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Triptolide
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。
Triptolide图片
CAS NO:38748-32-2
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
1mg电议
2mg电议
5mg电议
10mg电议
25mg电议
100mg电议
200mg电议
500mg电议

产品名称
雷公藤甲素
PG490
产品介绍
Triptolide是从雷公藤根中提取的二萜类三环氧化物,具有免疫抑制,抗炎,抗增殖和抗肿瘤作用。 雷公藤内酯是NF-κB活化的抑制剂。
生物活性

Triptolide is a diterpenoid triepoxide extracted from the root ofTripterygium wilfordiiwith immunosuppressive, anti-inflammatory, antiproliferative and antitumour effects. Triptolide is aNF-κBactivation inhibitor[1][2][3][4][5][6].

IC50& Target[1][2]

HSP90

 

MDM-2/p53

47-73 nM (IC50)

体外研究
(In Vitro)

Triptolide induces apoptosis in cultured and primary Chronic Lymphocytic Leukemia (CLL) B-cells. Treatment of CD19+B cells with Triptolide, induces a dose-dependent increase in apoptosis in cultured and primary CLL cells. Triptolide is selectively toxic to both high risk (n=5) and low risk CLL (n=12) B cells (10 to 50 nM range) while largely sparing normal B-cells (n=5). Consistent with the inhibition of heat-shock induced HSP transcription, treatment with Triptolide attenuates heat-shock induced expression of HSPs[1]. Triptolide is a natural product derived from the Chinese plantTripterygium wilfordii, is reported to exhibit antitumor effects in a broad range of cancers. Triptolide inhibits MDM2 expression in a dose-dependent manner, even at low concentrations spanning 20-100 nM in acute lymphoblastic leukemia (ALL) cells. Triptolide exhibits strongly cytotoxic activity in all 8 cell lines having native MDM2 overexpression, with IC50values range from 47 to 73 nM. Triptolide exhibits much less cytotoxic effect on EU-4 cells that express very low level of MDM2, while it effectively kill these cells when MDM2 is stably transfected (IC50values: 725 nM vs. 88 nM)[2]. Differentiated PC12 cells are incubated with different concentrations of Triptolide (0.01, 0.1, and 1 nM) in the presence of 10 μM Aβ25-35for 24 hours and MTT assay is used to detect the effect of Triptolide. The results show that Aβ25-35can decrease the cell viability and when treated with Triptolide the viability of differentiated PC12 cells is significantly increased. The results indicate that Triptolide can alleviate cellular damage caused by Aβ25-35, which means that Triptolide has a neuroprotective effect[3].

体内研究
(In Vivo)

The Triptolide (TP) plasma concentrations are declined rapidly in mice after receive an intravenous dose. After 2h of injection, the Triptolide concentrations are dropped below the lower limit of quantification for all three groups. A comparison of the parameters is made between the control and the treated groups to assess the effect of P-gp inhibition on the Triptolide exposure and elimination. Treatment with the mdr1a-siRNA can significantly enhance the Triptolide plasma exposure, with the Cmaxincreases from 413±74 to 510±94 ng/mL (P<0.05) and the AUC from 103.5±9.6 to 154.3±30.2 ngoh/mL (P<0.05). In the concomitant group with Tariquidar, the significantly increased AUC is also noted, from 103.5±9.6 of the control to 145.9±24.6 ngoh/mL of the Triptolide+Tariquidar group (P<0.05). Accordingly, the total body clearance of Triptolide in mice is remarkably decreased, from 9564±1024.2 mL/min/kg of the control to 6576.4±1438.5 (P<0.05) and 5755.4±1200.1 mL/min/kg (P<0.05) for Triptolide+Tariquidar and Triptolide+mdr1a-siRNA groups, respectively[4].

Clinical Trial
分子量

360.40

性状

Solid

Formula

C20H24O6

CAS 号

38748-32-2

中文名称

雷公藤甲素;雷藤素甲;雷公藤内酯醇;雷公藤多甙

结构分类
  • Terpenoids
  • Diterpenoids
来源
  • Plants
  • Celastraceae
  • Tripterygium wilfordiiHook. f.
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据
In Vitro: 

DMSO : 25 mg/mL(69.37 mM;Need ultrasonic)

H2O :< 0.1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.7747 mL13.8735 mL27.7469 mL
5 mM0.5549 mL2.7747 mL5.5494 mL
10 mM0.2775 mL1.3873 mL2.7747 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 (stored under nitrogen)。-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    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 1.17 mg/mL (3.25 mM); Clear solution

    此方案可获得 ≥ 1.17 mg/mL (3.25 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 11.7 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
  • 2.

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

    Solubility: ≥ 1.17 mg/mL (3.25 mM); Clear solution

    此方案可获得 ≥ 1.17 mg/mL (3.25 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 11.7 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。