| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
| Targets |
The primary molecular target of triptolide is the transcription factor XPB (xeroderma pigmentosum group B-complementing protein), a subunit of the TFIIH complex involved in RNA polymerase II-mediated transcription. Triptolide covalently binds to XPB, inhibiting transcription and leading to decreased expression of many genes. This broad transcriptional inhibition underlies its diverse pharmacological effects, including immunosuppressive and anticancer activities. The compound may also affect other targets such as HSP90 and NF-κB.
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| ln Vitro |
In vitro studies have demonstrated the potent anticancer activity of triptolide against various cancer cell lines, including leukemia, pancreatic, lung, breast, and ovarian cancer cells. The compound has IC₅₀ values in the low nanomolar range. Triptolide induces apoptosis, inhibits cell proliferation, and suppresses angiogenesis. The compound also exhibits potent immunosuppressive activity, inhibiting T-cell proliferation and cytokine production. Anti-inflammatory activity has been demonstrated through inhibition of NF-κB and other inflammatory pathways.
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| ln Vivo |
In vivo studies have shown the efficacy of triptolide in animal models of cancer, autoimmune diseases, and inflammatory conditions. The compound has demonstrated antitumor activity in mouse xenograft models of various cancers. Immunosuppressive effects have been shown in models of rheumatoid arthritis, lupus, and organ transplantation. However, triptolide's narrow therapeutic window and significant toxicity limit its clinical application. The compound is used as a research tool and lead compound for derivative development.
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| Enzyme Assay |
For in vitro activity assays, standard cell viability assays (MTT, MTS, or resazurin) are used with various cancer cell lines. Cells are treated with serial dilutions of triptolide, and IC₅₀ values are calculated. For mechanism studies, Western blotting is used to analyze protein expression, and qPCR for gene expression. Transcription inhibition can be assessed by measuring RNA synthesis using radioactive or fluorescent labels. XPB binding can be studied using biochemical or biophysical methods.
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| Cell Assay |
For in vitro cell-based studies, various cancer cell lines (e.g., HeLa, MCF-7, A549, Jurkat) are cultured in appropriate media and treated with serial dilutions of triptolide. Cell viability, apoptosis, cell cycle distribution, and protein expression are analyzed. For immunosuppression studies, primary T-cells or T-cell lines are stimulated and treated with triptolide, and proliferation is measured by thymidine incorporation or CFSE dilution. Cytokine production is measured by ELISA.
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| Animal Protocol |
In vivo animal studies for triptolide typically use mouse models. For anticancer studies, tumor xenografts are established in immunodeficient mice, and triptolide is administered via intraperitoneal or oral routes. Tumor growth is monitored. For autoimmune studies, mouse models of rheumatoid arthritis or lupus are used. The compound is administered, and disease progression is assessed by clinical scores, histological analysis, and biomarker measurement. Standard protocols for these models are described in the literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of triptolide have been characterized. The compound has poor oral bioavailability due to extensive first-pass metabolism and P-glycoprotein efflux. It is highly protein bound. Triptolide has a short half-life and undergoes extensive metabolism via CYP450 enzymes, primarily CYP3A4. The compound's PK properties are challenging for therapeutic development. Specific PK parameters such as half-life, clearance, and bioavailability have been reported in the literature.
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| Toxicity/Toxicokinetics |
Triptolide has significant toxicity, limiting its clinical use. The compound causes severe gastrointestinal, hepatic, renal, and reproductive toxicity. The narrow therapeutic window is a major challenge for drug development. Triptolide is a potent teratogen. The toxicity is partly related to its mechanism of transcriptional inhibition. Many derivatives have been developed to improve the therapeutic index. Comprehensive toxicological data are available from studies of Tripterygium wilfordii extracts and purified triptolide.
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| References | |
| Additional Infomation |
There have been reports that Tripterygium wilfordii and Tripterygium hypoglaucum contain wilffordlin, and relevant data are available for reference.
Triptolide (wilfortrine) is a research compound with potent pharmacological activities and significant toxicity. It is a major bioactive component of Tripterygium wilfordii, a traditional Chinese medicine used for autoimmune and inflammatory diseases. Triptolide is used as a research tool for studying transcription, inflammation, and cancer biology. No triptolide-containing drugs have been approved in Western countries, though derivatives are in development. The compound serves as a lead for medicinal chemistry optimization to improve the therapeutic index. |
| Molecular Formula |
C41H47NO20
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|---|---|
| Molecular Weight |
873.81
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| Exact Mass |
873.269
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| CAS # |
37239-48-8
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| PubChem CID |
102004803
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
884.4±65.0 °C at 760 mmHg
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| Melting Point |
237.5-238.0°C(lit.)
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| Flash Point |
488.6±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.592
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| Source |
Originated from plants: Celastraceae Tripterygium wilfordii Hook. f.
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| LogP |
4.12
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
21
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
62
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| Complexity |
1840
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| Defined Atom Stereocenter Count |
12
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| SMILES |
CC(=O)OC[C@]12[C@@H]([C@@H]([C@@H]3[C@H]([C@]14[C@@]([C@H]([C@@H]([C@@H]2OC(=O)C)OC(=O)C5=COC=C5)OC(=O)[C@](CCC6=C(C=CC=N6)C(=O)OC[C@@]3(O4)C)(C)O)(C)O)OC(=O)C)OC(=O)C)OC(=O)C
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| InChi Key |
JOKOHWLSQAZHFX-DQZYHKMLSA-N
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| InChi Code |
InChI=1S/C41H47NO20/c1-19(43)54-18-40-32(58-22(4)46)28(56-20(2)44)27-30(57-21(3)45)41(40)39(8,52)31(29(33(40)59-23(5)47)60-34(48)24-12-15-53-16-24)61-36(50)37(6,51)13-11-26-25(10-9-14-42-26)35(49)55-17-38(27,7)62-41/h9-10,12,14-16,27-33,51-52H,11,13,17-18H2,1-8H3/t27-,28-,29+,30-,31+,32-,33+,37-,38+,39+,40-,41+/m1/s1
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| Chemical Name |
[(1S,3R,15R,18S,19R,20R,21R,22S,23R,24R,25R,26S)-20,22,23,25-tetraacetyloxy-21-(acetyloxymethyl)-15,26-dihydroxy-3,15,26-trimethyl-6,16-dioxo-2,5,17-trioxa-11-azapentacyclo[16.7.1.01,21.03,24.07,12]hexacosa-7(12),8,10-trien-19-yl] furan-3-carboxylate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~50 mg/mL (~57.2 mM; with ultrasonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (1.43 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (12.5 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (1.43 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (12.5 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1444 mL | 5.7221 mL | 11.4441 mL | |
| 5 mM | 0.2289 mL | 1.1444 mL | 2.2888 mL | |
| 10 mM | 0.1144 mL | 0.5722 mL | 1.1444 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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