H3R antagonist 5
H3R antagonist 5 (Compound 1b) is a selective histamine H3 receptor inverse agonist with a IC50 of 0.54 nM and the ability to cross the blood-brain barrier. H3R antagonist 5 can be used in central nervous system-related research.
For research use only. We do not sell to patients.
- CAS No.: 879368-27-1
- Formula: C23H32N2O4
- Molecular Weight:400.51
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Histamine Receptor Isoforms
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Biological Activity
Description
IC50 & Target
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H3 receptor 0.54 nM (IC50) |
H1 Receptor >10 μM (IC50) |
H2 Receptor >10 μM (IC50) |
H4 receptor >10 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>10000 nM
Compound: 1b
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Displacement of [35S]N-[(4R)-1'-[(2R)-6-cyano-1,2,3,4-tetrahydro-2-naphthalenyl]-3,4-dihydro-4-hydroxyspiro[2H-1-benzopyran-2,4'-piperidin]-6-yl]methanesulfonamide from human ERG in HEK293 cells
Displacement of [35S]N-[(4R)-1'-[(2R)-6-cyano-1,2,3,4-tetrahydro-2-naphthalenyl]-3,4-dihydro-4-hydroxyspiro[2H-1-benzopyran-2,4'-piperidin]-6-yl]methanesulfonamide from human ERG in HEK293 cells
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[PMID: 18768318] |
Chemical Information
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CAS No. 879368-27-1
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Molecular Weight 400.51
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Formula C23H32N2O4
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SMILES
COC1=CC=C2C(C(O[C@@]23CC[C@@H](C(N(CCN4CCCCC4)C)=O)CC3)=O)=C1
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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.
Protocols
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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)