Sembragiline
Sembragiline (EVT 302) is a potent, selective and reversible monoamine oxidase B (MAO-B) inhibitor. Sembragiline reduces the metabolism of dopamine and other amine neurotransmitters by inhibiting the activity of the MAO-B enzyme, thereby potentially increasing the concentration of these neurotransmitters in the brain. Inhibition of the MAO-B enzyme also reduces the formation of toxic reactive oxygen species (ROS) that play a role in the pathological process of AD. Sembragiline has good oral activity and blood-brain barrier permeability. Sembragiline can be used in studies of AD, especially in patients with AD who show increased MAO-B activity.
For research use only. We do not sell to patients.
- CAS No.: 676479-06-4
- Formula: C19H19FN2O3
- Molecular Weight:342.36
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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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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BTI-TN-5B1-4 | IC50 |
3852 nM
Compound: EVT-302; RG1577
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Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate preincubated for 15 mins and measured after 45 mins by resorufin-based fluorescence assay
Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate preincubated for 15 mins and measured after 45 mins by resorufin-based fluorescence assay
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[PMID: 30522087] |
| BTI-TN-5B1-4 | IC50 |
5.9 nM
Compound: EVT-302; RG1577
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Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate preincubated for 15 mins and measured after 45 mins by resorufin-based fluorescence assay
Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate preincubated for 15 mins and measured after 45 mins by resorufin-based fluorescence assay
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[PMID: 30522087] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 676479-06-4
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Molecular Weight 342.36
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Formula C19H19FN2O3
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SMILES
CC(N[C@@H](C1)CN(C2=CC=C(OCC3=CC=CC(F)=C3)C=C2)C1=O)=O
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Synonyms
EVT 302; RG1577; RO4602522
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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)
Sembragiline Related Classifications
HY-16731 Related Classifications
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