Triptolide

别名: PG490, NSC 163062 中文名称：雷公藤甲素

目录号：S3604 Purity: 99.95%

Triptolide是一种三环氧二萜类化合物,是从中草药雷公藤中提取的免疫抑制剂。它是一种NF-κB抑制剂，抑制NF-κB转录活性，破坏p65/CBP的相互作用，减少p65蛋白。Triptolide (PG490) 可抑制 heat shock transcription factor 1 (HSF1) 的反式激活。Triptolide 可抑制 MDM2 并通过一个p53非依赖性通路来诱导凋亡。

Triptolide Chemical Structure

CAS: 38748-32-2

规格	价格	库存
10mM (1mL in DMSO)	2432.43	现货
1mg	576.89	现货
5mg	2060.55	现货
100mg	16298.78	现货
1g	39900	现货
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产品质控

批次：纯度： 99.95%

99.95

Triptolide相关产品

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细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述	文献信息
Pkd1-/-	Increase in	100 nM	96 hrs	Increase in p21CIP/WAF expression in mouse Pkd1-/- cells at 100 nM after 96 hrs by Western blot analysis	17360534
Pkd2+/-	Growth inhibition of PC2 expressing mouse	100 nM	24 hrs	Growth inhibition of PC2 expressing mouse Pkd2+/- cells as cell death at 100 nM after 24 hrs	17360534
KBM5	Cytotoxicity against	0.001 to 17 uM	72 hrs	Cytotoxicity against human KBM5 cells harboring wild type Bcr-Abl at 0.001 to 17 uM after 72 hrs by MTS assay	20149665
KBM5	Cytotoxicity against	0.001 to 17 uM	72 hrs	Cytotoxicity against imatinib-resistant human KBM5 cells harboring Bcr-Abl T315I mutant at 0.001 to 17 uM after 72 hrs by MTS assay	20149665
LNCAP	Antagonist activity at	5 uM	24 hrs	Antagonist activity at AR in human LNCAP cells assessed as suppression of DHT-induced receptor transcriptional activity at 5 uM after 24 hrs by dual luciferase reporter gene assay	27994731
LNCAP	Antagonist activity at	500 nM	24 hrs	Antagonist activity at AR in human LNCAP cells assessed as suppression of DHT-induced receptor transcriptional activity at 500 nM after 24 hrs by dual luciferase reporter gene assay	27994731
HepG2	Antitumor activity against	0.2 mg/kg	15 days	Antitumor activity against human HepG2 cells xenografted in Balb/c nude mouse assessed as reduction in tumor growth at 0.2 mg/kg, ip administered once daily for 15 days	30613335
Pkd1+/-	Increase in	100 nM		Increase in PC2 dependent calcium release in mouse Pkd1+/- cells at 100 nM	17360534
Pkd1-/-	Increase in	100 nM		Increase in PC2 dependent calcium release in mouse Pkd1-/- cells at 100 nM	17360534
Pkd1-/-	Increase in	50 uM		Increase in calcium release in mouse Pkd1-/- cells at 50 uM in presence of RyR antagonist dantrolene	17360534
SMMC7721	Cytotoxicity against		72 hrs	Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay, IC50=0.018μM	19637874
A549	Cytotoxic activity against		72 hrs	Cytotoxic activity against human A549 cells assessed as reduction in cell viability after 72 hrs by SRB assay, IC50=0.0175μM	28011223
MOLT4	Cytotoxicity against		72 hrs	Cytotoxicity against human MOLT4 cells after 72 hrs by MTT assay, IC50=0.017μM	19637874
SGC7901	Cytotoxicity against		72 hrs	Cytotoxicity against human SGC7901 cells after 72 hrs by MTT assay, IC50=0.015μM	19637874
Rh30	Cytotoxicity against		72 hrs	Cytotoxicity against human Rh30 cells after 72 hrs by MTT assay, IC50=0.014μM	19637874
KBM5	Cytotoxicity against		72 hrs	Cytotoxicity against human KBM5 cells harboring wild type Bcr-Abl after 72 hrs by MTS assay, IC50=0.0103μM	20149665
SKOV3	Cytotoxicity against		72 hrs	Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay, IC50=0.01μM	19637874
HCT116	Cytotoxicity against		72 hrs	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=0.01μM	19637874
KBM5	Cytotoxicity against		72 hrs	Cytotoxicity against imatinib-resistant human KBM5 cells harboring Bcr-Abl T315I mutant after 72 hrs by MTS assay, IC50=0.0083μM	20149665
SKOV3	Cytotoxic activity against		72 hrs	Cytotoxic activity against human SKOV3 cells assessed as reduction in cell viability after 72 hrs by SRB assay, IC50=0.0072μM	28011223
SKOV3	Cytotoxicity against		72 hrs	Cytotoxicity against human SKOV3 cells after 72 hrs by sulforhodamine B assay, IC50=0.006μM	24378709
SKOV3	Antiproliferative activity against		72 hrs	Antiproliferative activity against human SKOV3 cells after 72 hrs by SRB assay, IC50=0.006μM	20833543
PC3	Cytotoxic activity against		72 hrs	Cytotoxic activity against human PC3 cells assessed as reduction in cell viability after 72 hrs by SRB assay, IC50=0.0183μM	28011223
MCF7	Cytotoxicity against		72 hrs	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay, IC50=0.019μM	19637874
Bel7402	Cytotoxicity against		72 hrs	Cytotoxicity against human Bel7402 cells after 72 hrs by MTT assay, IC50=0.02μM	19637874
PC3	Antiproliferative activity against		72 hrs	Antiproliferative activity against human PC3 cells after 72 hrs by SRB assay, IC50=0.02μM	20833543
PC3	Cytotoxicity against		72 hrs	Cytotoxicity against human PC3 cells after 72 hrs by sulforhodamine B assay, IC50=0.02μM	24378709
786-O	Cytotoxicity against		72 hrs	Cytotoxicity against human 786-O cells after 72 hrs by MTT assay, IC50=0.022μM	19637874
MDA-MB-231	Cytotoxicity against		72 hrs	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50=0.024μM	19637874
DU145	Cytotoxicity against		72 hrs	Cytotoxicity against human DU145 cells after 72 hrs by MTT assay, IC50=0.024μM	19637874
HO8910	Cytotoxicity against		72 hrs	Cytotoxicity against human HO8910 cells after 72 hrs by MTT assay, IC50=0.028μM	19637874
HCT15	Cytotoxicity against		72 hrs	Cytotoxicity against human HCT15 cells after 72 hrs by MTT assay, IC50=0.029μM	19637874
32D	Cytotoxicity against		72 hrs	Cytotoxicity against mouse 32D cells harboring wild type Bcr-Abl after 72 hrs by MTS assay, IC50=0.032μM	20149665
32D	Cytotoxicity against		72 hrs	Cytotoxicity against imatinib-resistant mouse 32D cells harboring Bcr-Abl T315I mutant after 72 hrs by MTS assay, IC50=0.034μM	20149665
PC3	Cytotoxicity against		72 hrs	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay, IC50=0.043μM	19637874
KB	Cytotoxicity against		72 hrs	Cytotoxicity against human KB cells after 72 hrs by MTT assay, IC50=0.043μM	19637874
HepG2	Cytotoxicity against		48 hrs	Cytotoxicity against human HepG2 cells after 48 hrs by XTT assay, IC50=0.0433μM	30613335
HeLa	Cytotoxicity against		72 hrs	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay, IC50=0.047μM	19637874
U251	Cytotoxicity against		72 hrs	Cytotoxicity against human U251 cells after 72 hrs by MTT assay, IC50=0.049μM	19637874
K562	Cytotoxicity against		72 hrs	Cytotoxicity against human K562 cells after 72 hrs by MTT assay, IC50=0.05μM	19637874
SW1116	Cytotoxicity against		72 hrs	Cytotoxicity against human SW1116 cells after 72 hrs by MTT assay, IC50=0.052μM	19637874
A549	Cytotoxicity against		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50=0.059μM	19637874
MKN28	Cytotoxicity against		72 hrs	Cytotoxicity against human MKN28 cells after 72 hrs by MTT assay, IC50=0.2μM	19637874
A549	Antagonist activity at			Antagonist activity at human PAR2 expressed in human A549 cells assessed as inhibition of 2f-LIGRLO-NH2-induced NFkappaB activation by luciferase reporter gene assay, IC50=0.014μM	23895492
MDA-MB-468	Cytotoxicity against			Cytotoxicity against human MDA-MB-468 cells by SRB assay, IC50=0.01μM	19637874
SKOV3	Cytotoxicity against			Cytotoxicity against human SKOV3 cells by SRB assay, IC50=0.009μM	19637874
HCT116	Cytotoxicity against			Cytotoxicity against human HCT116 cells assessed as decrease in cell viability, IC50=0.0047μM	31121546
HT-29	Cytotoxicity against			Cytotoxicity against human HT-29 cells, IC50=0.0021μM	21470864
A549	Cytotoxicity against			Cytotoxicity against human A549 cells, IC50=0.019μM	21470864
PC3	Cytotoxicity against			Cytotoxicity against human PC3 cells by SRB assay, IC50=0.02μM	19637874
PC3	Cytotoxicity against			Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation by sulforhodamine B assay, IC50=0.02μM	25467158
A549	Antagonist activity at			Antagonist activity at human PAR2 expressed in human A549 cells coexpressing TACR1 assessed as inhibition of substance P-induced IL-8 production by ELISA, IC50=0.023μM	23895492
A549	Growth inhibition of human			Growth inhibition of human A549 cells, IC50=0.03μM	28814374
U251	Cytotoxicity against			Cytotoxicity against human U251 cells assessed as inhibition of cell proliferation by sulforhodamine B assay, IC50=0.033μM	25467158
NIH/3T3	Cytotoxicity against			Cytotoxicity against mouse NIH/3T3 cells assessed as decrease in cell viability, IC50=0.05μM	31121546
HeLa	Cytotoxicity against			Cytotoxicity against human HeLa cells assessed as decrease in cell viability, IC50=0.087μM	31121546
Jurkat	Cytotoxicity against			Cytotoxicity against human Jurkat cells assessed as decrease in cell viability, IC50=0.14μM	31121546
MDCK	Cytotoxicity against			Cytotoxicity against MDCK cells assessed as decrease in cell viability, IC50=1.2μM	31121546
Pkd1-/-	Induction of			Induction of cell growth arrest in mouse Pkd1-/- cells in presence of calcium	17360534
点击查看更多细胞系数据

生物活性

产品描述

靶点

NF-κB ^[1]

HSF1 ^[1]

MDM2 ^[1]

体外研究(In Vitro)
体外研究活性	Triptolide是一种三环氧二萜类化合物，具有强效的免疫抑制和抗炎性能。在嘌呤盒/核因子和NF-κB介导的转录激活水平，Triptolide能够抑制激活的T细胞中IL-2的表达。^[1] Triptolide在极低浓度下(2–10纳克/毫升)能够抑制肿瘤细胞的增殖和集落形成。Triptolide对乳腺癌，胃癌和白血病细胞系HL-60细胞具有抑制活性。在肿瘤细胞中，Triptolide通过阻断NF-κB激活并使肿瘤细胞对TNF-&alpha诱导的程序性细胞死亡敏感来诱导细胞凋亡。^[2]
实验图片	检测方法	检测指标	实验图片	PMID
	Western blot	c-Jun MDM2 p-AKT / AKT / p-Foxo3a / Foxo3a / p53 p-PI3K / PI3K / p85 / p110		22666381
	Growth inhibition assay	Cell viability		22666381

体内研究(In Vivo)
体内研究活性	Triptolide与cyclosporin A协同促进动物模型中移植物的存活，并协同抑制同种异体骨髓移植伴随的移植物抗宿主病。此外，通过抑制c-IAP2 和c-IAP1的诱导作用，它会引起肿瘤细胞的细胞凋亡，同时部分增强肿瘤坏死因子(TNF-α)诱导的细胞凋亡。^[1] ^[3] Triptolide治疗2-3周抑制由四种不同肿瘤细胞系(B16 黑色素瘤，MDA-435 乳腺癌，TSU 膀胱癌，以及MGC80-3 胃癌)形成的异种移植物的生长，表明TPL具有广谱的抗肿瘤活性，对野生型和突变体p53均具有作用。此外，在实验中，Triptolide抑制B16F10细胞转移到小鼠的肺和脾脏中。^[2] 在小鼠模型中，Triptolide在体内外均具有抗多囊性肾病的作用。^[4] LD50: 小鼠0.83毫克/千克(静脉注射)。 ^[5]

参考文献
[1] Qiu D, et al. J Biol Chem, 1999, 274(19), 13443-13450. [2] Yang S, et al. Mol Cancer Ther, 2003, 2(1), 65-72. [3] Lee KY, et al. J Biol Chem, 1999, 274(19), 13451-13455. [4] Leuenroth SJ, et al. Proc Natl Acad Sci, 2007, 104(11), 4389-4394. [5] Xu L, et al. Food Chem Toxicol, 2013, 57, 371-379. + 展开

参考文献

+ 展开

化学信息&溶解度

分子量	360.4	分子式	C₂₀H₂₄O₆
CAS号	38748-32-2	SDF	Download Triptolide SDF
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 72 mg/mL ( (199.77 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 72 mg/mL ( (199.77 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解配方批次：现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂				动物体内配方计算器
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	2%DMSO 1 30%PEG300 2 2%Tween80 3 66%ddH2O 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	3.000mg/ml (8.32mM)	以 1 mL 工作液为例，取20μL150mg/ml的澄清DMSO储备液加到300μL PEG300中，混合均匀使其澄清；向上述体系中加入20μLTween80，混合均匀使其澄清；然后继续加入660μL ddH2O定容至 1 mL。工作液请现配现用！

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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