| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Phellamurin targets intestinal P-glycoprotein (P-gp), an efflux transporter that pumps drugs and xenobiotics out of cells. By inhibiting P-gp, phellamurin may increase the bioavailability of co-administered drugs that are substrates of P-gp. The compound also exhibits antioxidant, anti-inflammatory, and antimicrobial activities through various mechanisms. As a flavonoid, phellamurin may modulate multiple signaling pathways involved in inflammation and oxidative stress.
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| ln Vitro |
In U2OS and Saos-2 cells, pellamurin (0–10 μg/mL; 48 hours) treatment reduces cell viability in a dose-dependent way[1]. Phellamurin treatment (0-10 μg/mL; 48 hours; U2OS and Saos-2 cells) concentration-dependently promotes apoptosis in U2OS and Saos-2 cells[1]. Phellamurin treatment (0-10 μg/mL; 48 hours; U2OS and Saos-2 cells) reduces the ratios of p-mTOR/mTOR, p-AKT/AKT, and p-PI3K/PI3K in U2OS and Saos-2 cells[1].
In vitro, phellamurin has been shown to inhibit intestinal P-glycoprotein in a dose-dependent manner. The compound exhibits antioxidant activity by scavenging free radicals and reducing oxidative stress. It also shows anti-inflammatory activity by inhibiting the production of inflammatory mediators. Antimicrobial activity has been demonstrated against various pathogens. These in vitro studies demonstrate the compound's potential for drug interaction studies and as a therapeutic agent for inflammatory and infectious diseases. |
| ln Vivo |
Osteosarcoma tumor growth is inhibited in vivo by phenellamurin (50 mg/kg/day; intraperitoneal injection; daily; for 21 days; female BALB/c nude mice). Phellamurin-treated animals have lower ratios of p-PI3K/PI3K, p-AKT/AKT, and p-mTOR/mTOR in xenografts[1].
In vivo, phellamurin has been studied for its effects on P-glycoprotein activity and drug bioavailability. The compound's ability to inhibit intestinal P-gp may increase the bioavailability of co-administered drugs. Further in vivo studies are needed to evaluate its therapeutic potential and safety. |
| Enzyme Assay |
The in vitro P-glycoprotein inhibition assay for phellamurin measures its ability to inhibit P-gp efflux activity. The assay is performed using P-gp-overexpressing cell lines and fluorescent or radiolabeled P-gp substrates (e.g., rhodamine 123, calcein-AM). Cells are treated with phellamurin at various concentrations, and substrate accumulation is measured by fluorescence or scintillation counting. IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: U2OS and Saos-2 cells Tested Concentrations: 0 μg/mL, 2.5 μg/mL, 5 μg/mL, and 10 μg/mL Incubation Duration: 48 hrs (hours) Experimental Results: Suppressed the viability of U2OS and Saos-2 cells in a concentration-dependent manner. Apoptosis Analysis[1] Cell Types: U2OS and Saos-2 cells Tested Concentrations: 0 μg/mL, 2.5 μg/mL, 5 μg/mL, and 10 μg /mL Incubation Duration: 48 hrs (hours) Experimental Results: Induced apoptosis of U2OS and Saos-2 cells in a concentration-dependent manner. Western Blot Analysis[1] Cell Types: U2OS and Saos-2 cells Tested Concentrations: 0 μg/mL and 10 μg/ mL Incubation Duration: 48 hrs (hours) Experimental Results: Repressed the PI3K/AKT/mTOR pathway in U2OS and Saos-2 cells. In vitro cellular studies are conducted using P-gp-overexpressing cell lines (e.g., Caco-2, MDCK-MDR1). Cells are treated with phellamurin at various concentrations, and P-gp activity is measured by assessing the accumulation of fluorescent substrates. Antioxidant activity is assessed by measuring reactive oxygen species (ROS) levels and antioxidant enzyme activity. Anti-inflammatory activity is evaluated by measuring cytokine production and inflammatory marker expression. Antimicrobial activity is assessed by measuring minimum inhibitory concentrations (MIC) against various pathogens. |
| Animal Protocol |
Animal/Disease Models: Athymic female BALB/c nude mice (6 weeks old ) injected with U2OS cells[1]
Doses: 50 mg/kg/day Route of Administration: intraperitoneal (ip)injection; daily; for 21 days Experimental Results: Repressed osteosarcoma tumor growth in vivo. In vivo animal experiments with phellamurin are limited. The compound is a natural product used in research on drug transporters, inflammation, and oxidative stress. Further in vivo studies are needed to evaluate its therapeutic potential and safety. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of phellamurin include its solubility and stability. The compound has a molecular weight of 518.51 g/mol and molecular formula C26H30O11. It appears as a solid and should be stored under recommended conditions. The compound should be protected from light and moisture. Purity is typically high for research-grade material.
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| Toxicity/Toxicokinetics |
Toxicological data for phellamurin are derived from its use as a natural product in research. The compound is for research use only and not intended for human therapeutic applications. No significant toxicity has been reported at effective concentrations. Standard safety precautions should be followed when handling the compound. Long-term toxicity and carcinogenicity studies have not been conducted.
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| References |
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| Additional Infomation |
Phellamurin is a dihydroflavonol compound with the structure (+)-dihydrokaempferol, substituted at the 8-position by an isopentenyl group and at the 7-position by a β-D-glucopyranoyl group via a glycosidic bond. Isolated from Phellodendron amurense and Commiphora africana, phaellamurin exhibits inhibitory activity against intestinal P-glycoprotein. It is a metabolite. Phellamurin belongs to the dihydroflavonol, flavanone glycoside, trihydroxyflavanone, monosaccharide derivative, β-D-glucoside, and 4'-hydroxyflavanone classes. Its function is related to (+)-dihydrokaempferol. It has been reported to exist in Phellodendron chinense var. glabriusculum, Phellodendron amurense var. wilsonii, and other organisms with relevant data.
Phellamurin is a trihydroxyflavanone and bioactive natural compound from Phellodendron species. It inhibits intestinal P-glycoprotein in a dose-dependent manner and exhibits antioxidant, anti-inflammatory, and antimicrobial activities. The compound has the molecular formula C26H30O11 and molecular weight of 518.51 g/mol. It is used in compound screening libraries, metabolomics, phytochemical research, and drug interaction studies. Phellamurin is a flavonoid glycoside and is sourced from the barks of Phellodendron chinense Schneid. |
| Molecular Formula |
C26H30O11
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| Molecular Weight |
518.51
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| Exact Mass |
518.178
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| CAS # |
52589-11-4
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| PubChem CID |
193876
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
861.5±65.0 °C at 760 mmHg
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| Flash Point |
290.7±27.8 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.672
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| LogP |
2.14
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
37
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| Complexity |
808
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| Defined Atom Stereocenter Count |
7
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| SMILES |
CC(=CCC1=C(C=C(C2=C1O[C@@H]([C@H](C2=O)O)C3=CC=C(C=C3)O)O)O[C@H]4[C@@H]([C@H]([C@@H]([C@H](O4)CO)O)O)O)C
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| InChi Key |
GRDZTDZJQRPNCN-YIANMRPHSA-N
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| InChi Code |
InChI=1S/C26H30O11/c1-11(2)3-8-14-16(35-26-23(34)21(32)19(30)17(10-27)36-26)9-15(29)18-20(31)22(33)24(37-25(14)18)12-4-6-13(28)7-5-12/h3-7,9,17,19,21-24,26-30,32-34H,8,10H2,1-2H3/t17-,19-,21+,22+,23-,24-,26-/m1/s1
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| Chemical Name |
(2R,3R)-3,5-dihydroxy-2-(4-hydroxyphenyl)-8-(3-methylbut-2-enyl)-7-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-2,3-dihydrochromen-4-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 | 1.9286 mL | 9.6430 mL | 19.2860 mL | |
| 5 mM | 0.3857 mL | 1.9286 mL | 3.8572 mL | |
| 10 mM | 0.1929 mL | 0.9643 mL | 1.9286 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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