2. Neuronal Signaling Membrane Transporter/Ion Channel
  3. Cholinesterase (ChE) TRP Channel
  4. Imperatorin

Imperatorin  (Synonyms: Ammidin)

Cat. No.: HY-N0285 Purity: 98.72%
COA Handling Instructions

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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.

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

Imperatorin Chemical Structure

Imperatorin Chemical Structure

CAS No. : 482-44-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 55 In-stock
Solution
10 mM * 1 mL in DMSO USD 55 In-stock
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100 mg USD 130 In-stock
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Based on 2 publication(s) in Google Scholar

Other Forms of Imperatorin:

Imperatorin Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

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Description

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.

IC50 & Target

AChE

 

BChE

 

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.

Imperatorin Related Antibodies
In Vivo

At doses of 10 and 20 mg/kg and 30 min after injection, Imperatorin shows an anxiolytic effect and improved different stages of memory and learning processes-both acquisition and consolidation. It is also shown that acute administration Imperatorin at doses of 10 and 20 mg/kg reduced the anxiogenic effect of nicotine (0.1 mg/kg, subcutaneous, s.c.). At 30 and 40 mg/kg, i.p. Imperatorin significantly potentiates the anticonvulsant activity of carbamazepine against maximal electroshock-induced seizures expressed by lowering the ED50 from 10.8 to 6.8 mg/kg (by 34 %) and 6 mg/kg (by 42 %), respectively. Moreover, Imperatorin at 30 mg/kg and carbamazepine at 6.8 mg/kg shows increases the total brain concentration of carbamazepine from 1.260 to 2.328 μg/mL (by 85%), which may be caused by modifying the blood-barrier permeability or acting like an inhibitor of multi-drug resistance proteins[1]. Imperatorin, a naturally occurring furanocoumarin, inactivates gamma-aminobutyric acid transaminase and inhibits acetylcholinesterase activity. Imperatorin administered acutely at the doses of 5 and 10 mg/kg prior to the injection of scopolamine (1 mg/kg) improves memory acquisition and consolidation impaired by scopolamine. Furthermore, repeatable (7 days, twice daily) administration of the highest dose of Imperatorin (10 mg/kg) significantly attenuates the effects of scopolamine on memory acquisition, whereas the doses of 5 and 10 mg/kg of this furanocoumarin are effective when memory consolidation is measured [3].

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

270.28

Formula

C16H14O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C=CC2=CC3=C(OC=C3)C(OC/C=C(C)/C)=C2O1
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 : 50 mg/mL (184.99 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 3.6999 mL 18.4993 mL 36.9987 mL
5 mM 0.7400 mL 3.6999 mL 7.3997 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.

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  • 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

×
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 (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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (9.25 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)

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: 98.72%

COA (255 KB) HNMR (251 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References
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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 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
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Imperatorin Related Classifications

Help & FAQs
  • 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.

Keywords:

Imperatorin482-44-0AmmidinCholinesterase (ChE)TRP ChannelTransient receptor potential channelsInhibitorinhibitorinhibit

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