| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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Fraxinellone is a naturally occurring anti-inflammatory agent isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone acts a PD-L1 inhibitor and inhibitor of HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone was able to inhibit LPS-induced nitric oxide (NO) and prostaglandin E(2) (PGE(2)) production, and to reduce the LPS-induced expressions of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) at the mRNA and protein levels in a dose-dependent manner.
| ln Vitro |
In A549 cells, fraxinellone (0-100 μM; 12 hours) lowers the proportion of PD-L1-positive cells from 20.4% to 11.4% [1].
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|---|---|
| ln Vivo |
Oral gavage of fraxinellone (30 and 100 mg/kg; every three days; 30 days) effectively reduced the amount of HIF-1α, pTyr705 STAT3, PD-L1, and VEGF-stained animals and suppressed tumor growth [1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: A549 cells Tested Concentrations: 0 μM, 10 μM, 30 μM, 100 μM Incubation Duration: 12 hrs (hours) Experimental Results: Inhibited the percent of PD-L1 positive cells. |
| Animal Protocol |
Animal/Disease Models: BALB/c nude mice[1]
Doses: 30 and 100 mg/kg Route of Administration: po (oral gavage); 30 and 100 mg/kg; every three days; 30 days Experimental Results: Dramatically suppressed tumor growth. |
| References | |
| Additional Infomation |
Fraxinellone is a member of 2-benzofurans.
Fraxinellone has been reported in Raulinoa echinata, Fagaropsis glabra, and other organisms with data available. |
| Molecular Formula |
C14H16O3
|
|---|---|
| Molecular Weight |
232.2750
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| Exact Mass |
232.109
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| CAS # |
28808-62-0
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| PubChem CID |
124039
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
372.9±30.0 °C at 760 mmHg
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| Melting Point |
116ºC
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| Flash Point |
179.3±24.6 °C
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| Vapour Pressure |
0.0±0.8 mmHg at 25°C
|
| Index of Refraction |
1.552
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| LogP |
2.85
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
17
|
| Complexity |
385
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| Defined Atom Stereocenter Count |
2
|
| SMILES |
CC1=C2C(=O)O[C@H]([C@@]2(CCC1)C)C3=COC=C3
|
| InChi Key |
XYYAFLHHHZVPRN-GXTWGEPZSA-N
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| InChi Code |
InChI=1S/C14H16O3/c1-9-4-3-6-14(2)11(9)13(15)17-12(14)10-5-7-16-8-10/h5,7-8,12H,3-4,6H2,1-2H3/t12-,14+/m0/s1
|
| Chemical Name |
(3R,3aR)-3-(furan-3-yl)-3a,7-dimethyl-3,4,5,6-tetrahydro-2-benzofuran-1-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) |
DMSO : ~100 mg/mL (~430.51 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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: ≥ 2.5 mg/mL (10.76 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 | 4.3051 mL | 21.5257 mL | 43.0515 mL | |
| 5 mM | 0.8610 mL | 4.3051 mL | 8.6103 mL | |
| 10 mM | 0.4305 mL | 2.1526 mL | 4.3051 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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