| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
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| Targets |
PLA2 2.6 μM (IC50)
Rapanone targets human synovial phospholipase A2 (PLA2) with an IC50 of 2.6 μM. It also exhibits activity against apoptosis, bacterial, and parasitic targets. The compound's mechanisms of action include mitochondrial disruption and apoptosis induction. |
|---|---|
| ln Vitro |
In primary rats hepatocytes and HepG2 cells, rapanone (10–40 μM; 24 h) reduces cell viability with IC50s of 35.58 μM and 27.89 μM, respectively[1]. HepG2 cells are exposed to rapanone (10–40 μM) for 24 hours, which causes concentration-dependent ATP depletion, phosphatidyl serine externalization, hydrogen peroxide formation, and mitochondrial membrane potential dissipation[1]. Rapanone induces mitochondrial dysfunction by blocking electron transport at Complex III[1].
Rapanone exhibits a broad spectrum of biological actions, including anti-tumor, antioxidant, anti-inflammatory, antibacterial, and antiparasitic activities. It is a potent and selective human synovial PLA2 inhibitor with an IC50 of 2.6 μM. |
| ln Vivo |
Mice with the carrageenan paw oedema paradigm have anti-inflammatory benefits when exposed to rapanone (2.5-10 mg/kg; ip)[4].
In vivo, Rapanone has shown anti-tumor, antioxidant, anti-inflammatory, antibacterial, and antiparasitic activities. Its mechanisms include mitochondrial disruption and apoptosis induction. Specific in vivo data are not extensively reported. |
| Enzyme Assay |
PLA2 inhibition assays are performed using recombinant human synovial PLA2. Rapanone is incubated with the enzyme and substrate, and inhibition of PLA2 activity is measured. IC50 values are determined from dose-response curves.
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| Cell Assay |
Cell-based assays are conducted to evaluate Rapanone's anti-tumor, antioxidant, anti-inflammatory, antibacterial, and antiparasitic activities. Apoptosis is assessed by measuring mitochondrial disruption and caspase activation.
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| Animal Protocol |
In vivo studies are performed in animal models to evaluate anti-tumor, anti-inflammatory, and antimicrobial activities. Specific dosing and administration details are not extensively reported.
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| ADME/Pharmacokinetics |
Rapanone has a molecular weight of 322.44 and a molecular formula of C19H30O4. Storage: powder at -20°C for up to 3 years; in solvent at -80°C for up to 6 months.
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| Toxicity/Toxicokinetics |
Rapanone is a research compound not intended for human use. Standard laboratory safety precautions should be followed when handling the compound.
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| References |
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| Additional Infomation |
Lapazone is a dihydroxy-1,4-benzoquinone compound. It has been reported to exist in Tapeinosperma pseudojambosa, Embelia schimperi, and other organisms with relevant data.
Rapanone is a natural benzoquinone with a broad spectrum of biological activities. It is a selective human synovial PLA2 inhibitor (IC50 = 2.6 μM) and exhibits anti-tumor, antioxidant, anti-inflammatory, antibacterial, and antiparasitic effects. Synonyms include 2,5-Dihydroxy-3-tridecyl-[1,4]benzoquinone. |
| Molecular Formula |
C19H30O4
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|---|---|
| Molecular Weight |
322.44
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| Exact Mass |
322.214
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| CAS # |
573-40-0
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| PubChem CID |
100659
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| Appearance |
Light yellow to orange solid powder
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| Density |
1.099g/cm3
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| Boiling Point |
457ºC at 760mmHg
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| Melting Point |
142-145ºC
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| Flash Point |
244.3ºC
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| Index of Refraction |
1.53
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| LogP |
5.093
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
23
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| Complexity |
460
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
AMKNOBHCKRZHIO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H30O4/c1-2-3-4-5-6-7-8-9-10-11-12-13-15-18(22)16(20)14-17(21)19(15)23/h14,20,23H,2-13H2,1H3
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| Chemical Name |
2,5-dihydroxy-3-tridecylcyclohexa-2,5-diene-1,4-dione
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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) |
DMSO : 25 mg/mL (77.53 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.75 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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1014 mL | 15.5068 mL | 31.0135 mL | |
| 5 mM | 0.6203 mL | 3.1014 mL | 6.2027 mL | |
| 10 mM | 0.3101 mL | 1.5507 mL | 3.1014 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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