| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Luffariellolide targets human synovial fluid phospholipase A2 (HSF-PLA2) with an IC50 of 5 µM. It is also an agonist for the retinoic acid receptors RARα, RARβ, and RARγ. It inhibits hypoxia (1% O2)-induced HIF-1 activation and inhibits cell growth.
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|---|---|
| ln Vitro |
In vitro, Luffariellolide inhibits HSF-PLA2 with an IC50 of 5 µM. It is a novel RAR agonist, inducing co-activator binding to RA receptors, further inhibiting cell growth and regulating RAR target genes in various cancer cells.
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| ln Vivo |
In vivo, Luffariellolide effectively inhibits phorbol ester (PMA)-induced ear edema with an ED50 of 50 µg/ear. It has been studied for its anti-inflammatory and anticancer activities. Detailed pharmacokinetic data are limited.
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| Enzyme Assay |
HSF-PLA2 inhibition is assessed using enzyme activity assays. Human synovial fluid phospholipase A2 is incubated with a phospholipid substrate and varying concentrations of Luffariellolide. The release of a fluorescent or radiolabeled product is measured. IC50 values for enzyme inhibition are calculated from dose-response curves. RAR agonism is assessed using cell-based reporter gene assays.
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| Cell Assay |
For cellular assays, cancer cell lines are treated with Luffariellolide at varying concentrations (0.1-100 µM). Cell viability is assessed by MTT assay. RAR target gene expression is measured by qRT-PCR. HIF-1 activation is assessed by measuring the expression of HIF-1 target genes under hypoxic conditions.
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| Animal Protocol |
For in vivo efficacy studies, mouse models of inflammation (e.g., PMA-induced ear edema) are used. Luffariellolide is applied topically at doses of 10-100 µg/ear. Ear thickness and weight are measured. For anticancer studies, tumor xenograft models are used. The compound is administered intraperitoneally or orally. Pharmacokinetic parameters are determined.
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| References | |
| Additional Infomation |
Luffariellolide is a diterpenoid lactone. It has been reported to exist in Fascaplysinopsis, Acanthodendrilla, and other organisms with relevant data.
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| Molecular Formula |
C25H38O3
|
|---|---|
| Molecular Weight |
386.56742
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| Exact Mass |
386.282
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| CAS # |
111149-87-2
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| PubChem CID |
5387248
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| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.0±0.1 g/cm3
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| Boiling Point |
541.7±50.0 °C at 760 mmHg
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| Flash Point |
209.3±22.9 °C
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| Vapour Pressure |
0.0±3.3 mmHg at 25°C
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| Index of Refraction |
1.517
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| Source |
Originated from animals: Palauan sponge
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| LogP |
7.27
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| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
28
|
| Complexity |
689
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C/C(=C\CCC1=CC(=O)OC1O)/CC/C=C(\C)/CCC2=C(C)CCCC2(C)C
|
| InChi Key |
JPWPYTMXSXYUPG-QZPYEDBESA-N
|
| InChi Code |
InChI=1S/C25H38O3/c1-18(11-7-13-21-17-23(26)28-24(21)27)9-6-10-19(2)14-15-22-20(3)12-8-16-25(22,4)5/h10-11,17,24,27H,6-9,12-16H2,1-5H3/b18-11+,19-10+
|
| Chemical Name |
3-[(3E,7E)-4,8-dimethyl-10-(2,6,6-trimethylcyclohexen-1-yl)deca-3,7-dienyl]-2-hydroxy-2H-furan-5-one
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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 | 2.5869 mL | 12.9343 mL | 25.8685 mL | |
| 5 mM | 0.5174 mL | 2.5869 mL | 5.1737 mL | |
| 10 mM | 0.2587 mL | 1.2934 mL | 2.5869 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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