins before LPS challenge measured after 24 hrs by Griess reagent method
[PMID: 20934336]
SH-SY5Y IC50
> 500 μM
Compound: KA
Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
[PMID: 36846369]
体外研究
(In Vitro)

Kojic acid (1000 μM,7 天) 增强 HCEC 细胞的细胞迁移能力,并对其具有抗衰老活性[1]
Kojic acid (1000 μM, 7 天) 可能通过 NF-κB 和 p21 信号通路缓解由衰老的 HCEC 细胞的上清液诱导的人脐静脉内皮细胞 (HUVEC) 血管生成[1]
Kojic acid (1.4-1000 μg/mL,3天) 对 M. incognita 表现出剂量依赖性的致死率和孵化抑制率,EC50 分别为 195.2 μg/mL 和 238.3 μg/mL[4]
Kojic acid (1000 μM,2-6 天) 以浓度依赖的方式抑制 B16-4A5 细胞和 HMV-II 细胞中的黑色素生成[6]
Kojic acid (500 或 1000 µM,72 小时) 降低了 B16-4A5 细胞 HMV-II 细胞中和酪氨酸酶表达,表明 Kojic acid 由于抑制酪氨酸酶活性而抑制黑色素生成[6]
Kojic acid (10-2500 μM,7 天) 对 HCEC 细胞活力无显著影响[1]

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

Cell Viability Assay[1]

Cell Line: HCEC-B4G12 cells (human corneal endothelial cell line)
Concentration: 10, 100 , 1000, 2500, 5000 μM
Incubation Time: 7 days
Result: Did not influence the cell viability of HCEC after 7 days' treatment at 10-2500 μM but decreased the cell viability a little bit at 5000 μM.

Cell Migration Assay [1]

Cell Line: HCEC-B4G12 cells (human corneal endothelial cell line)
Concentration: 1000 μM
Incubation Time: 7 days
Result: Delayed the reduction in cell migration ability caused by aging in HCEC cells.

Western Blot Analysis[1]

Cell Line: HCEC-B4G12 cells (human corneal endothelial cell line)
Concentration: 1000 μM
Incubation Time: 7 days
Result: Inhibited the abnormal high expression of galectin 8, laminin α1, laminin α2, laminin γ1, and p21 in senescent HCEC, as well as the significant decrease in p-NF-κB protein expression.
体内研究
(In Vivo)

Kojic acid (50 mg/kg,口服,1 天 1 次连续 3 周) 对 β-Amyloid (1-42), human (HY-P1363A) 诱导的阿尔兹海默症小鼠模型具有抗氧化和抗炎活性[8]
Kojic acid (4, 6.4, 10, 16 g/kg, 口服, 单次给药) 在急性口服实验中对 JCL-Wistar 大鼠的毒性较小[2]

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

Animal Model: β-Amyloid (1-42), human (HY-P1363A)-Induced Mouse Model of Alzheimer's Disease[8]
Dosage: 50 mg/kg
Administration: Oral gavage, once daily for 3 weeks
Result: Ameliorated β-Amyloid (1-42), human (HY-P1363A)-induced glial cell activation and reduced inflammatory markers in the hippocampus.
Reduced ROS and lipid peroxidase levels in Alzheimer's Disease mice model
Animal Model: JCL-Wistar rats[2]
Dosage: 4, 6.4, 10, 16 g/kg
Administration: Oral gavage (p.o.),single dose
Result: Had an oral LD50 in rats greater than 2 g/kg in acute toxicity studies[2].
分子量

142.11

Formula

C6H6O4

CAS 号
性状

固体

颜色

Off-white to light yellow

中文名称

曲酸

结构分类
初始来源

Aspergillus, Penicillium or Acetobacter spp

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 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 100 mg/mL (703.68 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : 50 mg/mL (351.84 mM; 超声助溶)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 7.0368 mL 35.1840 mL 70.3680 mL
5 mM 1.4074 mL 7.0368 mL 14.0736 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, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 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: 5 mg/mL (35.18 mM); 悬浊液; 超声助溶

    此方案可获得 5 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 50.0 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 (17.59 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。

    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。

以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 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: PBS

    Solubility: 14.29 mg/mL (100.56 mM); 澄清溶液; 超声助溶 (<60°C)

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
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 99.99%

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, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 7.0368 mL 35.1840 mL 70.3680 mL 175.9201 mL
5 mM 1.4074 mL 7.0368 mL 14.0736 mL 35.1840 mL
10 mM 0.7037 mL 3.5184 mL 7.0368 mL 17.5920 mL
15 mM 0.4691 mL 2.3456 mL 4.6912 mL 11.7280 mL
20 mM 0.3518 mL 1.7592 mL 3.5184 mL 8.7960 mL
25 mM 0.2815 mL 1.4074 mL 2.8147 mL 7.0368 mL
30 mM 0.2346 mL 1.1728 mL 2.3456 mL 5.8640 mL
40 mM 0.1759 mL 0.8796 mL 1.7592 mL 4.3980 mL
50 mM 0.1407 mL 0.7037 mL 1.4074 mL 3.5184 mL
60 mM 0.1173 mL 0.5864 mL 1.1728 mL 2.9320 mL
80 mM 0.0880 mL 0.4398 mL 0.8796 mL 2.1990 mL
100 mM 0.0704 mL 0.3518 mL 0.7037 mL 1.7592 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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产品名称:
Kojic acid
目录号:
HY-W050154
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