Pinostrobin

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Pinostrobin  纯度: 99.98%

Pinostrobin 是一种黄酮类化合物，具有抗癌、抗氧化、抗病毒和神经保护活性。Pinostrobin 具有口服活性。Pinostrobin 是一种有效的 PCSK9 抑制剂，可抑制 PCSK9 的催化活性。Pinostrobin 可用于病毒感染、癌症、白血病、心脑血管疾病、肝硬化、炎症和神经系统疾病的研究。

Pinostrobin

Pinostrobin Chemical Structure

CAS No. : 480-37-5

规格 价格 是否有货 数量
1 mg ￥880 In-stock
5 mg ￥2200 In-stock
10 mg ￥3550 In-stock
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100 mg   询价  

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Pinostrobin 相关产品

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生物活性

Pinostrobin is a flavonoid with anti-cancer, antioxidant, antiviral and neuroprotective activities. Pinostrobin has oral activity. Pinostrobin is a potent PCSK9 inhibitor that inhibits the catalytic activity of PCSK9. Pinostrobin can be used in the research of viral infections, cancer, leukemia, cardiovascular and cerebrovascular diseases, cirrhosis, inflammation and neurological diseases[1][2][3][4][5][6][7][8].

IC50 & Target

HSV-1

 

TNF-α

 

IL-1β

 

PCSK9

 

体外研究
(In Vitro)

Pinostrobin (0-100 μg/mL, 72 h) 抑制 HSV-1 病毒的 EC50 为 22.71 μg/mL[2]。
Pinostrobin (25-200 μM, 3 days) 通过刺激 cAMP/PKA 和 p38 MAPK 信号通路中相关黑色素生成调节因子的表达，促进 B16F10 细胞生成黑色素，且对细胞无毒性[5]。
Pinostrobin (130 and 150 μM, 48 h) 通过调控 miR-410-5p 和 SFRP5 诱导急性白血病细胞 NB4 和 MOLT-4 凋亡[6]。
Pinostrobin (0-200 μM, 24-96 h) 通过 ROS 介导的宫颈癌细胞 (HeLa, Ca Ski, SiHa) 线粒体损伤，有效地诱导细胞凋亡，同时对非癌细胞 HEK293 不具有毒性[7]。

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Pinostrobin 相关抗体:

Cell Viability Assay[2]

Cell Line: Vero cells
Concentration: 0-100 μg/mL
Incubation Time: 72 h
Result: The maximum noncytotoxic concentration (TD0) of pinostrobin was calculated as 95.37 ± 7.14μg/mL.

Western Blot Analysis[5]

Cell Line: B16F10 cell
Concentration: 25-200 μM
Incubation Time: 3 days
Result: Promoted phosphorylation of related targets under the cascade reaction of cAMP/PKA and p38 MAPK signaling pathways, such as MITF, tyrosinase, trp1, creb, GSK-3β, β-catenin, ERK, p38, etc.

体内研究
(In Vivo)

Pinostrobin (20 mg/kg , 50 mg/kg, i.g., daily for 7 days) 呈剂量依赖性地延缓 HSV-1 感染小鼠模型的病变发展[2]。
Pinostrobin (Single oral 10 and 20 mg/kg) 可通过抑制 LPS 诱导的炎症大鼠模型体内的 TNF-α 和 IL-1β 水平起到消炎作用[3]。
Pinostrobin (daily oral 30 and 60 mg/kg for 2 months) 对硫代乙酰胺 Thioacetamide (TAA) (HY-Y0698) 所致肝硬化大鼠具有肝保护作用[4]。

Pinostrobin在大鼠体内的相关药动学参数[8]

Route Dose (mg/kg) AUC0-t (ng·min/mL) MRT (h) Cmax (ng/mL) Tmax (h) t1/2 (min)
i.g. 0.5 3817.80 6.26 615.35 4 4.34

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Sprague Dawley (SD) rats (200–250 g), LPS (5 mg/kg) was administered after 2 h of the final dose. [3]
Dosage: Single oral 10 and 20 mg/kg
Administration: p.o.
Result: Did not cause any signs of abnormal behavior and toxicity in the rats.
Dose-dependent resulted in significant reductions in the levels of two cytokines, TNF-α and IL-1β.
Animal Model: healthy female male Sprague Dawley rats (6–7 weeks old, weighed between 180 and 210 g), Thioacetamide (HY-Y0698)-induced liver cirrhosis in rats[4]
Dosage: daily oral 30 and 60 mg/kg for 2 months, single oral 500mg/kg
Administration: p.o.
Result: Significantly reduced liver index and hepatocyte proliferation in rats, and significantly reduce cell damage.
Significantly down-regulated the expression levels of PCNA and α-SMA.
The activities of antioxidant enzymes (SOD) and CAT in liver homogenate were increased, and the level of malondialdehyde (MDA) was decreased. The levels of serum bilirubin, total protein, albumin and liver enzymes (ALP, ALT and AST) recovered to normal.
Decreased the levels of TNF-a and IL-6 and increased the levels of IL-10 in rats.
Acute toxicity with a higher dose of 500 mg/kg Pinostrobin did not manifest any toxicological signs in rats.

分子量

270.28

Formula

C16H14O4
CAS 号

480-37-5
性状

固体

颜色

White to yellow

结构分类
  • Flavonoids
  • Flavonones
  • Phenols
  • Monophenols
初始来源
  • 植物
  • 其他科
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

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

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (369.99 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6999 mL 18.4993 mL 36.9987 mL
5 mM 0.7400 mL 3.6999 mL 7.3997 mL
10 mM 0.3700 mL 1.8499 mL 3.6999 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 (protect from light)。-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。

  • 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

In Vivo:

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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.25 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。

    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。

    20% SBE-β-CD in Saline 的配制（4°C，储存一周）：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。

  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (9.25 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，此方案实验周期在半个月以上的动物实验酌情使用。

    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。

扫码获得
动物溶解方案

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

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：
%

DMSO +

% 

%

Tween-80 +

%

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO， ，均可在 Shanghai Jinpan Biotech Co Ltd 网站选购。 ，Tween 80，均可在 Shanghai Jinpan Biotech Co Ltd 网站选购。

计算结果
工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。

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

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动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

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

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.98%

Data Sheet (647 KB) SDS (251 KB)

COA (264 KB) HNMR (90 KB) CNMR (100 KB) RP-HPLC (189 KB) MS (260 KB)

产品使用指南 (1538 KB)

参考文献

  • [1]. Gao WY, et al. Pinostrobin Inhibits Proprotein Convertase Subtilisin/Kexin-type 9 (PCSK9) Gene Expression through the Modulation of FoxO3a Protein in HepG2 Cells.J Agric Food Chem. 2018 Jun 20;66(24):6083-6093.  [Content Brief]

    [2]. Wu N, et al. Activity investigation of pinostrobin towards herpes simplex virus-1 as determined by atomic force microscopy. Phytomedicine. 2011 Jan 15;18(2-3):110-8.

    [3]. Patel NK, et al. Pinostrobin and Cajanus lactone isolated from Cajanus cajan (L.) leaves inhibits TNF-α and IL-1β production: in vitro and in vivo experimentation. Phytomedicine. 2014 Jun 15;21(7):946-53.  [Content Brief]

    [4]. Shareef SH, et al. Hepatoprotective effect of pinostrobin against thioacetamide-induced liver cirrhosis in rats. Saudi J Biol Sci. 2023 Jan;30(1):103506.  [Content Brief]

    [5]. Yoon JH, et al. Discovery of Pinostrobin as a Melanogenic Agent in cAMP/PKA and p38 MAPK Signaling Pathway. Nutrients. 2022 Sep 9;14(18):3713.  [Content Brief]

    [6]. Norkaew C, et al. Pinostrobin induces acute leukemia cell apoptosis via the regulation of miR-410-5p and SFRP5. Life Sci. 2023 Jul 15;325:121739.  [Content Brief]

    [7]. Jaudan A, et al. Induction of apoptosis by pinostrobin in human cervical cancer cells: Possible mechanism of action. PLoS One. 2018 Feb 8;13(2):e0191523.  [Content Brief]

    [8]. Hua X, et al. Determination of pinostrobin in rat plasma by LC-MS/MS: application to pharmacokinetics. J Pharm Biomed Anal. 2011 Dec 5;56(4):841-5.  [Content Brief]

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