| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Plasmodium
The primary target of tectol is farnesyltransferase (FTase), an enzyme involved in protein prenylation. Tectol inhibits human FTase with an IC₅₀ of 2.09 µM and Trypanosoma brucei FTase with an IC₅₀ of 1.73 µM. The compound also has anti-plasmodial activity against drug-resistant Plasmodium falciparum (FcB1) with an IC₅₀ of 3.44 µM. |
|---|---|
| ln Vitro |
In vitro studies have demonstrated the biological activities of tectol. The compound inhibits human and T. brucei FTase. Tectol shows anti-plasmodial activity against P. falciparum with an IC₅₀ of 3.44 µM. It exhibits significant activity against human leukemia cell lines HL60 and CEM. These activities support its potential for further investigation.
|
| ln Vivo |
In vivo activity of tectol has been studied in the context of its anti-plasmodial and antitumor effects. The compound has shown moderate anti-plasmodial activity. It exhibits significant activity against human leukemia cell lines. Specific in vivo data have been reported in the literature. Further studies are needed to fully characterize its in vivo efficacy.
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| Enzyme Assay |
For FTase inhibition assays, recombinant FTase is incubated with a fluorescent or radioactive substrate in the presence of tectol. Enzyme activity is measured, and IC₅₀ values are calculated. For anti-plasmodial assays, P. falciparum parasites are cultured and treated with serial dilutions of tectol. Parasite growth inhibition is assessed.
|
| Cell Assay |
For in vitro cell-based studies, leukemia cell lines (HL60, CEM) are cultured in appropriate media and treated with serial dilutions of tectol. Cell viability is assessed using MTT or other assays. For anti-plasmodial studies, P. falciparum parasites are cultured and treated with the compound. Parasite growth is assessed.
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| Animal Protocol |
In vivo animal studies for tectol have been conducted in models of malaria and cancer. The compound has shown anti-plasmodial activity. Standard protocols for in vivo efficacy studies are described in the literature.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of tectol have not been extensively characterized. As a lipophilic natural product, it is expected to have reasonable membrane permeability. Specific PK parameters such as half-life and bioavailability have not been reported. Further studies are needed.
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| Toxicity/Toxicokinetics |
Toxicological data for tectol are limited. Tectol may cause itchy dermatitis. As a natural product, it may have a favorable safety profile, but systematic toxicological studies have not been published. Standard safety assessments would be needed for therapeutic development.
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| References | |
| Additional Infomation |
Tectol has reportedly been found in Lippia origanoides, Markhamia stipulata, and other organisms with available data.
Tectol is a research compound used in studies of natural products and their biological activities. It is isolated from Lippia sidoides. The compound has anti-plasmodial, antitumor, and FTase inhibitory activities. No clinical trials or therapeutic applications have been reported. Tectol serves as a research tool for studying FTase inhibition, anti-plasmodial mechanisms, and antitumor activity. |
| Molecular Formula |
C30H26O4
|
|---|---|
| Molecular Weight |
450.53
|
| Exact Mass |
450.183
|
| CAS # |
24449-39-6
|
| PubChem CID |
161453
|
| Appearance |
White to off-white solid powder
|
| LogP |
7.439
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
34
|
| Complexity |
762
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
FVTJXDIACKJEPH-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C30H26O4/c1-29(2)15-13-21-23(25(31)17-9-5-7-11-19(17)27(21)33-29)24-22-14-16-30(3,4)34-28(22)20-12-8-6-10-18(20)26(24)32/h5-16,31-32H,1-4H3
|
| Chemical Name |
5-(6-hydroxy-2,2-dimethylbenzo[h]chromen-5-yl)-2,2-dimethylbenzo[h]chromen-6-ol
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 2.2196 mL | 11.0980 mL | 22.1961 mL | |
| 5 mM | 0.4439 mL | 2.2196 mL | 4.4392 mL | |
| 10 mM | 0.2220 mL | 1.1098 mL | 2.2196 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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