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
-
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]
-
Biological Activity
-
Chemical Information
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
IC50 & Target
|
MAO-B 4 nM (IC50) |
In Vitro
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. Further protocols information, click here.
-
Cell Line:SH-SY5Y neuroblastoma cell[1]
-
Concentration:0, 6.25, 12.5, 25, 50, 100 μM
-
Incubation Time:24 h
-
Result:Showed non-toxic at the concentrations of 25 μM.
In Vivo
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.
-
Animal Model:Sprague-Dawley rats (male, 220±20 g)[1]
-
Dosage:3 mg/kg (IV), 10 mg/kg (PO)
-
Administration:IV, PO (Pharmacokinetic Analysis)
-
Result:Had acceptable pharmacokinetic properties, and showed a high maximal concentration, appropriate half-life, and good oral bioavailability.
Chemical Information
-
CAS No. 2454459-87-9
-
Molecular Weight 301.38
-
Formula C18H23NO3
-
SMILES
C#CCN(CCCCCOC1=CC2=C(C(CCO2)=O)C=C1)C
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
-
EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
The EdU incorporation assay measures DNA synthesis by adding the thymidine analog 5-ethynyl-2′-deoxyuridine to cells or tissues, where it is incorporated into newly synthesized DNA during S phase. Incorporated EdU is detected by copper-catalyzed azide-alkyne cycloaddition, in which a fluorescent azide covalently reacts with the ethynyl group on EdU, allowing S-phase cells to be detected by fluorescence microscopy, flow cytometry, or high-content imaging. EdU detection does not require DNA denaturation or anti-BrdU antibody access, which preserves sample structure and improves compatibility with immunostaining and multiparameter cytometry compared with BrdU-based detection. EdU can be cytotoxic in a cell-type- and exposure-dependent manner, so pulse duration, concentration, and continuous-labeling designs should be validated for each cell type.
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
hMAO-B-IN-2 Related Classifications
HY-146691 Related Classifications
Powered by Bioz