MF 268
MF 268 is an orally active, blood-brain barrier-permeable acetylcholinesterase (AChE) inhibitor with an IC50 of 9 nM in rats. MF 268 binds to both the catalytic site and the regulatory anionic site of acetylcholinesterase, and increases the extracellular levels of acetylcholine, norepinephrine, dopamine and serotonin in the rat cortex via a dose-dependent pathway. MF 268 exhibits anti-amnesic effects in rats. MF 268 can be used in research related to Alzheimer's disease.
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- CAS No.: 154619-51-9
- Formule: C28H46N4O3
- Masse moléculaire:486.70
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Activité biologique
Description
IC50 & Target
[1]|
AChE 9 nM (IC50) |
In Vitro
MF 268 (120 min) potently inhibits acetylcholinesterase from rat whole brain in vitro, with an IC50 of 9 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MF 268 (0.5-2.0 mg/kg; s.c.; single dose) dose-dependently increases extracellular acetylcholine levels in the cortex of healthy rats, while moderately inhibiting cholinesterase[1].
MF 268 (50 μM; intracortical perfusion via microdialysis probe; continuous administration; 6 hr) increased extracellular ACh levels in the cortical cells of healthy rats by 5900%, while also altering the levels of NE, DA and 5-HT[1].
MF 268 (2-12 mg/kg; p.o.; single administration) exerts a persistent and selective reversal effect on Scopolamine (HY-N0296)-induced amnesia in rats, and the inhibition rate of whole-brain cholinesterase remains at 55% at 360 min after administration at 5 mg/kg[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male; 225-320 g for microdialysis; 170-190 g for cholinesterase activity assays)[1]
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Dosage:0.5 mg/kg; 2.0 mg/kg; 5.0 mg/kg
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Administration:p.o.; single dose
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Result:Elevated cortical extracellular acetylcholine (ACh), peaking at 300 % (0.5 mg/kg), 460 % (2.0 mg/kg, 4 hr), 1200 % (5.0 mg/kg, 5.5 hr).
Attained maximal whole‑brain cholinesterase inhibition of 2.3 % (2.0 mg/kg, 9 hr) and 9.7 % (5.0 mg/kg, 12 hr).
Raised norepinephrine (NE) levels to 70 % (0.5 mg/kg), 100 % (2.0 mg/kg), 180 % (5.0 mg/kg).
Boosted dopamine (DA) levels to 70 % (0.5 mg/kg), 60 % (2.0 mg/kg), 100 % (5.0 mg/kg).
Maintained ACh and monoamine elevation ≥5 hr under 2.0 and 5.0 mg/kg doses.
Produced negligible serotonin (5‑HT) fluctuations across all doses.
Triggered mild cholinergic adverse events (chewing, tremor) exclusively at 5.0 mg/kg.
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Animal Model:Sprague-Dawley (male; 225-320 g for microdialysis; 170-190 g for cholinesterase activity assays)[1]
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Dosage:0.5 mg/kg; 2.0 mg/kg
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Administration:s.c.; single dose
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Result:Produced dose-dependent increases in extracellular cortical ACh with maximal increases of 360% (0.5 mg/kg at 5.5 hr) and 2500% (2.0 mg/kg at 5 hr), which remained elevated for at least 6 hr.
Achieved maximal whole-brain cholinesterase inhibition of 13% (0.5 mg/kg) and 41% (2.0 mg/kg).
Caused no consistent changes in NE levels with either dose.
Induced a transient increase in DA with the 0.5 mg/kg dose, while no DA change occurred with the 2.0 mg/kg dose.
Caused no major changes in 5-HT levels at either dose.
Induced slight cholinergic side effects (chewing, tremor) at both doses.
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Animal Model:Wistar albino (male, ~300 g, scopolamine-induced amnesia)[2]
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Dosage:2, 5 mg/kg (cholinesterase inhibition)
6, 8, 12 mg/kg (radial maze, locomotor activity) -
Administration:p.o.; single dose
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Result:Exhibited an inverted U‑shaped dose‑response for reversing Scopolamine‑induced amnesia at 120 min pre‑test.
Maximally mitigated Scopolamine‑raised maze errors and completion time at 6 mg/kg.
Preserved baseline locomotion at 6, 8 mg/kg; counteracted Scopolamine‑triggered hypermotility at 12 mg/kg.
Reduced amnesic animal proportion to 16 % and lowered maze errors vs Scopolamine‑treated rats at 360 min pre‑test.
Delivered 55 % whole‑brain cholinesterase inhibition at 360 min post‑dose (30 % remaining at 15 h, 5 mg/kg).
Reached 22 % peak cholinesterase inhibition at 30 min post‑dose (18 % remaining at 15 h, 2 mg/kg).
Chemical Information
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CAS No. 154619-51-9
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Masse moléculaire 486.70
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Formule C28H46N4O3
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SMILES
C[C@]12C=3C(N(C)[C@]1(N(C)CC2)[H])=CC=C(OC(NCCCCCCCCN4C[C@H](C)O[C@H](C)C4)=O)C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MF 268 Related Classifications
HY-105461 Related Classifications
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