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Immunology / Inflammation NOD Imperatorin

Imperatorin

Catalog No. T2845   CAS 482-44-0
Synonyms: Ammidin, Marmelosin, Pentosalen, 8-Isoamylenoxypsoralen, 8-Isopentenyloxypsoralene
Purity 98.07% Datasheet MSDS

Imperatorin is a modulator of p38,ERK pathway. Imperatorin increases BMP-2 expression (mRNA) and increases bone density/volume and mineralization in vivo.

Imperatorin, CAS 482-44-0
Pack Size Availability Price/USD Quantity
5 mg In stock 50.00
10 mg In stock 68.00
25 mg In stock 163.00
50 mg In stock 213.00
100 mg In stock 332.00
1 mL * 10 mM (in DMSO) In stock 53.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Imperatorin is a modulator of p38,ERK pathway. Imperatorin increases BMP-2 expression (mRNA) and increases bone density/volume and mineralization in vivo.
Targets&IC50 BChE :ic50 31.4μmol,   NO synthesis :ic50 9.2μmol,   TRPV1 :ic50 EC50:12.6±3.2μM,  
Animal Research
Animal Model: Swiss mice

Description

Imperatorin is a modulator of p38,ERK pathway. Imperatorin increases BMP-2 expression (mRNA) and increases bone density/volume and mineralization in vivo.

Targets&IC50

BChE :ic50 31.4μmol

NO synthesis :ic50 9.2μmol

TRPV1 :ic50 EC50:12.6±3.2μM

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].

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].

Animal Research

Animal Model: Swiss mice

Synonyms Ammidin, Marmelosin, Pentosalen, 8-Isoamylenoxypsoralen, 8-Isopentenyloxypsoralene
Purity 98.00%
Appearance solid
Molecular Weight 270.29
Formula C16H14O4
CAS No. 482-44-0

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 10 mM

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Kozio?, E., & Skalicka-Wo?niak, K. (2016). Imperatorin–pharmacological meaning and analytical clues: profound investigation.?Phytochemistry Reviews,?15(4), 627-649. doi: 10.1007/s11101-016-9456-2 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. 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.

Related Compound Libraries

This product is contained In the following compound libraries:
Approved Drug Library Bioactive Compound Library Natural Compound Library for HTS Anti-cancer Compound Library Neuronal Signaling Compound Library Ion Channel Inhibitor Library Immunology/Inflammation Compound Library Selected Plant-sourced Compound Library NF-κB Signaling Compound Library

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