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Parthenolide
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。
Parthenolide图片
CAS NO:20554-84-1
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
50mg电议
100mg电议
200mg电议
500mg电议
1 g电议

产品名称
小白菊内酯
(-)-Parthenolide
产品介绍
Parthenolide是在药草短舌匹菊中发现的倍半萜内酯。 Parthenolide通过抑制NF-κB活化而表现出抗炎活性; 它还可抑制HDAC1蛋白而不影响其他I/II类HDAC。
生物活性

Parthenolide is a sesquiterpene lactone found in the medicinal herb Feverfew. Parthenolide exhibits anti-inflammatory activity by inhibitingNF-κBactivation; also inhibitsHDAC1protein without affecting other class I/II HDACs.

IC50& Target[1]

NF-κB

 

Autophagy

 

Mitophagy

 

体外研究
(In Vitro)

Parthenolide (PTL) has a dose-dependent growth inhibition effect on NSCLC cells Calu-1, H1792, A549, H1299, H157, and H460. Parthenolide can induce cleavage of apoptotic proteins such as CASP8, CASP9, CASP3 and PARP1 both in concentration- and time-dependent manner in tested lung cancer cells, indicating that apoptosis is trigged after Parthenolide exposure. In addition to induction of apoptosis, Parthenolide also induces G0/G1cell cycle arrest in a concentration-dependent manner in A549 cells and G2/M cell cycle arrest in H1792 cells[2].

体内研究
(In Vivo)

Only Parthenolide, the HDAC inhibitor with anti-inflammatory features, displayed a potent anti-apoptotic effect inPhb1KO hepatocytes. Indeed, TSA and Parthenolide-treated hepatocytes showed increased levels of FXR, and reduced levels of CYP7A1, HDAC4, TNFα, TRAIL and Bax suggesting a less toxic effect of bile acids as a results of specific HDAC inhibition, resulting in the attenuation of thePhb1KO hepatocytes apoptotic response. Importantly, Parthenolide exerts a protective effect from the liver injury after BDL inPhb1KO mice. Indeed, Parthenolide treatment results in a reduction of the mortality rate of this mice after BDL associated with a lower apoptotic response as revealed by a reduction of necrotic areas, Tunel-staining, as well as decreased ALT (8431±957 vs.4225±210 U/L) and AST (4805±300 vs.2242±438 U/L) activities compared to controlPhb1KO mice[3].

Clinical Trial
分子量

248.32

性状

Solid

Formula

C15H20O3

CAS 号

20554-84-1

中文名称

小白菊内酯;银胶菊内酯

结构分类
  • Terpenoids
  • Sesquiterpenes
来源
  • Plants
  • Leguminosae
  • Euchresta formosana(Hayata) Ohwi
  • Plants
  • Compositae
运输条件

Room temperature in continental US; may vary elsewhere.

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

DMSO : ≥ 100 mg/mL(402.71 mM)

H2O :< 0.1 mg/mL(insoluble)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM4.0271 mL20.1353 mL40.2706 mL
5 mM0.8054 mL4.0271 mL8.0541 mL
10 mM0.4027 mL2.0135 mL4.0271 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: ≥ 2.08 mg/mL (8.38 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.38 mM,饱和度未知) 的澄清溶液。

    以 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;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: ≥ 2.08 mg/mL (8.38 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.38 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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: ≥ 2.08 mg/mL (8.38 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.38 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 20.8 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。