1. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Apoptosis Anti-infection Neuronal Signaling Membrane Transporter/Ion Channel
  2. Reactive Oxygen Species Apoptosis Bacterial Fungal RSV GABA Receptor
  3. Amentoflavone

Amentoflavone  (Synonyms: Didemethyl-ginkgetin)

Cat. No.: HY-N0662 Purity: 99.81%
SDS COA Handling Instructions

Amentoflavone (Didemethyl-ginkgetin) is a potent and orally active GABA(A) negative modulator. Amentoflavone also shows anti-inflammatory, antioxidative, anti-viral, anti-tumor, anti-radiation, anti-fungal, antibacterial activity. Amentoflavone induces apoptosis and cell cycle arrest at sub-G1 phase.

For research use only. We do not sell to patients.

Amentoflavone Chemical Structure

Amentoflavone Chemical Structure

CAS No. : 1617-53-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 71 In-stock
Solution
10 mM * 1 mL in DMSO USD 71 In-stock
Solid
5 mg USD 60 In-stock
10 mg USD 95 In-stock
25 mg USD 165 In-stock
50 mg USD 290 In-stock
100 mg USD 470 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of Amentoflavone:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Amentoflavone (Didemethyl-ginkgetin) is a potent and orally active GABA(A) negative modulator. Amentoflavone also shows anti-inflammatory, antioxidative, anti-viral, anti-tumor, anti-radiation, anti-fungal, antibacterial activity. Amentoflavone induces apoptosis and cell cycle arrest at sub-G1 phase[1][2][3][4].

Cellular Effect
Cell Line Type Value Description References
A549 IC50
8.36 μM
Compound: 10
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 29921475]
Calu-1 IC50
> 100 μM
Compound: 6
Cytotoxicity against human Calu1 cells after 3 days
Cytotoxicity against human Calu1 cells after 3 days
[PMID: 10843573]
Fibroblast IC50
1.8 μM
Compound: 4
Inhibition of UVB irradiation-induced MMP1 production in human dermal fibroblasts after 48 hrs
Inhibition of UVB irradiation-induced MMP1 production in human dermal fibroblasts after 48 hrs
[PMID: 18029185]
HCT-15 IC50
> 50 μM
Compound: 8
Cytotoxicity against human HCT15 cells assessed as cell viability after 24 hrs by MTT assay
Cytotoxicity against human HCT15 cells assessed as cell viability after 24 hrs by MTT assay
[PMID: 23206866]
HeLa IC50
> 100 μM
Compound: 6
Cytotoxicity against human HeLa cells after 3 days
Cytotoxicity against human HeLa cells after 3 days
[PMID: 10843573]
HeLa IC50
46.4 μM
Compound: amentoflavone
Cytotoxicity against human HeLa cells assessed as growth inhibition by sulforhodamine B assay
Cytotoxicity against human HeLa cells assessed as growth inhibition by sulforhodamine B assay
[PMID: 26722868]
HeLa IC50
5.3 μM
Compound: 7
Antiproliferative activity against human HeLa cells after 48 hrs by CCK8 assay
Antiproliferative activity against human HeLa cells after 48 hrs by CCK8 assay
[PMID: 29475587]
HepG2 IC50
> 50 μM
Compound: 8
Cytotoxicity against human HepG2 cells assessed as cell viability after 24 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as cell viability after 24 hrs by MTT assay
[PMID: 23206866]
HepG2 IC50
9.13 μM
Compound: 10
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 29921475]
HL-60 IC50
> 50 μM
Compound: 8
Cytotoxicity against human HL60 cells assessed as cell viability after 24 hrs by MTT assay
Cytotoxicity against human HL60 cells assessed as cell viability after 24 hrs by MTT assay
[PMID: 23206866]
HL-60 IC50
51.2 μM
Compound: 7
Antiproliferative activity against human HL60 cells after 48 hrs by CCK8 assay
Antiproliferative activity against human HL60 cells after 48 hrs by CCK8 assay
[PMID: 29475587]
Huh-7 CC50
> 50 μM
Compound: 12
Cytotoxicity against human Huh7.5.1 cells by MTT assay
Cytotoxicity against human Huh7.5.1 cells by MTT assay
[PMID: 22445328]
Jurkat IC50
> 50 μM
Compound: 8
Cytotoxicity against human Jurkat cells assessed as cell viability after 24 hrs by MTT assay
Cytotoxicity against human Jurkat cells assessed as cell viability after 24 hrs by MTT assay
[PMID: 23206866]
K562 IC50
> 100 μM
Compound: 6
Cytotoxicity against human K562 cells after 3 days
Cytotoxicity against human K562 cells after 3 days
[PMID: 10843573]
MCF7 IC50
75.4 μM
Compound: 4
Cytotoxicity against human MCF7 cells measured after 24 hrs by MTT assay
Cytotoxicity against human MCF7 cells measured after 24 hrs by MTT assay
[PMID: 34875389]
MGC-803 IC50
9.86 μM
Compound: 10
Cytotoxicity against human MGC803 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human MGC803 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 29921475]
Monocyte IC50
3 μM
Compound: amentoflavone
Inhibition of procoagulant activity in monocyte from human blood assessed as counteraction of IL1-induced tissue factor expression after 18 hrs
Inhibition of procoagulant activity in monocyte from human blood assessed as counteraction of IL1-induced tissue factor expression after 18 hrs
[PMID: 8882428]
Neutrophil IC50
0.75 μM
Compound: 7
Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release pretreated for 5 mins followed by fMLP/CB stimulation using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as substrate
Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release pretreated for 5 mins followed by fMLP/CB stimulation using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as substrate
[PMID: 29381070]
Neutrophil IC50
1.01 μM
Compound: 7
Anti-inflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation pretreated for 5 mins followed by cytochalasin B addition for 3 mins and subsequent fMLP stimulation for 10 mins by superoxide dismutase
Anti-inflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation pretreated for 5 mins followed by cytochalasin B addition for 3 mins and subsequent fMLP stimulation for 10 mins by superoxide dismutase
[PMID: 29381070]
PBMC IC50
35 μM
Compound: 1
Cytotoxicity against uninfected PHA-stimulated human PBMC assessed as thymidine incorporation after 24 hrs by trypan blue exclusion method
Cytotoxicity against uninfected PHA-stimulated human PBMC assessed as thymidine incorporation after 24 hrs by trypan blue exclusion method
[PMID: 9322359]
Raji IC50
> 100 μM
Compound: 6
Cytotoxicity against human Raji cells after 3 days
Cytotoxicity against human Raji cells after 3 days
[PMID: 10843573]
SW480 IC50
111 μM
Compound: 9
Cytotoxicity against human SW480 cells after 72 hrs by MTT assay
Cytotoxicity against human SW480 cells after 72 hrs by MTT assay
[PMID: 15787435]
T-24 IC50
10.67 μM
Compound: 10
Cytotoxicity against human T24 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human T24 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 29921475]
THP-1 IC50
> 50 μM
Compound: 8
Cytotoxicity against human THP1 cells assessed as cell viability after 24 hrs by MTT assay
Cytotoxicity against human THP1 cells assessed as cell viability after 24 hrs by MTT assay
[PMID: 23206866]
U-937 IC50
> 50 μM
Compound: 8
Cytotoxicity against human U937 cells assessed as cell viability after 24 hrs by MTT assay
Cytotoxicity against human U937 cells assessed as cell viability after 24 hrs by MTT assay
[PMID: 23206866]
Vero IC50
> 100 μM
Compound: 6
Cytotoxicity against african green monkey Vero cells after 3 days
Cytotoxicity against african green monkey Vero cells after 3 days
[PMID: 10843573]
WISH IC50
> 100 μM
Compound: 6
Cytotoxicity against human Wish cells after 3 days
Cytotoxicity against human Wish cells after 3 days
[PMID: 10843573]
In Vitro

Amentoflavone (1-60 μM) inhibits the production of nitric oxide in a concentration-dependent manner in RAW 264.7 cells[2].
? Amentoflavone (50-200 μM) inhibits the viability of U-87 MG cells with IC50 value of 100 μM at 48 h[3].
? Amentoflavone (0, 50, 100 μM; 48 h) induces apoptosis and cell cycle arrest at sub-G1 phase[3].
? Amentoflavone (0, 50, 100 μM; 48 h) inhibits NF-?B activation and decreases the expression of MCL1 and C-FLIP protein in U-87 MG cells[3].
? Amentoflavone (0-32 μg/ml) shows antibacterial activity with MICs of 8, 4, 32, 8, 16, 8 μg/ml for E. faecium ATCC 19434, S. aureus ATCC 25923, S. mutans ATCC 3065, E. coli O-157 ATCC 25922, E. coli ATCC 43895, P. aeruginosa ATCC 27853, respectively[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[3]

Cell Line: U-87 MG cells
Concentration: 0, 50, 75, 100, 200 µM
Incubation Time: 48 h
Result: Significantly inhibited the viability of U-87 MG cells by 23-71% with an IC50 value of 100 µM at 48 h.

Apoptosis Analysis[3]

Cell Line: U-87 MG cells
Concentration: 0, 50, 100 µM
Incubation Time: 48 h
Result: Significantly induced the accumulation of cells in the sub-G1 population and increased the level of active caspase-3 by 14-52% and 24-42%, respectively, and significantly triggered the loss of Ψm and the expression of active caspase-8 by 23-53% and 25-50%, respectively.

Western Blot Analysis[3]

Cell Line: U-87 MG cells
Concentration: 0, 50, 100 µM
Incubation Time: 48 h
Result: Significantly reduced NF-ĸB activation in a dose-dependent manner by 25-87% and reduced protein expression of MCL1 and C-FLIP by 50-80% and 38-57%, respectively.
In Vivo

Amentoflavone (25 mg/kg; p.o.; once a day for 3 consecutive days) shows neuroprotective role in epilepsy via anti-inflammatory effects in mouse[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 5-6 weeks, 28-32 g, kunming mice[1]
Dosage: 25 mg/kg
Administration: P.o.; once a day for 3 consecutive days
Result: Inhibited activation and nuclear translocation of NF-κB subunits p65, decreased IL-6 and IL-1β production and significantly decreased NO and prostaglandin E2 production.
Molecular Weight

538.46

Formula

C30H18O10

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C=C(C2=CC=C(O)C=C2)OC3=C(C4=CC(C5=CC(C6=C(O)C=C(O)C=C6O5)=O)=CC=C4O)C(O)=CC(O)=C13

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (232.14 mM; Need ultrasonic; 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 1.8571 mL 9.2857 mL 18.5715 mL
5 mM 0.3714 mL 1.8571 mL 3.7143 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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 (4.64 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% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (4.64 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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).
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: 99.81%

References

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8571 mL 9.2857 mL 18.5715 mL 46.4287 mL
5 mM 0.3714 mL 1.8571 mL 3.7143 mL 9.2857 mL
10 mM 0.1857 mL 0.9286 mL 1.8571 mL 4.6429 mL
15 mM 0.1238 mL 0.6190 mL 1.2381 mL 3.0952 mL
20 mM 0.0929 mL 0.4643 mL 0.9286 mL 2.3214 mL
25 mM 0.0743 mL 0.3714 mL 0.7429 mL 1.8571 mL
30 mM 0.0619 mL 0.3095 mL 0.6190 mL 1.5476 mL
40 mM 0.0464 mL 0.2321 mL 0.4643 mL 1.1607 mL
50 mM 0.0371 mL 0.1857 mL 0.3714 mL 0.9286 mL
60 mM 0.0310 mL 0.1548 mL 0.3095 mL 0.7738 mL
80 mM 0.0232 mL 0.1161 mL 0.2321 mL 0.5804 mL
100 mM 0.0186 mL 0.0929 mL 0.1857 mL 0.4643 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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