| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
|
| ln Vitro |
Imperatorin is a secondary metabolite found in plants that is a member of the coumarin family, namely the furanocoumarins. Imperatorin acts through α1β2η2S receptors to increase GABA-induced chloride currents (IGABA). At 100 μmol and 300 μmol, respectively, imperatorin increased IGABA by 50.5±16.3% and 109.8±37.7%. In vitro, [3H]diazepam's binding to the benzodiazepine site of the GABAA receptor in rat brain is inhibited by both Phellopterin and Imperatorin, which are both present in resveratrol root. Imperatorin's IC50 is 12.3 μmol, while Phellopterin's is There is a 400 nmol IC50. By permanently attaching to the GABA-T active site, imperatorin strongly and irreversibly inhibits GABA-T at concentrations ranging from 3.5 to 14 mmol in a way that is dependent on time and concentration. Imperatorin functions as a dose-dependent reversible inhibitor of acetylcholinesterase (AChE). Utilizing spectrophotometry, the AChE and BChE inhibitory properties of imperatorin and crude extract from Angelica sinensis fruit were examined at doses of 12.5, 25, 50, and 100 μg/mL. The inhibitory impact of imperatorin on AChE is low (13.75-46.11%), while it is significant (37.46-83.98%) on BChE. The IC50 of 31.4 μmol for BChE indicated that imperatorin was selective for BChE but not AChE. The most effective BACE-1 inhibitors were discovered to be imperatorin and (+)-Byakangelicol, with IC50 values of 91.8 and 104.9 μmol, respectively. Strong NO synthesis inhibition is also exhibited by imperatorin (IC50=9.2 μmol) [1]. Imperatorin, whose EC50 is 12.6±3.2 μM, is a mild agonist of TRPV1, a channel that is implicated in sensing a range of unpleasant stimuli [2].
|
|---|---|
| ln Vivo |
Imperatorin had anxiolytic effects and enhanced memory at dosages of 10 and 20 mg/kg and 30 minutes post-injection. It also increased learning at two distinct stages: acquisition and consolidation. It has also been demonstrated that acute administration of imperatorin at doses of 10 and 20 mg/kg reduces the anxiogenic effects of nicotine (subcutaneous injection, 0.1 mg/kg). The anticonvulsant effectiveness of carbamazepine against maximal shock-induced seizures was dramatically increased by intraperitoneal injection of imperatorin at doses of 30 and 40 mg/kg. This resulted in a lowering of the ED50 from 10.8 to 6.8 mg/kg (34% reduction) and 6 mg/kg (42% reduction), respectively. Additionally, the total brain concentration of carbamazepine increased by 85% (from 1.260 μg/mL to 2.328 μg/mL) when imperatorin at 30 mg/kg and carbamazepine at 6.8 mg/kg were administered. This increase may have resulted from altered blood barrier permeability or from effects akin to those of multidrug resistance protein inhibitors [1]. A naturally occurring furanocoumarin called imperatorin inhibits the action of acetylcholinesterase and inactivates gamma-aminobutyric acid transaminase. Scopolamine-impaired memory consolidation and acquisition are improved when imperatorin, at doses of 5 and 10 mg/kg, is administered acutely prior to scopolamine injection (1 mg/kg). Additionally, the effects of scopolamine on memory acquisition were greatly reduced by the maximum dose of imperatorin (10 mg/kg), which was given twice a day for seven days. In contrast, doses of 5 and 10 mg/kg of furanocoumarins had the same effect. efficient when memory is improved. Measurement is consolidation [3].
|
| References |
[1]. Kozio? E, et al. Imperatorin-pharmacological meaning and analytical clues: profound investigation. Phytochem Rev. 2016;15:627-649.
[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 |
| Molecular Formula |
C16H14O4
|
|---|---|
| Molecular Weight |
270.284
|
| Exact Mass |
270.0892
|
| CAS # |
482-44-0
|
| SMILES |
O(C([H])([H])/C(/[H])=C(\C([H])([H])[H])/C([H])([H])[H])C1=C2C(C([H])=C([H])C(=O)O2)=C([H])C2C([H])=C([H])OC1=2
|
| Synonyms |
Ammidin MarmelosinImperatorin Pentosalen
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~184.99 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.25 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.25 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.3700 mL | 1.8499 mL | 3.6999 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
