1. Neuronal Signaling
  2. Monoamine Oxidase
  3. MAO-B-IN-6

MAO-B-IN-6 

Cat. No.: HY-115987
Handling Instructions

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.

MAO-B-IN-6 Chemical Structure

MAO-B-IN-6 Chemical Structure

CAS No. : 2376198-66-0

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products

View All Monoamine Oxidase Isoform Specific Products:

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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)[1].

IC50 & Target[1]

MAO-B

0.019 μM (IC50)

MAO-A

46.365 μM (IC50)

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

MAO-B-IN-6 (1 mg/kg, i.v.; 5 mg/kg, p.o.) shows oral bioavailability in rats (F=55.2%) and monkeys (F=107.1%)[1].
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
SD rats; 1 mg/kg, i.v.; 5 mg/kg, p.o.; Cynomolgus monkeys; 1 mg/kg, i.v.; 5 mg/kg, p.o.[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SD rats[1]
Dosage: 1, 5 mg/kg
Administration: 1 mg/kg, i.v.; 5 mg/kg, p.o.
Result: Showed oral bioavailability in rats (F=55.2%).
Animal Model: cynomolgus monkeys[1]
Dosage: 1, 5 mg/kg
Administration: 1 mg/kg, i.v.; 5 mg/kg, p.o.
Result: Showed oral bioavailability in monkeys (F=107.1%).
Animal Model: mice[1]
Dosage: 0.08, 0.4, 2 mg/kg
Administration: i.p.
Result: Displayed stronger MAO-B inhibitory activity.
Animal Model: PD mouse mode[1]
Dosage: 0.625, 1.25, 2.5 mg/kg
Administration: i.p.
Result: Increased the rearing activity in a dose-dependent manner.
Animal Model: C57BL/6 mice[1]
Dosage: 0.156, 0.312, 0.625, 1.25 mg/kg
Administration: i.p.
Result: Increased the effect of levodopa on dopamine concentration in the striatum.
Animal Model: SD rats[1]
Dosage: 0.156, 0.312, 0.625, 1.25 (3.0 mg/kg galantamine, i.p.)
Administration: i.p.
Result: Showed a significant reduction in galantamine-induced tremulous jaw movements.
Molecular Weight

346.37

Formula

C19H20F2N2O2

CAS No.
SMILES

O=C([[email protected]]1N(CC2=CC=C(OCC3=CC=CC(F)=C3)C=C2)C[[email protected]@H](F)C1)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
MAO-B-IN-6
Cat. No.:
HY-115987
Quantity:
MCE Japan Authorized Agent: