| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Wilfordine targets Na+-K+-ATPase, which may be an acting target of wilfordine against some insect larvae. It may also inhibit acetylcholinesterase, contributing to its insecticidal and antibacterial effects. By inhibiting Na+-K+-ATPase, it disrupts ion gradients across plasma membranes, affecting nerve impulse transmission and cellular function.
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| ln Vitro |
Wilfordine demonstrates insecticidal activity against various insect larvae. It shows inhibitory effects on the growth of bacteria by inhibiting acetylcholinesterase. It has synergistic effects with chemical pesticides, such as those from Tripterygium. In vitro, it may also exhibit cytotoxic effects against cancer cell lines.
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| ln Vivo |
In vivo, Wilfordine exhibits insecticidal activity in insect models. It has been shown to have synergistic effects with chemical pesticides. The compound's activity against Na+-K+-ATPase suggests potential for cardiovascular and neurological effects in mammals. However, detailed in vivo pharmacological studies are limited.
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| Enzyme Assay |
Cell-free enzyme assays for Wilfordine: Na+-K+-ATPase activity is measured using membrane preparations from insect or mammalian tissues. The enzyme is incubated with ATP and varying concentrations of Wilfordine (0.1-100 µM). Inorganic phosphate released from ATP hydrolysis is quantified colorimetrically. Acetylcholinesterase inhibition is assessed using Ellman's method with acetylthiocholine as substrate.
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| Cell Assay |
Cellular assays for Wilfordine: insect cell lines (e.g., Sf9 cells) or mammalian cells are treated with Wilfordine at concentrations of 0.1-100 µM for 24-72 hours. Cell viability is measured using MTT or CellTiter-Glo assays. Na+-K+-ATPase activity in treated cells is assessed by measuring ouabain-sensitive ATPase activity. Apoptosis and cell cycle analysis are performed by flow cytometry.
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| Animal Protocol |
In vivo animal studies for Wilfordine: insect models (e.g., larvae of Spodoptera or Helicoverpa species) are used to evaluate insecticidal activity. Wilfordine is applied topically or incorporated into diet at various concentrations. Mortality and growth inhibition are recorded. In mammalian models, the compound is administered to evaluate potential toxicity and pharmacological effects.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Wilfordine are limited. As a complex alkaloid, it may have poor oral bioavailability. It is likely metabolized in the liver by esterases and cytochrome P450 enzymes. Tissue distribution and elimination pathways require further investigation. The compound's large molecular size (883.85) may limit membrane permeability and tissue penetration.
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| Toxicity/Toxicokinetics |
Toxicity of Wilfordine: as an insecticidal alkaloid from Tripterygium wilfordii, it may exhibit significant toxicity in mammals. Tripterygium preparations are known for hepatotoxicity, nephrotoxicity, and reproductive toxicity. Wilfordine should be handled with caution. No clinical use has been approved due to safety concerns. The compound is for research use only.
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| References | |
| Additional Infomation |
Wilfordine is a sesquiterpene compound. It has been reported to exist in Tripterygium wilfordii, Tripterygium hypoglaucum, and Tripterygium forrestii, and relevant data are available for reference.
Wilfordine is a research compound used for studying insecticidal mechanisms and Na+-K+-ATPase inhibition. It is a minor constituent of Tripterygium wilfordii extracts. Its mechanism involves ion pump inhibition and acetylcholinesterase inhibition. No clinical trials or FDA approvals have been reported. The compound is available as a reference standard for analytical and pharmacological studies. |
| Molecular Formula |
C43H49NO19
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|---|---|
| Molecular Weight |
883.84
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| Exact Mass |
883.289
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| CAS # |
37239-51-3
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| PubChem CID |
442556
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
895.5±65.0 °C at 760 mmHg
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| Flash Point |
495.4±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.598
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| LogP |
5.05
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
20
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
63
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| Complexity |
1850
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| Defined Atom Stereocenter Count |
11
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| SMILES |
O1[C@]2(C([H])([H])[H])C([H])([H])OC(C3C([H])=C([H])C([H])=NC=3C([H])([H])C([H])([H])C(C([H])([H])[H])(C(=O)O[C@@]3([H])[C@@]([H])([C@@]([H])([C@@]4(C([H])([H])OC(C([H])([H])[H])=O)[C@@]([H])(C([H])(C2([H])[C@]([H])([C@@]14C3(C([H])([H])[H])O[H])OC(C([H])([H])[H])=O)OC(C([H])([H])[H])=O)OC(C([H])([H])[H])=O)OC(C([H])([H])[H])=O)OC(C1C([H])=C([H])C([H])=C([H])C=1[H])=O)O[H])=O
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| InChi Key |
XQDBHSNYTFRCNJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C43H49NO19/c1-21(45)55-20-42-34(59-24(4)48)30(57-22(2)46)29-32(58-23(3)47)43(42)41(8,54)33(31(35(42)60-25(5)49)61-36(50)26-13-10-9-11-14-26)62-38(52)39(6,53)17-16-28-27(15-12-18-44-28)37(51)56-19-40(29,7)63-43/h9-15,18,29-35,53-54H,16-17,19-20H2,1-8H3
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| Chemical Name |
[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] benzoate
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1314 mL | 5.6571 mL | 11.3143 mL | |
| 5 mM | 0.2263 mL | 1.1314 mL | 2.2629 mL | |
| 10 mM | 0.1131 mL | 0.5657 mL | 1.1314 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05166616 | Recruiting | Procedure: Biopsy Drug: Osimertinib Drug: Triptolide Analog |
Stage III Lung Cancer AJCC v8 Stage IV Lung Cancer AJCC v8 |
City of Hope Medical Center | March 7, 2022 | Phase 1 |
| NCT00801268 | Terminated | Drug: tripterygium wilfordii Drug: Emodin |
Polycystic Kidney | Zhi-Hong Liu, M.D. | November 2008 | Not Applicable |
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