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  2. Membrane Transporter/Ion Channel Metabolic Enzyme/Protease
  3. SGLT Endogenous Metabolite GLUT
  4. Phloretin

Phloretin  (Synonyms: 根皮素; NSC 407292; RJC 02792)

目錄號: HY-N0142 純度: 99.67%
COA 產(chǎn)品使用指南

Phloretin (NSC 407292; RJC 02792) 是一種從蘋果中提取的黃酮類化合物，具有抗炎活性。Phloridzin 是一種特異性、競爭性和口服活性的鈉/葡萄糖協(xié)同轉(zhuǎn)運(yùn)蛋白 (sodium/glucose cotransporters) 抑制劑，在腸道 (SGLT1) 和腎臟 (SGLT2)。Phloretin 抑制 Yeast-made GLUT1 以及人類紅細(xì)胞 GLUT1 的 IC50 值分別為 49 μM 和 61 μM。Phloretin 具有潛力用于類風(fēng)濕性關(guān)節(jié)炎 (RA) 和過敏性氣道炎癥的相關(guān)研究。

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Phloretin Chemical Structure

Phloretin Chemical Structure

CAS No. : 60-82-2

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥500
In-stock
250 mg ￥400
In-stock
500 mg ￥515
In-stock
1 g   詢價  
5 g   詢價  

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  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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[1].Phloretin has the potential for the treatment of rheumatoid arthritis (RA)?and allergic airway inflammation[4].

IC50 & Target[1]

SGLT1

 

SGLT2

 

Microbial Metabolite

 

GLUT1

 

GLUT2

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
12.4 μM
Compound: 9h
Inhibition of human SGLT1 expressed in HEK293 cells assessed as reduction in 2-deoxyglucose uptake pretreated for 10 mins followed by 2-deoxyglucose addition in presence of sodium buffer measured after 1 hr by resazurin dye based fluorescence assay
Inhibition of human SGLT1 expressed in HEK293 cells assessed as reduction in 2-deoxyglucose uptake pretreated for 10 mins followed by 2-deoxyglucose addition in presence of sodium buffer measured after 1 hr by resazurin dye based fluorescence assay
[PMID: 28098449]
HEK293 IC50
18.3 μM
Compound: 9h
Inhibition of human SGLT2 expressed in HEK293 cells assessed as reduction in 2-deoxyglucose uptake pretreated for 10 mins followed by 2-deoxyglucose addition in presence of sodium buffer measured after 1 hr by resazurin dye based fluorescence assay
Inhibition of human SGLT2 expressed in HEK293 cells assessed as reduction in 2-deoxyglucose uptake pretreated for 10 mins followed by 2-deoxyglucose addition in presence of sodium buffer measured after 1 hr by resazurin dye based fluorescence assay
[PMID: 28098449]
HEK293 IC50
90 μM
Compound: 4788
Inhibition of the Sodium/Hydrogen Exchanger-Like Domain-Containing Protein 2 (NHA2, SLC9B2) as assessed by a sensor pH-sensitive genetically encoded fluorescent sensor (pHAxensor) in HEK-293 cells stably transfected with SLC9B2
Inhibition of the Sodium/Hydrogen Exchanger-Like Domain-Containing Protein 2 (NHA2, SLC9B2) as assessed by a sensor pH-sensitive genetically encoded fluorescent sensor (pHAxensor) in HEK-293 cells stably transfected with SLC9B2
10.5281/zenodo.7360521
K562 IC50
41 μM
Compound: Phloretin
Inhibition of NF-kappaB transactivation in TNF-alpha-stimulated human K562 cells preincubated for 2 hrs followed by TNF-alpha challenge measured after 6 hrs by dual luciferase reporter gene assay
Inhibition of NF-kappaB transactivation in TNF-alpha-stimulated human K562 cells preincubated for 2 hrs followed by TNF-alpha challenge measured after 6 hrs by dual luciferase reporter gene assay
[PMID: 24775915]
MCF7 IC50
> 10 μM
Compound: 5b
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 26690274]
MCF7 IC50
7 μM
Compound: Phloretin
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 6 days by SRB assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 6 days by SRB assay
[PMID: 33257172]
MDA-MB-231 IC50
> 10 μM
Compound: 5b
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 26690274]
NCI-H1299 IC50
54 μM
Compound: Phloretin
Cytotoxicity against human H1299 cells assessed as growth inhibition after 48 hrs by MTT assay
Cytotoxicity against human H1299 cells assessed as growth inhibition after 48 hrs by MTT assay
[PMID: 24200808]
Vero IC50
125 μg/mL
Compound: 31
Cytotoxicity against African green monkey Vero cells assessed as inhibition of cell growth after 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as inhibition of cell growth after 72 hrs by MTT assay
[PMID: 22169259]
Vero CC50
735.47 μg/mL
Compound: 31
Cytotoxicity against african green monkey Vero cells assessed as cell death after 72 hrs by MTT assay
Cytotoxicity against african green monkey Vero cells assessed as cell death after 72 hrs by MTT assay
[PMID: 22169259]
體外研究
(In Vitro)

Phloretin 對 BEL-7402 細(xì)胞具有明顯的細(xì)胞毒性，IC50 為 89.23 μM[2]。
Phloretin (40-160 μM；24 hours) 誘導(dǎo) BEL-7402 細(xì)胞通過線粒體途徑發(fā)生凋亡，暴露于 Phloretin 的細(xì)胞表現(xiàn)出核染色質(zhì)濃縮和熒光強(qiáng)度增加。在 12 h 達(dá)到 caspase-9 的峰值，分別在暴露后 18 和 24 h 發(fā)生 caspase-6 和 caspase-3 leak 值[2]。
(0-100 μM；24 小時) 對分化的 3T3-L1 脂肪細(xì)胞中脂肪形成的轉(zhuǎn)錄因子有影響，以劑量依賴方式降低 PPAR-γ、C/EBPα 和 C/EBPβ[3]。
Phloretin (0-100 μM；24 小時) 對分化的 3T3-L1 脂肪細(xì)胞中的 AMPK 通路有影響，增加 PT 處理細(xì)胞中底物 ACC-1、AMPK 的磷酸化[3]。

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

Apoptosis Analysis[2]

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[3]

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[3]

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 .
體內(nèi)研究
(In Vivo)

Phloretin (口服給藥；50 或 100 mg/kg；每天一次) 降低爪組織中的氧化應(yīng)激和丙二醛 (MDA) 和過氧化氫 (H2O2) 的水平，降低血清中抗膠原抗體的生產(chǎn)率[3]。

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

Animal Model: Collagen-Induced Arthritis (CIA) Mice[3]
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.
分子量

274.27

Formula

C15H14O5
CAS 號
性狀

固體

顏色

Off-white to pink

中文名稱

根皮素
結(jié)構(gòu)分類
初始來源
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 50 mg/mL (182.30 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制儲備液
濃度 溶劑體積 質(zhì)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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲存時，請?jiān)?年內(nèi)使用， -20°C儲存時，請?jiān)?個月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物實(shí)驗(yàn)：

請根據(jù)您的 實(shí)驗(yàn)動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.12 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.12 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
動物溶解方案計(jì)算器
請輸入動物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲備液濃度超過該產(chǎn)品的實(shí)測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
動物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.67%

參考文獻(xiàn)

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲存時，請?jiān)?年內(nèi)使用， -20°C儲存時，請?jiān)?個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.6460 mL 18.2302 mL 36.4604 mL 91.1511 mL
5 mM 0.7292 mL 3.6460 mL 7.2921 mL 18.2302 mL
10 mM 0.3646 mL 1.8230 mL 3.6460 mL 9.1151 mL
15 mM 0.2431 mL 1.2153 mL 2.4307 mL 6.0767 mL
20 mM 0.1823 mL 0.9115 mL 1.8230 mL 4.5576 mL
25 mM 0.1458 mL 0.7292 mL 1.4584 mL 3.6460 mL
30 mM 0.1215 mL 0.6077 mL 1.2153 mL 3.0384 mL
40 mM 0.0912 mL 0.4558 mL 0.9115 mL 2.2788 mL
50 mM 0.0729 mL 0.3646 mL 0.7292 mL 1.8230 mL
60 mM 0.0608 mL 0.3038 mL 0.6077 mL 1.5192 mL
80 mM 0.0456 mL 0.2279 mL 0.4558 mL 1.1394 mL
100 mM 0.0365 mL 0.1823 mL 0.3646 mL 0.9115 mL
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產(chǎn)品名稱：
Phloretin
目錄號：
HY-N0142
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