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Andrographolide
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Andrographolide图片
CAS NO:5508-58-7

穿心莲内酯
Andrographis
Andrographolide 是一种NF-κB抑制剂,通过共价修饰内皮细胞中p50的半胱氨酸残基而抑制 NF-κB 活化,而不影响 IκBα 降解或 p50/p65 核易位。Andrographolide 具有抗病毒作用。
生物活性

Andrographolide is aNF-κBinhibitor, which inhibitsNF-κBactivation through covalent modification of a cysteine residue onp50in endothelial cells without affecting IκBα degradation or p50/p65 nuclear translocation. Andrographolide has antiviral effects.

IC50& Target[1]

p50

 

体外研究
(In Vitro)

Andrographolide (AP) concentration-dependently suppresses receptor activator of nuclear factor kappa B ligand (RANKL)-mediated osteoclast differentiation and bone resorption in vitro and reduces the expression of osteoclast-specific markers. Andrographolide attenuates inflammation by inhibition of TNFα-induced NF-κB activation through covalent modification of reduced Cys62of p50, without affecting IκBα degradation or p50/p65 nuclear translocation. Andrographolide also inhibits the ERK/MAPK signalling pathway without affecting p38 or JNK signalling. Andrographolide inhibits osteoclast differentiation of RAW 264.7 cells in a concentration-dependent manner. Andrographolide suppresses osteoclast formation in a concentration-dependent manner without any obvious cytotoxic effects, in both BMMs and RAW 264.7 cells. Andrographolide treatment substantially reduces the area of bone resorption. Only approximately 30% of the bone resorption observed in the control group is achieved after treatment with 2.5 μM Andrographolide. Osteoclastic bone resorption is almost completely inhibited after treatment with 10 μM Andrographolide[1].

体内研究
(In Vivo)

Treatment with Andrographolide (5 or 30 mg/kg) reduces the extent of bone loss induced by LPS. Moreover, Andrographolide slightly increases the BMD and cortex thickness compared to LPS treatment. Histological examination confirms the protective effects of Andrographolide on LPS-induced bone loss. LPS injection leads to inflammatory bone erosion and increased numbers of TRAP-positive osteoclasts[1].

Clinical Trial
分子量

350.45

性状

Solid

Formula

C20H30O5

CAS 号

5508-58-7

中文名称

穿心莲内酯

结构分类
  • Terpenoids
  • Diterpenoids
来源
  • Plants
  • Acanthaceae
  • Andrographis paniculata(Burm. F.) Nees
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL(285.35 mM;Need ultrasonic)

H2O : 0.1 mg/mL(0.29 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.8535 mL14.2674 mL28.5347 mL
5 mM0.5707 mL2.8535 mL5.7069 mL
10 mM0.2853 mL1.4267 mL2.8535 mL
*

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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

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

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.5 mg/mL (7.13 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.13 mM,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 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.5 mg/mL (7.13 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.13 mM,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 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (7.13 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.13 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    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。

*以上所有助溶剂都可在本网站选购。
 
 
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