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Triptolide. (Synonyms: 雷公藤甲素; PG490)
目录号: PC11539 纯度: ≥98%
CAS No. :38748-32-2
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中文名称
Triptolide.
中文别名
雷公藤甲素;雷公藤多甙;雷藤素甲;雷公藤内酯醇;雷公藤甲素(雷公藤内酯醇) TLC;雷公藤甲素(雷公藤内酯醇);2-甲基-1 8-萘啶-3-羧酸;Triptolide 雷公藤甲素;Triptolide 雷公藤甲素 标准品;zzstandard 品牌 雷公藤甲素对照品;雷公藤甲素 对照品标准品;雷公藤甲素 Triptolide;雷公藤甲素 雷公藤内酯醇 雷公藤多甙 Triptolide;雷公藤甲素(P);雷公藤甲素(标准品);雷公藤甲素(雷公藤内酯醇),Triptolide,植物提取物,标准品,对照品;雷公藤甲素,分析标准品;雷公藤甲素粉末;雷公藤甲素固体状;雷公藤甲素中间体;雷公藤提取物;雷公藤提取物(雷公藤甲素);临床实验雷公藤甲素;藤甲素;医药级雷公藤甲素;雷公藤甲素(雷公藤多甙,雷公藤内酯醇,雷藤素甲);雷公藤甲素,雷公藤内酯醇;雷公藤内酯醇,雷公藤多甙
英文名称
Triptolide
英文别名
triptolide;PG490;TRIPTOLIDE, TRIPTERYGIUM WILFORDII;8b,9,10-decahydro-6-hydroxy-8b-methyl-6a-(1-methylethyl)-,(3bs,4as,5as,6r,6ar;TRIPTOLIDE TLC;TRIPTOLIDE(P);TRIPTONIDE(P);(3bS,4aS,5aS,6R,6aR,7aS,7bS,8aS,8bS)-3b,4,4a,6,6a,7a,7b,8b,9,10-decahydro-6-hydroxy-8b-methyl-6a-(1-methylethyl)-trisoxireno[4b,5:6,7:8a,9]phenanthro[1,2-c]furan-1(3H)-one;NSC 163062;TRIPTOLIDE(P) PrintBack;Triptolide(PG490);Triptolide(TPL,PG490,NSC 163062);Triptonide;Common Threewingnut Root Extract;(3bS,4aS,5aS,6R,6aR,7aS,7bS,8aS,8bS)-3b,4,4a,6,6a,7a,7b,8b,9,10-decahydro-6-hydroxy-6a-isopropyl-8b-methyltrisoxireno[6,7:8a,9:4b,5]phenanthro[1,2-c]furan-1(3H)-one;(3bS,4aS,5aS,6R,6aR,7aS,7bS,8aS,8bS)-3b,4,4a,6,6a,7a,7b,8b,9,10-decahydro-6-hydroxy-8b-methyl-6a-(1-methylethyl)trisoxireno[4b,5:6,7:8a,9]phenanthro[1,2-c]furan-1(3H)-one;PG-490;triptergium wilfordii;TRIPTO;triptolid;Triptolide?;(-)-Triptolide;[3bS-(3ba,4aa,5aR*,6b,6ab,7ab,7ba,8aR*,8bb)]-3b,4,4a,6,6a,7a,7b,8b,9,10-Decahydro-6-hydroxy-8b-methyl-6a-(1-methylethyl)trisoxireno[4b,5:6,7:8a,9]phenanthro[1,2-c]furan-1(3H)-one;PG 490;19ALD1S53J;C20H24O6;Triptolide (PG490);CPD000466307;SMR000466307;NSC163062;Triptolide, 1;Triptolide(PG490)/;BSPBio_001595;KBioSS_000315;KBioGR_000315;MLS006010844;MLS001424107
Cas No.
38748-32-2
分子式
C20H24O6
分子量
360.40
包装储存

4°C, stored under nitrogen

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

生物活性

Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory, antiproliferative and antitumour effects. Triptolide is a NF-κB activation inhibitor.

性状

Solid

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. Triptolide is a natural product derived from the Chinese plant Tripterygium 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 IC50 values 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 (IC50 values: 725 nM vs. 88 nM). Differentiated PC12 cells are incubated with different concentrations of Triptolide (0.01, 0.1, and 1 nM) in the presence of 10 μM Aβ25-35 for 24 hours and MTT assay is used to detect the effect of Triptolide. The results show that Aβ25-35 can 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.

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

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 Cmax increases from 413±74 to 510±94 ng/mL (P<0.05) and the AUC from 103.5±9.6 to 154.3±30.2 ng?h/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 ng?h/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.

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

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, stored under nitrogen

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

ClinicalTrial
结构分类
来源
参考文献
溶解度数据
体外研究: 

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

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

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7747 mL 13.8735 mL 27.7469 mL
5 mM 0.5549 mL 2.7747 mL 5.5494 mL
10 mM 0.2775 mL 1.3873 mL 2.7747 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,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 (stored under nitrogen)。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

    建议依照次序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in 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 μL 20% 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.

    建议依照次序添加每种溶剂: 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。

*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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