MAO-B-IN-6
MAO-B-IN-6 is a potent, selective and orally active MAO-B inhibitor with an IC50 of 0.019 µM. MAO-B-IN-6 shows more efficacious than Safinamide in vitro and in vivo. MAO-B-IN-6 has the potential for the research of parkinson's disease (PD).
For research use only. We do not sell to patients.
- CAS No.: 2376198-66-0
- Formula: C19H20F2N2O2
- Molecular Weight:346.37
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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MAO-B 0.019 μM (IC50) |
MAO-A 46.365 μM (IC50) |
MAO-B-IN-6 (compound D5) (Sf9 cells) shows inhibitory activities towards monoamine oxidase (MAO) with the IC50s of 46.365 µM and 0.019 µM for MAO-A and MAO-B, respectively[1].
MAO-B-IN-6 shows no inhibition potential towards cytochrome P450 (IC50=>29 µM for 1A2, 2B6, 2C8, 2C9, 2C19, 2D6 and 3A4/5 enzymes)[1].
MAO-B-IN-6 (10 µM) shows high permeability through MDR1-MDCK II cell monolayers[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MAO-B-IN-6 (0.08, 0.4, 2 mg/kg; i.p.) diaplays stronger MAO-B inhibitory activity[1].
MAO-B-IN-6 (0.625, 1.25, 2.5 mg/kg; i.p.) increases the rearing activity in a dose-dependent manner[1].
MAO-B-IN-6 (0.625, 1.25, 2.5 mg/kg; i.p.) shows a potential efficacy for alleviating dopamine (DA) deficits in the MPTP-induced Parkinson's disease (PD) mouse model[1].
MAO-B-IN-6 (0.156, 0.312, 0.625, 1.25 mg/kg; i.p.) increases the effect of levodopa on dopamine concentration in the striatum[1].
MAO-B-IN-6 (0.156, 0.312, 0.625, 1.25 mg/kg; i.p.) shows a significant reduction in galantamine-induced tremulous jaw movements[1].
Pharmacokinetic Parameters of MAO-B-IN-6 in SD rats and cynomolgus monkeys[1].
| Compound | Route | Dose (mg/kg) | Cmax (ng/mL) | AUCt (ng·h/mL) | T1/2 (h) | Vss (h) | Cl (mL/min/kg) | F (%) |
| D5 (Rats) | iv | 1 | 690 | 505 | 0.67 | 1.37 | 32.9 | / |
| D5 (Rats) | po | 5 | 1000 | 1400 | 0.57 | / | / | 55.2 |
| D5 (Monkeys) | iv | 1 | 924 | 2120 | 1.77 | 1.06 | 7.54 | / |
| D5 (Monkeys) | po | 5 | 2280 | 11,300 | 2.80 | / | / | 107.1 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SD rats[1]
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Dosage:1, 5 mg/kg
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Administration:1 mg/kg, i.v.; 5 mg/kg, p.o.
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Result:Showed oral bioavailability in rats (F=55.2%).
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Animal Model:cynomolgus monkeys[1]
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Dosage:1, 5 mg/kg
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Administration:1 mg/kg, i.v.; 5 mg/kg, p.o.
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Result:Showed oral bioavailability in monkeys (F=107.1%).
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Animal Model:mice[1]
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Dosage:0.08, 0.4, 2 mg/kg
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Administration:i.p.
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Result:Displayed stronger MAO-B inhibitory activity.
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Animal Model:PD mouse mode[1]
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Dosage:0.625, 1.25, 2.5 mg/kg
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Administration:i.p.
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Result:Increased the rearing activity in a dose-dependent manner.
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Animal Model:C57BL/6 mice[1]
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Dosage:0.156, 0.312, 0.625, 1.25 mg/kg
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Administration:i.p.
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Result:Increased the effect of levodopa on dopamine concentration in the striatum.
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Animal Model:SD rats[1]
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Dosage:0.156, 0.312, 0.625, 1.25 (3.0 mg/kg galantamine, i.p.)
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Administration:i.p.
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Result:Showed a significant reduction in galantamine-induced tremulous jaw movements.
Chemical Information
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CAS No. 2376198-66-0
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Molecular Weight 346.37
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Formula C19H20F2N2O2
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SMILES
O=C([C@H]1N(CC2=CC=C(OCC3=CC=CC(F)=C3)C=C2)C[C@@H](F)C1)N
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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