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Phloretin
在苹果中发现的二氢查耳酮,Phloretin(NSC 407292; RJC 02792)是天然多酚,能抑制通过SGLT1、SGLT2和GLUT1的葡萄糖转运。
目录号: PC10640 纯度: ≥98%
CAS No. :60-82-2
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中文名称
Phloretin
中文别名
根皮素;2',4',6'-三羟基-3-(4-羟基苯基)苯丙酮;三羟苯酚丙酮;根皮酸苯三酚一酯;Phloretin 根皮素;根皮苷;根皮素 标准品;根皮素(标准品);根皮素,Phloretin,植物提取物,标准品,对照品;根皮素Phloretin;三羟苯酚丙酮对照品;3-(4-羟苯基)-1-(2,4,6-三羟基苯基)-1-丙酮;根皮素(根皮酸苯三酚一酯,三羟苯酚丙酮);根皮素, 三羟苯酚丙酮
英文名称
Phloretin
英文别名
Phloretin;2',4',6',4-TETRAHYDROXYDIHYDROCHALCONE;2',4',6'-TRIHYDROXY-3-(4-HYDROXYPHENYL)-1-PROPIOPHENONE;2',4',6'-TRIHYDROXY-3-(4-HYDROXYPHENYL)-PROPIOPHENONE;2',4',6'-TRIHYDROXY-3-P-HYDROXYPHENYLPROPIOPHENONE;2,4,6-TRIHYDROXY-BETA-(4-HYDROXYPHENYL)PROPIOPHENONE;3-[4-HYDROXYPHENYL]-1-[2,4,6-TRIHYDROXYPHENYL]-1-PROPANONE;4,2',4',6'-TETRAHYDROXYDIHYDROCHALCONE;BETA-(4-HYDROXYPHENYL)-2,4,6-TRIHYDROXY-PROPIOPHENONE;PHLORETIN (NATURAL);3-(4-hydroxyphenyl)-1-(2,4,6-trihydroxyphenyl)propan-1-one;2,4,6-Trihydroxy-B-(4-Hydroxyphenyl)Propiophenone;β-(4-hydroxyphenyl)-2,4,6-trihydroxypropiophenone;PHLORETIN(RG);1-Propanone, 3-(4-hydroxyphenyl)-1-(2,4,6-;Dihydronaringenin;Floretin;NSC 407292;Phloretol;RJC 02792;UNII-S5J5OE47MK;2′,4′,6′-Trihydroxy-3-(4-hydroxyphenyl)propiophenone;3-(4-Hydroxyphenyl)-1-(2,4,6-trihydroxyphenyl)-1-propanone;2',4',6'-Trihydroxy-3-(4-hydroxyphenyl)propiophenone;[ "" ];1-Propanone, 3-(4-hydroxyphenyl)-1-(2,4,6-trihydroxyphenyl)-;beta-(p-Hydroxyphenyl)phloropropiophenone;2',4',6'-Trihydroxy-3-(p-hydroxyphenyl)propiophenone;NSC407292;S5J5OE47MK;beta-(p-Hydroxyphenyl)-2,4,6-trihydrox
Cas No.
60-82-2
分子式
C15H14O5
分子量
274.27
包装储存
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
生物活性

Phloretin (NSC 407292; RJC 02792) is a flavonoid extracted from Malus pumila Mill., has anti-inflammatory activities. Phloridzin is a specific, competitive and orally active inhibitor of sodium/glucose cotransporters in the intestine (SGLT1) and kidney (SGLT2). Phloretin inhibits Yeast-made GLUT1 as well as Human erythrocyte GLUT1 with IC50values of 49 μM and 61 μM, respectively.Phloretin has the potential for the treatment of rheumatoid arthritis (RA) and allergic airway inflammation.

性状

Solid

IC50 & Target[1][2]

Human Endogenous Metabolite

 

Microbial Metabolite

 

GLUT1

 

GLUT2

 

体外研究(In Vitro)

Phloretin induced obvious cytotoxicity against BEL-7402 cells with IC50 of 89.23 μM.
Phloretin (40-160 μM; 24 hours) induces BEL-7402 cell apoptosis though the mitochondrial pathway, the cells exposed to phloretin exhibits nuclear chromatin condensation and increased fluorescence intensity. The caspase-9 reaches the peak level at 12 h, and leak levels of caspase-6 and caspase-3 activities occurrs 18 and 24 h after the exposure, respectively.
Phloretin (0-100 μM; 24 hours) has effects on transcription factors of adipogenesis in differentiated 3T3-L1 adipocytes, decreases PPAR-γ, C/EBPα and C/EBPβ as a dose-dependent manner.
Phloretin (0-100 μM; 24 hours) has effects on the AMPK pathway in differentiated 3T3-L1 adipocytes, increases the phosphorylation of substrate ACC-1, AMPK in PT-treated cells.

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

Apoptosis Analysis

Cell Line: BEL-7402 cell
Concentration: 40-160 μM
Incubation Time: 24 hours
Result: Induced cell apoptosis and activated caspase 3, 6 and 9.

Western Blot Analysis

Cell Line: 3T3-L1 adipocytes
Concentration: 0 μM, 3 μM, 10 μM, 30 μM, 100 μM
Incubation Time: 24 hours
Result: Inhibited PPAR-γ, C/EBPα and C/EBPβ expression.

Western Blot Analysis

Cell Line: 3T3-L1 adipocytes
Concentration: 0 μM, 3 μM, 10 μM, 30 μM, 100 μM
Incubation Time: 24 hours
Result: Upregulated the expression of p-ACC-1, p-AMPK, p-AMPKα and β .
体内研究(In Vivo)

Phloretin (oral administration; 50 or 100?mg/kg; once daily) decreases oxidative stress and diminished levels of malondialdehyde (MDA) and hydrogen peroxide (H2O2) in paw tissue, reduces productivity of anti-collagen antibodies in serum.

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

Animal Model: Collagen-Induced Arthritis (CIA) Mice
Dosage: 50 or 100?mg/kg
Administration: Oral adminstration
Result: Showed mitigation of clinical symptoms of RA in addition to reduced inflammation of hind-limbs compared to the control group.
运输条件

Room temperature or refrigerated transportation.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
结构分类
来源
参考文献
溶解度数据
体外研究: 

DMSO : 50 mg/mL (182.30 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (ultrasonic) (insoluble)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6460 mL 18.2302 mL 36.4604 mL
5 mM 0.7292 mL 3.6460 mL 7.2921 mL
10 mM 0.3646 mL 1.8230 mL 3.6460 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,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,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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

  • 1.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (9.12 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.12 mM,饱和度未知) 的澄清溶液。

    以 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;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
  • 2.

    建议依照次序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (9.12 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.12 mM,饱和度未知) 的澄清溶液。

    以 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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    建议依照次序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.12 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.12 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 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玉米油中,混合均匀。

*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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