3,5,7,3′,4′-Pentamethoxyflavone
Based on 1 Customer Validation
3,5,7,3’,4’-Pentamethoxyflavone is a Ca2+ channel inhibitor. 3,5,7,3’,4’-Pentamethoxyflavone can protect DNA from oxidative damage. 3,5,7,3’,4’-Pentamethoxyflavone can induce relaxation of the human corpus cavernosum through calcium mobilization-related mechanisms. 3,5,7,3’,4’-Pentamethoxyflavone can promote the expression of eNOS and cystathionine gamma lyase CSE proteins in middle-aged male rats and regulate vascular function. 3,5,7,3’,4’-Pentamethoxyflavone can be used in research related to diabetes and cardiovascular diseases.
For research use only. We do not sell to patients.
- Purity: 99.69%
- CAS No.: 1247-97-8
- Formula: C20H20O7
- Molecular Weight:372.37
-
Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Membrane Transporter/Ion Channel Compound Library
HY-L011
-
Neuronal Signaling Compound Library
HY-L013
-
Natural Product Library
HY-L021
-
Anti-diabetic Compound Library
HY-L040
-
Anti-Cardiovascular Disease Compound Library
HY-L046
-
Orally Active Compound Library
HY-L061
-
Traditional Chinese Medicine Active Compound Library
HY-L065
-
Flavonoids Library
HY-L068
-
Neuroprotective Compound Library
HY-L070
-
Plant-Sourced Natural Product Library
HY-L115
-
Calcium Channel Blocker Library
HY-L117
-
Human Metabolite Library
HY-L123
-
Antihypertensive Compound Library
HY-L145
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Ion Channel Compound Library
HY-L166
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Natural Product Library Plus
HY-L021P
-
Natural Product and Natural Product-Like Compound Library
HY-L021M
-
Bioactive Compound Library
HY-L001
-
RO5 Drug-like Natural Product Library
HY-L200
-
High-Throughput Bioactive Compound Library
HY-L205
-
High-Throughput Natural Product Library
HY-L206
-
Mass Spectrometry Human Metabolite Library
HY-L215
-
Mass Spectrometry Natural Product Library
HY-L262
All Calcium Channel Isoforms
More
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| 2008 | IC50 |
26.35 μM
Compound: 10
|
Inhibition of MRP1 (unknown origin) expressed in human 2008 cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay
Inhibition of MRP1 (unknown origin) expressed in human 2008 cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay
|
[PMID: 23851114] |
| A2780 ADR | IC50 |
23.4 μM
Compound: 10
|
Inhibition of p-glycoprotein (unknown origin) expressed in human A2780Adr cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay
Inhibition of p-glycoprotein (unknown origin) expressed in human A2780Adr cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay
|
[PMID: 23851114] |
| KB | ED50 |
25 μg/mL
Compound: NSC-115922
|
Cytotoxicity against human KB cells
Cytotoxicity against human KB cells
|
[PMID: 469554] |
| L929 | IC50 |
>100 μM
Compound: 10
|
Cytotoxicity against mouse L929 cells after 5 days by MTS assay
Cytotoxicity against mouse L929 cells after 5 days by MTS assay
|
[PMID: 22743241] |
| MDA-MB-231 | IC50 |
2.042 μM
Compound: 30
|
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
|
[PMID: 34971873] |
| MDCK-II | IC50 |
0.822 μM
Compound: 10
|
Inhibition of human BCRP expressed in MDCK2 cells assessed as accumulation of Hoechst 33342 preincubated for 30 mins before Hoechst 33342 addition measured after 120 mins by fluorescence assay
Inhibition of human BCRP expressed in MDCK2 cells assessed as accumulation of Hoechst 33342 preincubated for 30 mins before Hoechst 33342 addition measured after 120 mins by fluorescence assay
|
[PMID: 23851114] |
| MDCK-II | IC50 |
1.88 μM
Compound: 10
|
Inhibition of human BCRP expressed in MDCK2 cells assessed as accumulation of pheophorbide-A preincubated for 30 mins before pheophorbide-A addition measured after 120 mins by flow cytometry
Inhibition of human BCRP expressed in MDCK2 cells assessed as accumulation of pheophorbide-A preincubated for 30 mins before pheophorbide-A addition measured after 120 mins by flow cytometry
|
[PMID: 23851114] |
3,5,7,3’,4’-Pentamethoxyflavone (25-100 μg/mL) can protect pUC19 plasmid DNA from oxidative damage[1]. 3,5,7,3’,4’-Pentamethoxyflavone (25-100 μg/mL) can reduce oxidative DNA damage in peripheral blood mononuclear cells of mice[1]. 3,5,7,3’,4’-Pentamethoxyflavone induces relaxation of the human corpus cavernosum through mechanisms related to voltage dependent Ca2+channels and calcium mobilization[2]. 3,5,7,3’,4’-Pentamethoxyflavone (100 μM, 48 h) can increase the expression of tight junction (TJ) protein in human intestinal Caco-2 cells and exert an in vitro intestinal barrier promoting effect[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Human intestinal Caco-2 cells
-
Concentration:100 μM
-
Incubation Time:48 h
-
Result:Increased the cytoskeletal association of TJ proteins, such as ZO1, ZO2, occludin,claudin-1, claudin-3, and claudin-4, in the cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Middle-aged (12–14 month old) Wistar male rats[4].
-
Dosage:22 mg/kg
-
Administration:Oral gavage (p.o.); twice daily; 6 weeks
-
Result:Caused a decrease in plasma glucose and an increase in plasma HDL cholesterol levels of the rats.
Chemical Information
-
CAS No. 1247-97-8
-
Appearance Solid
-
Molecular Weight 372.37
-
Formula C20H20O7
-
Color White to light brown
-
SMILES
O=C1C(OC)=C(C2=CC=C(OC)C(OC)=C2)OC3=CC(OC)=CC(OC)=C13
-
Structure Classification
-
Initial Source
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 25 mg/mL (67.14 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
-
Data Sheet (277 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
References
[1]. Jakhar R, et al. 3,5,7,3',4'-pentamethoxyflavone, a quercetin derivative protects DNA from oxidative challenges: potential mechanism of action. J Photochem Photobiol B. 2014 Feb 5;131:96-103. [Content Brief]
[2]. Jansakul C, et al. Relaxant mechanisms of 3, 5, 7, 3', 4'-pentamethoxyflavone on isolated human cavernosum. Eur J Pharmacol. 2012 Sep 15;691(1-3):235-44. [Content Brief]
[3]. Mayangsari Y, et al. 3,5,7,3',4'-Pentamethoxyflavone Enhances the Barrier Function through Transcriptional Regulation of the Tight Junction in Human Intestinal Caco-2 Cells. J Agric Food Chem. 2021 Sep 8;69(35):10174-10183. [Content Brief]
[4]. Yorsin S, et al. Increased vascular eNOS and cystathionine-γ-lyase protein after 6 weeks oral administration of 3, 5, 7, 3', 4'-pentamethoxyflavone to middle-aged male rats. Naunyn Schmiedebergs Arch Pharmacol. 2016 Nov;389(11):1183-1194. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6855 mL | 13.4275 mL | 26.8550 mL | 67.1375 mL |
| 5 mM | 0.5371 mL | 2.6855 mL | 5.3710 mL | 13.4275 mL | |
| 10 mM | 0.2686 mL | 1.3428 mL | 2.6855 mL | 6.7138 mL | |
| 15 mM | 0.1790 mL | 0.8952 mL | 1.7903 mL | 4.4758 mL | |
| 20 mM | 0.1343 mL | 0.6714 mL | 1.3428 mL | 3.3569 mL | |
| 25 mM | 0.1074 mL | 0.5371 mL | 1.0742 mL | 2.6855 mL | |
| 30 mM | 0.0895 mL | 0.4476 mL | 0.8952 mL | 2.2379 mL | |
| 40 mM | 0.0671 mL | 0.3357 mL | 0.6714 mL | 1.6784 mL | |
| 50 mM | 0.0537 mL | 0.2686 mL | 0.5371 mL | 1.3428 mL | |
| 60 mM | 0.0448 mL | 0.2238 mL | 0.4476 mL | 1.1190 mL |
Powered by Bioz