5,7-Dimethoxyflavone

Cat No.:V40552 Purity: ≥98%
5,7-Dimethoxyflavone is one of the major components of Kaempferia parviflora and has anti-obesity, anti~inflammatory and anti-tumor effects.
5,7-Dimethoxyflavone Chemical Structure CAS No.: 21392-57-4
Product category: Cytochrome P450
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
5,7-Dimethoxyflavone is one of the major components of Kaempferia parviflora and has anti-obesity, anti~inflammatory and anti-tumor effects. 5,7-Dimethoxyflavone inhibits cytochrome P450 (CYP) 3As. 5,7-Dimethoxyflavone is also a potent inhibitor of breast cancer protein (BCRP).
Biological Activity I Assay Protocols (From Reference)
ln Vitro
In MDCK/Bcrp1 cells, 5,7-Dimethoxyflavone (5 and 50 μM, 1 hour) inhibits Bcrp1-mediated sorafenib efflux [2]. In B16F10 melanoma cells, 5,7-dimethoxyflavone (0-25 μM, 48 hours) promotes melanogenesis by raising cAMP [4]. 5,7-dimethoxyflavone (0 - 100 μM, 48 hours) can block ischemia, promote oxidative termination, and trigger apoptosis in VK2/E6E7 and End1/E6E7 cells. It can also dilute the cells in cells by accumulation of TG in 3T3-L1 adipocytes [6].Cell.
ln Vivo
In mouse liver, 5,7-dimethoxyflavone (10 mg/kg, facial, once daily for 10 days) can lower the expression levels of CYP3A11 and CYP3A25 proteins [1]. In HFD mice, 5,7-Dimethoxyflavone (25 and 50 mg/kg, face) and 5,7-Dimethoxyflavone (50 mg/kg/d, epidermis, for 6 weeks) decrease body weight while increasing and inhibiting liver function[5].
Cell Assay
Western Blot Analysis[4]
Cell Types: B16F10 melanoma cells
Tested Concentrations: 0-25 μM
Incubation Duration: 48 hrs (hours)
Experimental Results: Induces CREB phosphorylation and inhibits Akt and GSK-3β phosphorylation.
Animal Protocol
Animal/Disease Models: Aged mice [3]
Doses: 25 and 50 mg/kg
Route of Administration: Oral
Experimental Results: Increased grip strength and running endurance. Increase muscle size, weight, and cross-sectional area. Serum and gastrocnemius muscle IL-6 and TNF-α levels were diminished.
References
[1]. Ochiai W, et al. Effect of the active ingredient of Kaempferia parviflora, 5,7-dimethoxyflavone, on the pharmacokinetics of midazolam. J Nat Med. 2018 Jun;72(3):607-614.
[2]. Bae S, et al. Effect of 5,7-dimethoxyflavone on Bcrp1-mediated transport of sorafenib in vitro and in vivo in mice. Eur J Pharm Sci. 2018 May 30;117:27-34.
[3]. Kim C, Hwang JK. The 5,7-Dimethoxyflavone Suppresses Sarcopenia by Regulating Protein Turnover and Mitochondria Biogenesis-Related Pathways. Nutrients. 2020 Apr 13;12(4):1079.
[4]. Kang YG, et al. 5,7-dimethoxyflavone induces melanogenesis in B16F10 melanoma cells through cAMP-dependent signalling. Exp Dermatol. 2011 May;20(5):445-7.
[5]. Song Y, et al. 5,7-Dimethoxyflavone Attenuates Obesity by Inhibiting Adipogenesis in 3T3-L1 Adipocytes and High-Fat Diet-Induced Obese C57BL/6J Mice. J Med Food. 2016 Dec;19(12):1111-1119.
[6]. Park W, et al. 5,7-Dimethoxyflavone induces apoptotic cell death in human endometriosis cell lines by activating the endoplasmic reticulum stress pathway. Phytother Res. 2020 Sep;34(9):2275-2286.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C17H14O4
Molecular Weight
282.2907
CAS #
21392-57-4
SMILES
O1C(C2C([H])=C([H])C([H])=C([H])C=2[H])=C([H])C(C2C(=C([H])C(=C([H])C1=2)OC([H])([H])[H])OC([H])([H])[H])=O
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)
Solubility Data
Solubility (In Vitro)
DMSO : ~62.5 mg/mL (~221.40 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.86 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 (8.86 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.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (7.37 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline 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 3.5425 mL 17.7123 mL 35.4246 mL
5 mM 0.7085 mL 3.5425 mL 7.0849 mL
10 mM 0.3542 mL 1.7712 mL 3.5425 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.

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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