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  3. Homoplantaginin

Homoplantaginin  (Synonyms: 高车前苷)

目录号: HY-N1949 纯度: 99.90%
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Homoplantaginin是来自中药Salvia plebeia的具有抗炎和抗氧化活性的类黄酮。

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Homoplantaginin Chemical Structure

Homoplantaginin Chemical Structure

CAS No. : 17680-84-1

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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Homoplantaginin is a flavonoid from a traditional Chinese medicine Salvia plebeia with antiinflammatory and antioxidant properties. Homoplantaginin could inhibit TNF-α and IL-6 mRNA expression, IKKβ and NF-κB phosphorylation.

IC50 & Target

p65

 

体外研究
(In Vitro)

Homoplantaginin shows IC50 of reduction level of DPPH radical at 0.35 μg/mL. In human hepatocyte HL-7702 cells exposed to H2O2, the addition of 0.1-100μg/mL of homoplantaginin significantly reduces lactate dehydrogenase leakage, and increases glutathione, glutathione peroxidase and superoxide dismutase in supernatant[1]. Homoplantaginin (0.1, 1, 10 μM) dose-dependently reduces expression of toll-like receptor-4 evoked by palmitic acid (100 μM). Homoplantaginin tightly controlls palmitic acid-induced reactive oxygen species to prevent nucleotide-binding domain-like receptor 3 (NLRP3) inflammasome activation by suppressing reactive oxygen species-sensitive thioredoxin-interacting protein, NLRP3, and caspase-1[2]. Pre-treatment of homoplantaginin on human umbilical vein endothelial cells significantly inhibits palmitic acid induced TNF-α and IL-6 mRNA expression, and IKKβ and NF-κB p65 phosphorylation. Homoplantaginin significantly modulates the Ser/Thr phosphorylation of IRS-1, improves phosphorylation of Akt and endothelial nitric oxide synthase, and increases NO production in the presence of insulin[3].

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

体内研究
(In Vivo)

Homoplantaginin(25-100mg/kg) significantly reducesthe increase in serum alanine aminotranseferase and aspartate aminotransferase, decreases the levels of TNF-α and IL-1. The same treatment also reduces the content of thiobarbituric acid-reactive substances, elevates the levels of GSH, GSH-Px and SOD in hepatic homogenate[1]. Homoplantaginin is rapidly absorbed (Tmax=16.00±8.94min), reaching a mean Cmax between 0.77 and 1.27nmol/mL. The absolute oral bioavailability is calculated to be only 0.75%.

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

分子量

462.40

Formula

C22H22O11

CAS 号
性状

固体

颜色

Light yellow to yellow

中文名称

高车前苷;高车前甙

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 50 mg/mL (108.13 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 2.1626 mL 10.8131 mL 21.6263 mL
5 mM 0.4325 mL 2.1626 mL 4.3253 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.50 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制: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。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (4.50 mM); 悬浊液; 超声助溶

    此方案可获得 2.08 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    1 mL 工作液为例,取 100 μL 20.8 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。
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

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 MCE 网站选购。 Tween 80,均可在 MCE 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)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
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
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: 99.90%

参考文献
Cell Assay
[3]

The viability of cultured cells is determined using the MTT assay. Human umbilical vein endothelial cells are exposed to various concentrations of homoplantaginin (0.1, 1, 3, 10, 30, 100 μM) for 48 h. Subsequently, 20 μL of MTT (5 mg/mL) is added to each well for an additional 4 h at 37°C. The supernatant is removed, and DMSO is added to dissolve the formazan crystals. The optical absorbance is measured at 540 nm[3].

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

Animal Administration
[1][4]

Rats: Homoplantaginin is dissolved in a solution consistingof DMSO, PEG 400, ethanol and normal saline(2:2:3:3, v/v/v/v) at a concentration of 10 mg/mL. The rats are randomly divided into three groups to receive oral administration(150 mg/kg), tail vein injection (15 mg/kg) and peritoneal injectionv (15 mg/kg). Blood samples (approximately 0.5 mL) are collected from the retro-orbital plexus into heparinized microfugetubes at 5, 10, 20, 30, 45, 60, 90, 120, and 180 min after administration. The plasma samples, separated by centrifuging the blood samples at 10,000 rpm[4].

Mice: Homoplantaginin is dissolved in 5% amylum. Homoplantaginin is administered orally by gastric intubation during the experimental period at doses of 25, 50, 100 mg/kg/d, respectively. Eight hours after injection of LPS, the mice are anesthetized with ether and blood samples are collected by exsanguination from the inferior vein. The liver is removed and fixed in formalin for histological analysis[1].

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

参考文献

Homoplantaginin 相关分类

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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1626 mL 10.8131 mL 21.6263 mL 54.0657 mL
5 mM 0.4325 mL 2.1626 mL 4.3253 mL 10.8131 mL
10 mM 0.2163 mL 1.0813 mL 2.1626 mL 5.4066 mL
15 mM 0.1442 mL 0.7209 mL 1.4418 mL 3.6044 mL
20 mM 0.1081 mL 0.5407 mL 1.0813 mL 2.7033 mL
25 mM 0.0865 mL 0.4325 mL 0.8651 mL 2.1626 mL
30 mM 0.0721 mL 0.3604 mL 0.7209 mL 1.8022 mL
40 mM 0.0541 mL 0.2703 mL 0.5407 mL 1.3516 mL
50 mM 0.0433 mL 0.2163 mL 0.4325 mL 1.0813 mL
60 mM 0.0360 mL 0.1802 mL 0.3604 mL 0.9011 mL
80 mM 0.0270 mL 0.1352 mL 0.2703 mL 0.6758 mL
100 mM 0.0216 mL 0.1081 mL 0.2163 mL 0.5407 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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