Imperatorin
Based on 6 publication(s) in Google Scholar
Imperatorin is an effective of NO synthesis inhibitor (IC50=9.2 μmol), which also is a BChE inhibitor (IC50=31.4 μmol). Imperatorin is a weak agonist of TRPV1 with EC50 of 12.6±3.2 μM.
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- Pureté : 98.59%
- CAS No.: 482-44-0
- Formule: C16H14O4
- Masse moléculaire:270.28
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Imperatorin (Standard)Cholinesterase (ChE) Inhibitor
Publications Citing Use of MedChemExpress (MCE) Imperatorin
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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Cell Imaging/Staining
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Cell Imaging/Staining
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Cell Migration/Invasion Assay
Activité biologique
Description
IC50 & Target
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AChE |
BChE |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
>20 μg/mL
Compound: 13
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Cytotoxicity against human A549 cells by MTT assay
Cytotoxicity against human A549 cells by MTT assay
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[PMID: 29975532] |
| H9 | IC50 |
>100 mg/mL
Compound: 71
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Cytotoxicity against human H9 cells
Cytotoxicity against human H9 cells
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[PMID: 27484512] |
| HepG2 | IC50 |
>20 μg/mL
Compound: 13
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Cytotoxicity against human HepG2 cells by MTT assay
Cytotoxicity against human HepG2 cells by MTT assay
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[PMID: 29975532] |
| MDA-MB-231 | IC50 |
>20 μg/mL
Compound: 13
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Cytotoxicity against human MDA-MB-231 cells by MTT assay
Cytotoxicity against human MDA-MB-231 cells by MTT assay
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[PMID: 29975532] |
| Neutrophil | IC50 |
>10 μM
Compound: 13
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Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release preincubated for 5 mins followed by fMLP/CB stimulation and measured for 10 mins 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 preincubated for 5 mins followed by fMLP/CB stimulation and measured for 10 mins using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as substrate
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[PMID: 29975532] |
| Neutrophil | IC50 |
>10 μM
Compound: 15
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Antiinflammatory activity in human neutrophil assessed as inhibition of FMLP/CB-induced elastase release for 5 mins
Antiinflammatory activity in human neutrophil assessed as inhibition of FMLP/CB-induced elastase release for 5 mins
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[PMID: 24798144] |
| Neutrophil | IC50 |
0.2 μM
Compound: 13
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Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation preincubated for 5 mins followed by cytochalasin B/fMLP addition for 3 mins by superoxide dismutase inhibitable reduction of ferricytochro
Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation preincubated for 5 mins followed by cytochalasin B/fMLP addition for 3 mins by superoxide dismutase inhibitable reduction of ferricytochro
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[PMID: 29975532] |
| Neutrophil | IC50 |
1.7 μM
Compound: 31
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Anti-inflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation
Anti-inflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation
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[PMID: 28844340] |
| Neutrophil | IC50 |
3.5 μM
Compound: 15
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Antiinflammatory activity in human neutrophil assessed as inhibition of FMLP/CB-induced superoxide anion generation pretreated for 5 mins by spectrophotometry
Antiinflammatory activity in human neutrophil assessed as inhibition of FMLP/CB-induced superoxide anion generation pretreated for 5 mins by spectrophotometry
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[PMID: 24798144] |
| SH-SY5Y | EC50 |
>50 μM
Compound: 33
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Neuroprotective activity in human SH-SY5Y cells assessed as reduction in 1-methyl-4-phenylpyridinium ion-induced cell death after 48 hrs by MTT assay
Neuroprotective activity in human SH-SY5Y cells assessed as reduction in 1-methyl-4-phenylpyridinium ion-induced cell death after 48 hrs by MTT assay
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[PMID: 27420919] |
| SH-SY5Y | EC50 |
8.4 μM
Compound: 33
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Neuroprotective activity in human SH-SY5Y cells assessed as reduction in oxygen glucose deprivation-induced cell death incubated for 16 hrs under hypoxic condition followed by incubation for 24 hrs under normoxic condition by MTT assay
Neuroprotective activity in human SH-SY5Y cells assessed as reduction in oxygen glucose deprivation-induced cell death incubated for 16 hrs under hypoxic condition followed by incubation for 24 hrs under normoxic condition by MTT assay
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[PMID: 27420919] |
In Vitro
Imperatorin is a plant secondary metabolite belonging to the coumarins-specifically the furanocoumarins. Imperatorin enhances the GABA-induced chloride ion current (IGABA) through the α1β2γ2S receptors. Imperatorin potentiates IGABA at 100 μmol by 50.5±16.3 % and at 300 μmol by 109.8±37.7 %, respectively. Imperatorin, together with Phellopterin, found in the roots of A. dahurica, inhibit [3H]diazepam binding to the benzodiazepine site of the rat brain GABAA receptor in vitro with an IC50 of 12.3 μmol for Imperatorin and 400 nmol for Phellopterin. Imperatorin, in a concentration ranging from 3.5 to 14 mmol, significantly and irreversibly inhibits GABA-T in a time-dependent and concentration-dependent manner, by irreversibly binding with the active site of GABA-T.Imperatorin is a reversible acetylcholinesterase (AChE) inhibitor, and acts in dose-dependent manner. The AChE and BChE inhibitory activities of Imperatorin and a crude extract from the fruits of Angelica archangelica L. is tested by the spectrophotometric method at concentrations of 12.5, 25, 50, and 100 μg/mL. Imperatorin displays low inhibition towards AChE (13.75-46.11 %), whereas it has remarkable inhibitory effect against BChE (37.46-83.98 %). Imperatorin shows selectivity toward BChE rather than AChE, with an IC50 for BChE of 31.4 μmol. Imperatorin, together with (+)-Byakangelicol, are found to be the most effective BACE-1 inhibitors, with IC50s of 91.8 and 104.9 μmol, respectively. Imperatorin (IC50=9.2 μmol) is also effective as an inhibitor of NO synthesis[1]. Imperatorin is a weak agonist of TRPV1, a channel implicated in detecting several noxious stimuli, exhibiting EC50 of 12.6±3.2 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 482-44-0
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Appearance Solid
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Masse moléculaire 270.28
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Formule C16H14O4
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Color White to off-white
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SMILES
O=C1C=CC2=CC3=C(OC=C3)C(OC/C=C(C)/C)=C2O1
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Synonyms
Ammidin
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Structure Classification
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Initial Source
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Proc Natl Acad Sci U S A
Divergent amplifications of CYP9A cytochrome P450 genes provide two noctuid pests with differential protection against xenobiotics. [Abstract]2023 Sep 12;120(37):e2308685120. PMID: 37669374 -
Br J Pharmacol
Imperatorin ameliorates metabolic dysfunction-associated fatty liver disease through modulating Suv39h1/Fabps/Cept1 signalling pathway. [Abstract]2025 Nov 11. PMID: 41218845 -
Biochem Pharmacol
Imperatorin induces ferroptosis via mediating lipid peroxidation and SLC7A11/ACSL4/GPX4 signaling for inhibition and therapeutics of prostate cancer. [Abstract]2026 Mar:245:117683. PMID: 41506540
Imperatorin purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2026 Mar:245:117683. [Abstract]
Cell viability of normal prostate cells (WPMY-1 and RWPE-1) following treatment with increasing concentrations of imperatorin (0, 50, 100, 150, and 200 μM).
Imperatorin purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2026 Mar:245:117683. [Abstract]
Cell viability of PCa cell lines (DU145 and PC3) treated with increasing concentrations of Imperatorin (0, 50, 100, 150, and 200 μM), showing a significant dose-dependent reduction.
Imperatorin purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2026 Mar:245:117683. [Abstract]
EdU assay showed the proliferation of DU145 and PC3 cells treated with increasing concentrations of Imperatorin (0, 50, and 100 μM) for 24 h, scale bar = 100 μM.
Imperatorin purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2026 Mar:245:117683. [Abstract]
Representative images of colony formation assays in DU145 and PC3 cells treated with imperatorin (0, 50, and 100 μM) for 14 days, demonstrating reduced colony formation ability.
Imperatorin purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2026 Mar:245:117683. [Abstract]
Representative Transwell assay results of PCa cells treated with imperatorin at concentrations of 0, 50, and 100 μM, scale bar = 100 μM.
Imperatorin purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2026 Mar:245:117683. [Abstract]
Representative images of wound healing assays showed the migration of DU145 and PC3 cells treated with imperatorin at 0, 50, and 100 μM for 24 h, scale bar = 100 μM.
Imperatorin purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2026 Mar:245:117683. [Abstract]
The expression of SLC7A11, ACSL4, and GPX4 in DU145 and PC3 cells treated with imperatorin (0, 50, and 100 μM) for 24 h. GAPDH served as the loading control.
Imperatorin purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2026 Mar:245:117683. [Abstract]
Imperatorin (0, 50, and 100 μM) for 24 h. Fluorescence images of DU145 and PC3 cells stained with C11-BODIPY, scale bar = 50 μM.
Imperatorin purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2026 Mar:245:117683. [Abstract]
TEM images of DU145 and PC3 cells treated with vehicle (Blank) or imperatorin (100 μM, 24 h). Cells treated with imperatorin exhibited shrunken mitochondria, reduced or vanished cristae, and increased membrane density (red arrows), which were all hallmarks of ferroptosis development.
Imperatorin purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2026 Mar:245:117683. [Abstract]
Imperatorin (intraperitoneal administration, 25 mg/kg and 50 mg/kg, every other day for a total of 10 doses). DU145 cells were subcutaneously injected into the flank of BALB/c nude mice to establish a xenograft tumor model. Subcutaneous tumors were then weighed (n = 6).
Imperatorin purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2026 Mar:245:117683. [Abstract]
Imperatorin (intraperitoneal administration, 25 mg/kg and 50 mg/kg, every other day for a total of 10 doses). Body weight changes of tumor-bearing mice after treatment.
Imperatorin purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2026 Mar:245:117683. [Abstract]
Imperatorin (intraperitoneal administration, 25 mg/kg and 50 mg/kg, every other day for a total of 10 doses). H&E staining and IHC analysis of subcutaneous tumors, scale bar = 100 μM.
Imperatorin purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2026 Mar:245:117683. [Abstract]
Imperatorin (intraperitoneal administration, 25 mg/kg and 50 mg/kg, every other day for a total of 10 doses). H&E staining of key organs from mice in each treatment group. scale bar = 100 μM.
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Neuropharmacology
2025 Nov 1:278:110593. PMID: 40683349 -
Solvant et solubilité
In Vitro:
DMSO : 50 mg/mL (184.99 mM; Need ultrasonic; 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, 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.
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.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.25 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
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.
Protocole
Animal Administration[3]
Mice[3]
The experiments are carried out on naive male Swiss mice weighing 20-25 g. Drugs are administered intraperitoneally (i.p.) at the volume of 10 mL/kg. Fresh drug solutions are prepared on each day of experimentation. Control groups receive saline injections of the same volume and via the same route of administration. During the acute treatment, the animals are allocated to the following drug groups: saline, rivastigmine (0.5 mg/kg, i.p.), scopolamine (1 mg/kg, i.p.), Imperatorin (1, 5, 10 mg/kg, i.p.), or Imperatorin coadministered with scopolamine. To measure the memory acquisition processes, scopolamine is administered 20 min before the pretest, whereas Imperatorin and rivastigmine are administered 30 min before the pretest. To measure the memory consolidation processes, rivastigmine or scopolamine (1 mg/kg) is administered immediately after the pretest, whereas Imperatorin is administered 15 min after pretest or after scopolamine injection. On the second day, the mice are retested. In the second set of the experiments, animals are randomly allocated to receive 6 days of i.p. injections of Imperatorin (1, 5, and 10 mg/kg, i.p.) or saline, twice daily (8:00 a.m. and 8:00 p.m.). On the seventh day, these animals are subjected to saline, scopolamine (1 mg/kg, i.p.), Imperatorin (1, 5, and 10 mg/kg, i.p.), or Imperatorin coadministered with scopolamine. To measure the memory acquisition processes, scopolamine is administered 20 min before the pretest and Imperatorin 30 min before the pretest. To measure the memory consolidation processes, scopolamine (1 mg/kg) is administered immediately after the pretest, whereas Imperatorin is administered 15 min after the pretest or after scopolamine injection. On the eighth day, the mice are retested.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (285 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Kozio? E, et al. Imperatorin-pharmacological meaning and analytical clues: profound investigation. Phytochem Rev. 2016;15:627-649. [Content Brief]
[2]. Chen X, et al. Furanocoumarins are a novel class of modulators for the transient receptor potential vanilloid type 1 (TRPV1) channel. J Biol Chem. 2014 Apr 4;289(14):9600-10. [Content Brief]
[3]. Budzynska B, et al. Effects of imperatorin on scopolamine-induced cognitive impairment and oxidative stress in mice. Psychopharmacology (Berl). 2015 Mar;232(5):931-42. [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, 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 | 3.6999 mL | 18.4993 mL | 36.9987 mL | 92.4967 mL |
| 5 mM | 0.7400 mL | 3.6999 mL | 7.3997 mL | 18.4993 mL | |
| 10 mM | 0.3700 mL | 1.8499 mL | 3.6999 mL | 9.2497 mL | |
| 15 mM | 0.2467 mL | 1.2333 mL | 2.4666 mL | 6.1664 mL | |
| 20 mM | 0.1850 mL | 0.9250 mL | 1.8499 mL | 4.6248 mL | |
| 25 mM | 0.1480 mL | 0.7400 mL | 1.4799 mL | 3.6999 mL | |
| 30 mM | 0.1233 mL | 0.6166 mL | 1.2333 mL | 3.0832 mL | |
| 40 mM | 0.0925 mL | 0.4625 mL | 0.9250 mL | 2.3124 mL | |
| 50 mM | 0.0740 mL | 0.3700 mL | 0.7400 mL | 1.8499 mL | |
| 60 mM | 0.0617 mL | 0.3083 mL | 0.6166 mL | 1.5416 mL | |
| 80 mM | 0.0462 mL | 0.2312 mL | 0.4625 mL | 1.1562 mL | |
| 100 mM | 0.0370 mL | 0.1850 mL | 0.3700 mL | 0.9250 mL |
Imperatorin Related Classifications
HY-N0285 Related Classifications
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