3,5,7,3′,4′-Pentamethoxyflavone

Name: 3,5,7,3′,4′-Pentamethoxyflavone
Brand: MedChemExpress
SKU: HY-N7690
Rating: 4.5 (1 reviews)

Cat. No.: HY-N7690 Purity: 99.15%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

3,5,7,3′,4′-Pentamethoxyflavone Chemical Structure

CAS No. : 1247-97-8

Size	Price	Stock	Quantity
5 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 240	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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•Related Screening Libraries:

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View All Calcium Channel Isoform Specific Products:

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

Biological Activity
Purity & Documentation
References
Customer Review

Description

Cellular Effect

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]
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]

In Vitro

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.

Western Blot Analysis^[3].

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.

In Vivo

3,5,7,3’,4’-Pentamethoxyflavone (22 mg/kg; twice daily; 6 weeks; p.o.) can promote the expression of eNOS and CSE proteins in middle-aged male rats, and regulate vascular function by antagonizing the contraction of phenylephrine and enhancing the vasodilation of acetylcholine^[4].

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.

Molecular Weight

372.37

Formula

C₂₀H₂₀O₇

CAS No.

1247-97-8

Appearance

Solid

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

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6855 mL	13.4275 mL	26.8550 mL
5 mM	0.5371 mL	2.6855 mL	5.3710 mL
10 mM	0.2686 mL	1.3428 mL	2.6855 mL

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 99.15%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (251 KB) HNMR (259 KB) LCMS (94 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

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