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Cat. No.: IPRT-0.2 (for 10mM×0.2ml)

Cat. No.: IPRT-25 (for 25mg)

Cat. No.: IPRT-100 (for 100mg)

Description

Imperatorin is an effective inhibitor of NO synthesis (IC50=9.2 μmol) and also acts as a BChE inhibitor (IC50=31.4 μmol). Additionally, Imperatorin functions as a weak agonist of TRPV1, with an EC50 of 12.6±3.2 μM.

Basic Information

• Aliases: Marmelide; Ammidin; Marmelosin
• Source: Angelica dahurica （Fisch. ex Hoffm.）Benth. et Hook. f. ex Franch. et Sav; Peucedanum praeruptorum Dunn
• Compound type: Phenylpropanoids > Coumarins
• Chemical Formula: C₁₆H₁₄O₄
• Molecular Weight: 270.28
• CAS Number:  482-44-0
• Purity: 98%, HPLC
• Solvent/Solubility: Water: < 0.1 mg/ml (insoluble); DMSO: 50 mg/ml (184.99 mM)
• Solution Preparation: Add 5mg to 1.85ml of DMSO, or alternatively, add 2.70mg to 1ml of DMSO, to prepare a 10mM solution.

Signaling Pathway

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In Vitro Study

Imperatorin is a secondary metabolite found in plants, specifically belonging to the furanocoumarins subgroup of coumarins. It enhances the GABA-induced chloride ion current (IGABA) through the α1β2γ2S receptors, potentiating IGABA by 50.5±16.3% at 100 μmol and by 109.8±37.7% at 300 μmol. Together with Phellopterin, found in the roots of A. dahurica, Imperatorin inhibits [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 significantly and irreversibly inhibits GABA-T in a concentration-dependent and time-dependent manner, with concentrations ranging from 3.5 to 14 mmol, by binding irreversibly to the active site of GABA-T. It acts as a reversible acetylcholinesterase (AChE) inhibitor in a dose-dependent manner. In testing the AChE and BChE inhibitory activities of Imperatorin and a crude extract from the fruits of Angelica archangelica L., Imperatorin displays low inhibition towards AChE (13.75-46.11%), while exhibiting remarkable inhibitory effects against BChE (37.46-83.98%). It shows selectivity towards BChE over AChE, with an IC50 for BChE of 31.4 μmol. Together with (+)-Byakangelicol, Imperatorin is identified as one of the most effective BACE-1 inhibitors, with IC50s of 91.8 and 104.9 μmol, respectively. Additionally, Imperatorin is effective as an inhibitor of NO synthesis, with an IC50 of 9.2 μmol, and acts as a weak agonist of TRPV1, exhibiting an EC50 of 12.6±3.2 μM.

In Vivo Study

At doses of 10 and 20 mg/kg, administered 30 minutes after injection, Imperatorin exhibits an anxiolytic effect and improves various stages of memory and learning processes, including acquisition and consolidation. Additionally, acute administration of Imperatorin at doses of 10 and 20 mg/kg reduces the anxiogenic effect of nicotine (0.1 mg/kg, subcutaneous). At doses of 30 and 40 mg/kg administered intraperitoneally, Imperatorin significantly enhances the anticonvulsant activity of carbamazepine against maximal electroshock-induced seizures, resulting in a decrease in the ED50 from 10.8 to 6.8 mg/kg (by 34%) and 6 mg/kg (by 42%), respectively. Furthermore, Imperatorin at 30 mg/kg in combination with carbamazepine at 6.8 mg/kg increases the total brain concentration of carbamazepine from 1.260 to 2.328 μg/ml (by 85%), possibly by modifying blood-brain barrier permeability or acting as an inhibitor of multi-drug resistance proteins. Imperatorin, a naturally occurring furanocoumarin, inactivates gamma-aminobutyric acid transaminase and inhibits acetylcholinesterase activity. Acute administration of Imperatorin at doses of 5 and 10 mg/kg prior to scopolamine injection (1 mg/kg) improves memory acquisition and consolidation impaired by scopolamine. Moreover, repeated administration (twice daily for 7 days) of the highest dose of Imperatorin (10 mg/kg) significantly attenuates the effects of scopolamine on memory acquisition, while doses of 5 and 10 mg/kg of this furanocoumarin are effective when measuring memory consolidation.

Clinical Trial

N/A

Storage

Store at -20°C for at least one year. The solid powder is stable at 4°C for at least one month. If dissolved in a non-DMSO solvent, it is recommended to aliquot and store at -80°C for up to six months.

Precautions

• This product may have a certain degree of toxicity to the human body. Please take appropriate precautions to avoid direct contact with the body or inhalation.
• This product is for scientific research use only by professionals and is not intended for clinical diagnosis or treatment, food, or pharmaceutical purposes. It should not be stored in ordinary residential areas.
• For your safety and health, please wear laboratory attire and disposable gloves while handling.

Only for research and not intended for treatment of humans or animals

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