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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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Rhamnocitrin is a novel and potent naturally occurring flavonoid isolated from astragalus complanatus R. Br. Rhamnocitrin is a scavenger of DPPH(IC50 = 28.38 mM.) Rhamnocitrin has multipul bioactivities such as anti-oxidant activity, anti-inflammatory activity and an-tiatherosclerosis activity.
Targets |
Rhamnocitrin was shown to inhibit LDL oxidation (IC50: 12.5 μM) and reduce reactive oxygen species (ROS) production in macrophages, suggesting potential antioxidant and anti-inflammatory targets.
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ln Vitro |
Rhamnocitrin (0.1–10 μM) dose-dependently suppressed copper-induced LDL oxidation by 15–92% and decreased cholesteryl ester formation in macrophages by 23–69%. It downregulated ACAT-1 protein expression and reduced CD36 mRNA levels in oxidized LDL-treated macrophages.
[1]
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Enzyme Assay |
LDL oxidation assay: Human LDL incubated with 5 μM CuSO₄ and rhamnocitrin (0.1–10 μM) at 37°C for 24 h. Thiobarbituric acid-reactive substances (TBARS) measured at 532 nm to quantify inhibition.
ACAT activity assay: Macrophages pre-treated with oxidized LDL and rhamnocitrin (1–10 μM) for 24 h. Cellular cholesteryl ester content quantified via gas chromatography. [1] |
Cell Assay |
Macrophage foam cell formation: Mouse peritoneal macrophages incubated with 50 μg/mL oxidized LDL and rhamnocitrin (1–10 μM) for 48 h. Cells stained with Oil Red O, and lipid accumulation quantified spectrophotometrically.
Western blot: Macrophages treated with 10 μM rhamnocitrin for 24 h. ACAT-1 protein expression analyzed using specific antibodies. RT-PCR: CD36 mRNA levels measured in macrophages after 12 h treatment with 10 μM rhamnocitrin. [1] |
Animal Protocol |
Pharmacokinetic study: Rats (n=6) received 20 mg/kg rhamnocitrin via oral gavage (suspended in 0.5% carboxymethyl cellulose). Blood samples collected at 0.08, 0.25, 0.5, 1, 2, 4, 8, 12, and 24 h post-dose. Plasma separated by centrifugation and stored at −80°C until UHPLC-MS/MS analysis.
[2]
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ADME/Pharmacokinetics |
After oral administration (20 mg/kg) in rats, Rhamnocitrin showed rapid absorption (Tmax: 1.2 hours) with a Cmax of 1.8 μg/mL and elimination half-life (t1/2) of 4.3 hours.
[2]
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References |
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Additional Infomation |
Rhamnocitrin is an O-methylated flavonol isolated from Astragalus complanatus. It exhibits antiatherogenic effects by modulating cholesterol metabolism and suppressing foam cell formation.
[1]
Quantification of rhamnocitrin in biological samples uses UHPLC-MS/MS with a lower limit of detection (LLOD) of 0.5 ng/mL. [2] Rhamnocitrin is a monomethoxyflavone that is the 7-methyl ether derivative of kaempferol. It has a role as a plant metabolite. It is a trihydroxyflavone, a member of flavonols and a monomethoxyflavone. It is functionally related to a kaempferol. Rhamnocitrin has been reported in Populus szechuanica, Alpinia tonkinensis, and other organisms with data available. |
Molecular Formula |
C16H12O6
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Molecular Weight |
300.26288
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Exact Mass |
300.063
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Elemental Analysis |
C, 64.00; H, 4.03; O, 31.97
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CAS # |
569-92-6
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PubChem CID |
5320946
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Appearance |
White to yellow solid powder
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Density |
1.5±0.1 g/cm3
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Boiling Point |
571.9±50.0 °C at 760 mmHg
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Melting Point |
225-227ºC
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Flash Point |
218.4±23.6 °C
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Vapour Pressure |
0.0±1.7 mmHg at 25°C
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Index of Refraction |
1.710
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LogP |
2.56
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Hydrogen Bond Donor Count |
3
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Hydrogen Bond Acceptor Count |
6
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Rotatable Bond Count |
2
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Heavy Atom Count |
22
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Complexity |
465
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Defined Atom Stereocenter Count |
0
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SMILES |
COC1=CC(=C2C(=C1)OC(=C(C2=O)O)C3=CC=C(C=C3)O)O
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InChi Key |
MQSZRBPYXNEFHF-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C16H12O6/c1-21-10-6-11(18)13-12(7-10)22-16(15(20)14(13)19)8-2-4-9(17)5-3-8/h2-7,17-18,20H,1H3
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Chemical Name |
3,5-dihydroxy-2-(4-hydroxyphenyl)-7-methoxychromen-4-one
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Synonyms |
Kaempferol 7-O-methyl ether; Rhamnocitrin; 569-92-6; 7-Methylkaempferol; 3,4',5-Trihydroxy-7-methoxyflavone; 3,5-dihydroxy-2-(4-hydroxyphenyl)-7-methoxychromen-4-one; 4H-1-Benzopyran-4-one, 3,5-dihydroxy-2-(4-hydroxyphenyl)-7-methoxy-; CHEBI:80897; BZ59ZB4HBU; C.I. 75650; Rhamnocitrin; C.I-75650
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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 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)
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Solubility (In Vitro) |
DMSO : ~100 mg/mL (~333.04 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.93 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 20.8 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.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.3304 mL | 16.6522 mL | 33.3045 mL | |
5 mM | 0.6661 mL | 3.3304 mL | 6.6609 mL | |
10 mM | 0.3330 mL | 1.6652 mL | 3.3304 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.