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  2. Membrane Transporter/Ion Channel
  3. SGLT Na+/K+ ATPase
  4. Phlorizin

Phlorizin  (Synonyms: 根皮苷; Floridzin)

目錄號: HY-N0143 純度: 99.93%
COA 產(chǎn)品使用指南

Phlorizin (Floridzin) 是一種非選擇性的 SGLT 抑制劑，對于 hSGLT1 和 hSGLT2 的 Ki 值分別為 300 和 39 nM。Phlorizin 也是一個 Na+/K+-ATPase 抑制劑。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報，我們不為任何個人用途提供產(chǎn)品和服務(wù)

Phlorizin Chemical Structure

Phlorizin Chemical Structure

CAS No. : 60-81-1

1.  客戶無需承擔(dān)相應(yīng)的運輸費用。

2.  同一機構(gòu)（單位）同一產(chǎn)品試用裝僅限申領(lǐng)一次，同一機構(gòu)（單位）一年內(nèi)

     可免費申領(lǐng)三個不同產(chǎn)品的試用裝。

3.  試用裝只面向終端客戶。

規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥500
In-stock
500 mg ￥400
In-stock
1 g ￥500
In-stock
5 g ￥1100
In-stock
10 g   詢價  
50 g   詢價  

* Please select Quantity before adding items.

Customer Review

Other Forms of Phlorizin:

查看 SGLT 亞型特異性產(chǎn)品:

  • 生物活性

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Phlorizin (Floridzin) is a non-selective SGLT inhibitor with Kis of 300 and 39 nM for hSGLT1 and hSGLT2, respectively. Phlorizin is also a Na+/K+-ATPase inhibitor.

IC50 & Target

SGLT1

 

SGLT2

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
108 nM
Compound: 1
Inhibition of human SGLT2 expressed in CHO cells assessed as sodium-dependent [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting
Inhibition of human SGLT2 expressed in CHO cells assessed as sodium-dependent [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting
[PMID: 21128592]
CHO IC50
16 nM
Compound: 1
Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]AMG uptake after 45 mins
Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]AMG uptake after 45 mins
[PMID: 21873071]
CHO IC50
16.4 nM
Compound: 1
Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]methyl-alpha-D-glucopyranoside uptake after 45 mins
Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]methyl-alpha-D-glucopyranoside uptake after 45 mins
[PMID: 22889351]
CHO IC50
185 nM
Compound: 1
Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]methyl-alpha-D-glucopyranoside uptake after 45 mins
Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]methyl-alpha-D-glucopyranoside uptake after 45 mins
[PMID: 22889351]
CHO IC50
190 nM
Compound: 1
Inhibition of human SGLT1 expressed in CHO cells assessed as [14C]AMG uptake after 45 mins
Inhibition of human SGLT1 expressed in CHO cells assessed as [14C]AMG uptake after 45 mins
[PMID: 21873071]
CHO EC50
197.4 nM
Compound: 1
Inhibition of human SGLT1 expressed in CHO cells assessed as sodium-dependent [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting
Inhibition of human SGLT1 expressed in CHO cells assessed as sodium-dependent [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting
[PMID: 21128592]
CHO IC50
752 nM
Compound: 1
Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]alpha-methyl-D-glucopyranoside uptake by fluorescence polarization assay
Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]alpha-methyl-D-glucopyranoside uptake by fluorescence polarization assay
[PMID: 18755586]
CHO-K1 EC50
0.077 μM
Compound: 1
Inhibition of human SGLT2 expressed in CHO-K1 cells assessed as inhibition of [14C]-AMG uptake up to 120 mins by scintillation counting method
Inhibition of human SGLT2 expressed in CHO-K1 cells assessed as inhibition of [14C]-AMG uptake up to 120 mins by scintillation counting method
[PMID: 24071445]
CHO-K1 EC50
0.12 μM
Compound: 1
Inhibition of human SGLT1 expressed in CHO-K1 cells assessed as inhibition of [14C]-AMG uptake up to 120 mins by scintillation counting method
Inhibition of human SGLT1 expressed in CHO-K1 cells assessed as inhibition of [14C]-AMG uptake up to 120 mins by scintillation counting method
[PMID: 24071445]
CHO-K1 EC50
123 nM
Compound: PZN
Inhibition of human SGLT2 expressed in CHO-K1 cells assessed as reduction in [14C]AMG uptake after 120 mins by scintillation counting method
Inhibition of human SGLT2 expressed in CHO-K1 cells assessed as reduction in [14C]AMG uptake after 120 mins by scintillation counting method
[PMID: 27075813]
CHO-K1 EC50
153 nM
Compound: PZN
Inhibition of human SGLT1 expressed in CHO-K1 cells assessed as reduction in [14C]AMG uptake after 120 mins by scintillation counting method
Inhibition of human SGLT1 expressed in CHO-K1 cells assessed as reduction in [14C]AMG uptake after 120 mins by scintillation counting method
[PMID: 27075813]
CHO-K1 IC50
16 nM
Compound: Phlorizin
Inhibition of human SGLT2 expressed in CHO-K1 cells by [14C]AMG uptake assay
Inhibition of human SGLT2 expressed in CHO-K1 cells by [14C]AMG uptake assay
[PMID: 22652255]
CHO-K1 IC50
190 nM
Compound: Phlorizin
Inhibition of human SGLT1 expressed in CHO-K1 cells by [14C]AMG uptake assay
Inhibition of human SGLT1 expressed in CHO-K1 cells by [14C]AMG uptake assay
[PMID: 22652255]
COS-1 IC50
0.1 mM
Compound: Phlorizine
Inhibition of alpha-D-[U-14C]glucopyranoside uptake at human SGLT2 expressed in african green monkey COS1 cells after 30 mins by liquid scintillation counting
Inhibition of alpha-D-[U-14C]glucopyranoside uptake at human SGLT2 expressed in african green monkey COS1 cells after 30 mins by liquid scintillation counting
[PMID: 20189404]
COS-1 IC50
0.2 mM
Compound: Phlorizine
Inhibition of alpha-D-[U-14C]glucopyranoside uptake at human SGLT1 expressed in african green monkey COS1 cells after 30 mins by liquid scintillation counting
Inhibition of alpha-D-[U-14C]glucopyranoside uptake at human SGLT1 expressed in african green monkey COS1 cells after 30 mins by liquid scintillation counting
[PMID: 20189404]
COS-7 IC50
> 1000 μM
Compound: phlorizin
Inhibition of human CNT2 expressed in COS7 cells assessed as reduction in sodium-dependent [14C]-inosine uptake in presence of Na+ by liquid scintillation counting method
Inhibition of human CNT2 expressed in COS7 cells assessed as reduction in sodium-dependent [14C]-inosine uptake in presence of Na+ by liquid scintillation counting method
[PMID: 25815140]
HEK293 IC50
0.0673 μM
Compound: 1
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
0.499 μM
Compound: 1
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
58.6 nM
Compound: Phlorizin
Inhibition of SGLT2 (unknown origin) expressed in HEK293 cells using 2-NBDG as substrate incubated for 30 mins prior to substrate addition measured after 30 mins by nonradioactive fluorescence glucose uptake assay
Inhibition of SGLT2 (unknown origin) expressed in HEK293 cells using 2-NBDG as substrate incubated for 30 mins prior to substrate addition measured after 30 mins by nonradioactive fluorescence glucose uptake assay
[PMID: 24556379]
HEK293 IC50
60.7 nM
Compound: Phlorizin
Inhibition of SGLT1 (unknown origin) expressed in HEK293 cells using 2-NBDG as substrate incubated for 30 mins prior to substrate addition measured after 30 mins by nonradioactive fluorescence glucose uptake assay
Inhibition of SGLT1 (unknown origin) expressed in HEK293 cells using 2-NBDG as substrate incubated for 30 mins prior to substrate addition measured after 30 mins by nonradioactive fluorescence glucose uptake assay
[PMID: 24556379]
RAW264.7 IC50
14.4 μM
Compound: 14
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha secretion after 18 hrs by sandwich ELISA
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha secretion after 18 hrs by sandwich ELISA
[PMID: 24679441]
RAW264.7 IC50
14.6 μM
Compound: 16
Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as decrease in PGE2 production preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as decrease in PGE2 production preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
[PMID: 31747281]
體外研究
(In Vitro)

Phlorizin 是一種非選擇性 SGLT 抑制劑，對 hSGLT1 和 hSGLT2 的 Ki 分別為 300 和 39 nM[1]。Phlorizin 也是一種 Na+/K+-ATPase 抑制劑[2]。2×10-4 M 的根皮苷抑制 Na+ 和 Rb+ 激活的人紅細(xì)胞膜中 43 % 的 ATP 酶活性。在 1 mM 和 7 mM RbCl 下，銣的攝取沒有改變或被 2×10-4 M 根皮苷輕微抑制 (小于 15%)[2]。根皮苷 <100 μM 的劑量不會顯著改變細(xì)胞活力。用根皮苷預(yù)處理細(xì)胞不會顯著降低亞硝酸鹽或 PGE2 水平。根皮苷不抑制 IL-6 或 TNF-α 的產(chǎn)生，但 100 μM 根皮苷可顯著抑制 TNF-α 的表達(dá)[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

在根皮苷處理之前，SDT 肥胖大鼠的血糖水平為 370±49 mg/dL。給藥后 6 小時，根皮苷處理組的血糖水平降至接近正常水平 (139±32 mg/dL)。12 周后，根皮苷處理的 SDT 肥胖大鼠比媒介物處理的 SDT 肥胖大鼠更重。根皮苷處理顯著降低葡萄糖排泄并延遲胰島素降低。根皮苷處理后肌酐清除率顯著降低。根皮苷處理 23 周可防止神經(jīng)纖維減少 (23.6±3.2 纖維/毫米)。Phlorizin[4]可完全預(yù)防視網(wǎng)膜異常。

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

436.41

Formula

C21H24O10
CAS 號
性狀

固體

顏色

White to off-white

中文名稱

根皮苷；根皮甙
結(jié)構(gòu)分類
初始來源
運輸條件

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 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實驗： 

DMSO 中的溶解度 : ≥ 50 mg/mL (114.57 mM; 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 : 1 mg/mL (2.29 mM; 超聲助溶)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.2914 mL 11.4571 mL 22.9142 mL
5 mM 0.4583 mL 2.2914 mL 4.5828 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, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

* 備注：如您選擇水作為儲備液，請稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

  • 摩爾計算器

  • 稀釋計算器

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

動物實驗：

請根據(jù)您的 實驗動物和給藥方式 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：
——為保證實驗結(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)實驗的工作液，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 (5.73 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 (5.73 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。

以下溶解方案，請直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 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： PBS

    Solubility: 1.75 mg/mL (4.01 mM); 澄清溶液; 超聲助溶 (<60°C)

  • 方案 二

    請依序添加每種溶劑： 20% HP-β-CD in Saline

    Solubility: 15.15 mg/mL (34.72 mM); 澄清溶液; 超聲助溶

動物溶解方案計算器
請輸入動物實驗的基本信息：

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
由于實驗過程有損耗，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。
動物實驗體內(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
參考文獻(xiàn)
Kinase Assay
[1]

Resealed ghosts are obtained with the addition of 4×10-3 M ATP and 5×10-3 M MgCl2 with or without 5×10-4 M Phlorizin (final concentration) when red cells are hemolyzed. Ghosts corresponding to 0.4-0.45 mL of the original blood cells are incubated with 0.9 mL of Medium A and 86RbCl for 45 or 90 min and the radioactivity in 200 μL of the supernatant is determined. The ATPase activity in the resealed ghosts is determined from the increase in inorganic phosphate after incubation[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[3]

The RAW264.7 murine macrophage-derived cell line is used. Cell viability is measured using the 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Cells (105 cells/well) are cultured in 96-well plates and treated with varying concentrations of Phlorizin for 24 h. Next, the supernatant is removed and the cells are incubated with MTT (50 mg/mL) for 4 h at 37°C. The plates are washed and isopropanol is added to dissolve formazone crystals, then the absorbance values are measured at 570 nm using a microplate reader[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[4]

Female SDT fatty rats are used in this study. At six weeks of age, SDT fatty rats are divided into two groups (n=8); a Phlorizin treated group and a vehicle treated group. Age-matched female Sprague-Dawley (SD) rats are used as control animals (n=8). Animals are housed in a climate-controlled room (temperature 23±3°C, humidity 55±15%, 12 h lighting cycle) and allowed free access to basal diet and water. Phlorizin is injected subcutaneously once daily (100 mg/kg/day) to animals in the Phlorizin treated group for 23 weeks. Twenty % propylene glycol is administered to animals in the vehicle treated group and control SD rats[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.2914 mL 11.4571 mL 22.9142 mL 57.2856 mL
DMSO 5 mM 0.4583 mL 2.2914 mL 4.5828 mL 11.4571 mL
10 mM 0.2291 mL 1.1457 mL 2.2914 mL 5.7286 mL
15 mM 0.1528 mL 0.7638 mL 1.5276 mL 3.8190 mL
20 mM 0.1146 mL 0.5729 mL 1.1457 mL 2.8643 mL
25 mM 0.0917 mL 0.4583 mL 0.9166 mL 2.2914 mL
30 mM 0.0764 mL 0.3819 mL 0.7638 mL 1.9095 mL
40 mM 0.0573 mL 0.2864 mL 0.5729 mL 1.4321 mL
50 mM 0.0458 mL 0.2291 mL 0.4583 mL 1.1457 mL
60 mM 0.0382 mL 0.1910 mL 0.3819 mL 0.9548 mL
80 mM 0.0286 mL 0.1432 mL 0.2864 mL 0.7161 mL
100 mM 0.0229 mL 0.1146 mL 0.2291 mL 0.5729 mL

* 備注：如您選擇水作為儲備液，請稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

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產(chǎn)品名稱：
Phlorizin
目錄號：
HY-N0143
需求量：