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Imperatorin

Catalog No. T2845   CAS 482-44-0
Synonyms: Pentosalen, 欧前胡素, Ammidin, 8-Isopentenyloxypsoralene, Marmelosin, 8-Isoamylenoxypsoralen

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

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Imperatorin, CAS 482-44-0
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Purity: 98%
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Biological Description
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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 TRPV1:12.6±3.2 μM(EC50), BChE:31.4 μm
In vitro Imperatorin is a plant secondary metabolite that belongs to the coumarins-specifically the furanocoumarins. Imperatorin enhances the GABA-induced chloride ion current (IGABA) via 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 enhanced 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. Furthermore, Imperatorin at 30 mg/kg and carbamazepine at 6.8 mg/kg exhibit an increase 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].
Synonyms Pentosalen, 欧前胡素, Ammidin, 8-Isopentenyloxypsoralene, Marmelosin, 8-Isoamylenoxypsoralen
Molecular Weight 270.284
Formula C16H14O4
CAS No. 482-44-0

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 10 mM

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

References and Literature

1. Kozioł, E., & Skalicka-Woźniak, 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:
Anti-Cancer Compound Library HIF-1 Signaling Pathway Compound Library Traditional Chinese Medicine Monomer Library Neurotransmitter Receptor Compound Library Inhibitor Library Natural Product Library for HTS Ion Channel Inhibitor Library Anti-Tumor Natural Product Library Immunology/Inflammation Compound Library Anti-Alzheimer's Disease Compound Library

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Keywords

Imperatorin 482-44-0 NF-Kb信号通路 离子通道 免疫与炎症 神经科学 AChE AChR NOD TRP/TRPV Channel Ammidin 8-Isopentenyloxypsoralene TRP Channel inhibit Marmelosin 8-Isoamylenoxypsoralen Cholinesterase (ChE) Inhibitor Transient receptor potential channels Pentosalen inhibitor