1. Immunology/Inflammation Metabolic Enzyme/Protease
  2. NO Synthase Arginase
  3. Piceatannol 3'-O-glucoside

Piceatannol 3'-O-glucoside  (Synonyms: Quzhaqigan)

製品番号: HY-N2237 純度: 99.65%
COA 取扱説明書 Technical Support

Piceatannol 3'-O-glucoside, an active component of Rhubarb, activates endothelial nitric oxide (NO) synthase through inhibition of arginase activity with IC50s of 11.22 μM and 11.06 μM against arginase I and arginase II, respectively.

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Piceatannol 3'-O-glucoside

Piceatannol 3'-O-glucoside 構造式

CAS 番号 : 94356-26-0

容量 価格(税別) 在庫状況 数量
1 mg $80 在庫あり
5 mg $185 在庫あり
10 mg $275 在庫あり
25 mg $495 在庫あり
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100 mg   お問い合わせ  

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Based on 1 publication(s) in Google Scholar

Other Forms of Piceatannol 3'-O-glucoside:

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  • 純度とドキュメンテーション

  • 参考文献

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製品説明

Piceatannol 3'-O-glucoside, an active component of Rhubarb, activates endothelial nitric oxide (NO) synthase through inhibition of arginase activity with IC50s of 11.22 μM and 11.06 μM against arginase I and arginase II, respectively.

IC50 & Target

NO synthase[1]
IC50: 11.22 μM (Arginase I), 11.06 μM (Arginase II)[1]

体外実験

Piceatannol 3'-O-glucoside (Piceatannol-3'-O-β-D-glucopyranoside; PG) is a potent component of stilbenes, inhibits the activity of arginase I and II prepared from mouse liver and kidney lysates, respectively, in a dose-dependent manner. In human umbilical vein endothelial cells, incubation of Piceatannol 3'-O-glucoside markedly blocks arginase activity and increases nitrite and nitrate (NOx) production, as measured by Griess assay. In liver lysates, incubation of different concentrations of Piceatannol 3'-O-glucoside significantly decreases arginase I activity (75±5% at 1 μM, 72±7% at 3 μM, 62±1% at 10 μM) compared to untreated control (100±9%). In kidney lysates, the residual arginase activities after incubation of 1, 3 and 10 μM Piceatannol 3'-O-glucoside are 75±6, 74±5, and 53±8%, respectively. Arginase activity is measured in the presence of different concentration of Piceatannol 3'-O-glucoside (from 0 to 120 μM) using liver lysate and kidney lysate. The 50% inhibitory concentrations (IC50) are 11.22 μM for the liver lysate and 11.06 μM for kidney lysate. The values are obtained using the software of Graphpad prizm 4.0. Piceatannol 3'-O-glucoside inhibits arginase activity and increases NO production in HUVECs. Piceatannol 3'-O-glucoside inhibits lipoxygenase activity upto 66% at the concentration of 100 μM and IC50 value is 69 μM[1].

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

体内実験

In order to ascertain whether Piceatannol 3'-O-glucoside (PG) ameliorates vascular function in wild-type (WT) and atherogenic model mice [apolipoprotein E-null mice (ApoE-/-)] and to investigate the possible underlying mechanism. Preincubation of aortic vessels from WT mice fed a normal diet (ND) with Piceatannol 3'-O-glucoside attenuates vasoconstriction response to U46619 and phenylephrine (PE), while the vasorelaxant response to acetylcholine (Ach) is markedly enhanced in an endothelium-dependent manner. Piceatannol 3'-O-glucoside treatment attenuates the phenylephrine (PE)-dependent contractile response, and significantly improves the acetylcholine (Ach)-dependent vasorelaxation response in aortic rings from ApoE-/- mice fed a high-cholesterol diet (HCD). Piceatannol 3'-O-glucoside administration in the drinking water significantly reduces fatty streak formation in ApoE-/- mice fed an HCD[2].

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

分子量

406.38

分子式

C20H22O9

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O[C@H]([C@H]([C@@H]([C@@H](CO)O1)O)O)[C@@H]1OC2=CC(/C=C/C3=CC(O)=CC(O)=C3)=CC=C2O

Structure Classification
Initial Source
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶剤 & 溶解度
体外: 

DMSO : 50 mg/mL (123.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4608 mL 12.3038 mL 24.6075 mL
5 mM 0.4922 mL 2.4608 mL 4.9215 mL
10 mM 0.2461 mL 1.2304 mL 2.4608 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.87%

参考文献
キナーゼ実験
[1]

Tissue lysates are prepared using lysis buffer (50 mM Tris-HCl, pH 7.5, 0.1 mM EDTA and protease inhibitors) by homogenization at 4°C followed by centrifugation for 20 min at 14,000× g at 4°C. The supernatants are used to assay for arginase activity. The livers or kidneys from C57BL/6 mice (10 weeks) are homogenized in the buffer (50 mM Tris-HCl, 150 mM NaCl, 1% Nonidet P-40, 1 mM EDTA, 1 µg/mL of leupeptin, 1 µg/mL of pepstatin, 1 µg/mL of aprotinin, 1 mM phenylmethylsulfonylflouride, 1 mM sodium orthovanadate, and 1 mM NaF) and centrifuged for 30 min at 14,000× g. The protein amount of the supernatant is analyzed by the Bradford method. Protein (100 µg) are separated in a 10% SDS-PAGE and then transferred to a nitrocellulose membrane. The blots are incubated with a monoclonal anti-arginase I, anti-arginase II, anti-endothelial nitric oxide synthase (eNOS), or anti-β-tubulin antibodies followed by the secondary antibody. The signals are detected using an enhanced chemiluminescence detection reagent with X-ray films[1].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。

動物実験
[2]

Mice[2]
Twenty 10-week-old male wild-type (WT) (C57BL/6J) and ApoE-/- mice are studied. To determine the effect of Piceatannol 3'-O-glucoside on vascular reactivity, aortic rings isolated from 20 male C57BL/6J WT mice fed a normal diet (ND) and 20 male ApoE-/- mice fed an HCD are studied for 6 weeks. Aortic rings are incubated with or without Piceatannol 3'-O-glucoside (50 μM) for 18 h. For the pathological assay, Piceatannol 3'-O-glucoside is administered in the drinking water to ApoE-/- mice for 6 weeks when the mice are started on the HCD. Given that each mouse consumes ~10 mL water/day this represents a daily dose of ~500 μg/mouse/day of Piceatannol 3'-O-glucoside[2].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4608 mL 12.3038 mL 24.6075 mL 61.5188 mL
5 mM 0.4922 mL 2.4608 mL 4.9215 mL 12.3038 mL
10 mM 0.2461 mL 1.2304 mL 2.4608 mL 6.1519 mL
15 mM 0.1641 mL 0.8203 mL 1.6405 mL 4.1013 mL
20 mM 0.1230 mL 0.6152 mL 1.2304 mL 3.0759 mL
25 mM 0.0984 mL 0.4922 mL 0.9843 mL 2.4608 mL
30 mM 0.0820 mL 0.4101 mL 0.8203 mL 2.0506 mL
40 mM 0.0615 mL 0.3076 mL 0.6152 mL 1.5380 mL
50 mM 0.0492 mL 0.2461 mL 0.4922 mL 1.2304 mL
60 mM 0.0410 mL 0.2051 mL 0.4101 mL 1.0253 mL
80 mM 0.0308 mL 0.1538 mL 0.3076 mL 0.7690 mL
100 mM 0.0246 mL 0.1230 mL 0.2461 mL 0.6152 mL
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

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製品名:
Piceatannol 3'-O-glucoside
製品番号:
HY-N2237
数量:
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