Desfluoro-BMS-694153
Desfluoro-BMS-694153 (Compound 3) is a calcitonin gene-related peptide receptor (CGRP receptor) antagonist, with a Ki value of 0.01 nM. Desfluoro-BMS-694153 has a significantly reduced risk of CYP3A4 inhibition, and its IC50 values for CYP3A4-BFC and CYP3A4-BZR are 36 and 6 μM respectively. Desfluoro-BMS-694153 can be used for research on migraines.
For research use only. We do not sell to patients.
- CAS No.: 773886-89-8
- Formula: C35H46N8O3
- Molecular Weight:626.79
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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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CYP3A4 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SK-N-MC | EC50 |
0.017 nM
Compound: 3
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Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CCRP-induced cAMP production
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CCRP-induced cAMP production
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[PMID: 23402880] |
Chemical Information
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CAS No. 773886-89-8
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Molecular Weight 626.79
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Formula C35H46N8O3
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SMILES
O=C1N(C2CCN(CC2)C(N[C@@H](C(N3CCC(N4CCCCC4)CC3)=O)CC5=CC(C)=C(NN=C6)C6=C5)=O)CC7=CC=CC=C7N1
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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
[1]. Degnan AP, et al. Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptide receptor for migraine with rapid and efficient intranasal exposure. J Med Chem. 2008 Aug 28;51(16):4858-61. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Desfluoro-BMS-694153 Related Classifications
HY-180955 Related Classifications
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