上海金畔生物科技有限公司提供天然产物萜类及其苷类Terpenoids and Glycosides。
Triptolide (Synonyms: 雷公藤甲素; PG490) 纯度: 99.78%
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。
Triptolide Chemical Structure
CAS No. : 38748-32-2
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10 mM * 1 mL in DMSO | ¥1150 | In-stock | |
1 mg | ¥520 | In-stock | |
2 mg | ¥910 | In-stock | |
5 mg | ¥1450 | In-stock | |
10 mg | ¥2250 | In-stock | |
25 mg | ¥4500 | In-stock | |
100 mg | ¥14500 | In-stock | |
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Triptolide 相关产品
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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[1][2][3][4][5][6]. |
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IC50 & Target[1][2] |
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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 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)[2]. Differentiated PC12 cells are incubated with different concentrations of Triptolide (0.01, 0.1, and 1 nM) in the presence of 10 μM Aβ25-35 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[3]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only. |
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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[4]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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分子量 |
360.40 |
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Formula |
C20H24O6 |
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CAS 号 |
38748-32-2 |
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中文名称 |
雷公藤甲素;雷藤素甲;雷公藤内酯醇;雷公藤多甙 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
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溶解性数据 |
In Vitro:
DMSO : ≥ 33 mg/mL (91.56 mM) H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble) * “≥” means soluble, but saturation unknown. 配制储备液
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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。 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
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参考文献 |
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Cell Assay [3] |
The viability of differentiated PC12 cells treated with different concentrations of Triptolide. After differentiated PC12 cells are cultured on 96-well plates with RPMI 1640 medium for stabilization, differentiated PC12 cells are incubated with different concentrations of Triptolide (0.01, 0.1, and 1 nM) for 24 hours. The concentrations in this study are chosen. Then cell viability is determined by the MTT assay. Each condition and experiment is repeated three times[3]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only. |
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Animal Administration [4] |
Mice[4] Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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