hMAO-B-IN-2
hMAO-B-IN-2 (compound 6j) is an orally active, potent, selective and BBB penetrated and competitive reversible hMAO-B inhibitor, with an IC50 of 4 nM. hMAO-B-IN-2 shows low toxicity and good neuroprotective effects in SH-SY5Y cell. hMAO-B-IN-2 can be used for alzheimer’s disease research. hMAO-B-IN-2 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
For research use only. We do not sell to patients.
- CAS No.: 2454459-87-9
- Formula: C18H23NO3
- Molecular Weight:301.38
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Storage:
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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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 4 nM (IC50) |
hMAO-B-IN-2 (compound 6j) (0-100 μM, 15 min) exhibits potent inhibitory activity, with IC50 values of 4 nM (hMAO-B) and 6.04 nM (hMAO-A), respectively[1].
hMAO-B-IN-2 (30 min) is a reversible MAO-B inhibitor, the activity of MAO-B enzyme was restored to about 82% and 45% after compound 6j dilution to 0.1 × IC50 and 1 × 50, respectively[1].
hMAO-B-IN-2 (25 μM, 48 h) exhibits remarkable inhibitory activities against MAO-B, had good inhibition property of Aβ self-induce aggregation (40.78 ± 6.27%)[1].
hMAO-B-IN-2 (0-100 μM, 24 h) shows non-toxic at the concentrations of 25 μM[1].
hMAO-B-IN-2 (0-25 μM, 24 h) has neuroprotective capability against neurodegeneration disease, and increases cell survival rates in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SH-SY5Y neuroblastoma cell[1]
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Concentration:0, 6.25, 12.5, 25, 50, 100 μM
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Incubation Time:24 h
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Result:Showed non-toxic at the concentrations of 25 μM.
Pharmacokinetic Parameters of hMAO-B-IN-2 in male Sprague-Dawley rats[1].
| Parameters | IV (3 mg/kg) | PO (10 mg/kg) |
| T1/2 (h) | 1.02 ± 0.17 | 1.33 ± 0.16 |
| Tmax (h) | 0.3 | |
| Cmax (μg/L) | 639.29 ± 89.06 | 142.17 ± 72.21 |
| AUC0-inf (μg/L∗h) | 247.74 ± 11.48 | 268.49 ± 69.72 |
| CL (L/h/kg) | 3.33 ± 0.15 | |
| F (%) | 36.10% |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley rats (male, 220±20 g)[1]
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Dosage:3 mg/kg (IV), 10 mg/kg (PO)
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Administration:IV, PO (Pharmacokinetic Analysis)
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Result:Had acceptable pharmacokinetic properties, and showed a high maximal concentration, appropriate half-life, and good oral bioavailability.
Chemical Information
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CAS No. 2454459-87-9
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Molecular Weight 301.38
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Formula C18H23NO3
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SMILES
C#CCN(CCCCCOC1=CC2=C(C(CCO2)=O)C=C1)C
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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)
hMAO-B-IN-2 Related Classifications
HY-146691 Related Classifications
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