BMS-902483
BMS-902483 is a quinuclidine-containing spirooxazolidine that is a partial agonist of the α7 nicotinic acetylcholine receptor (nAChR). BMS-902483 improves cognitive ability in preclinical rodent models..
For research use only. We do not sell to patients.
- CAS No.: 1192810-88-0
- Formula: C18H20N4O
- Molecular Weight:308.38
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
α7 Nicotinic receptor (α7 nAChR)[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
>100 μM
Compound: 57; BMS 902483
|
Agonist activity at rat alpha1beta1deltaepsilon nAChR expressed in HEK293 cells for 2 mins by FLIPR assay
Agonist activity at rat alpha1beta1deltaepsilon nAChR expressed in HEK293 cells for 2 mins by FLIPR assay
|
[PMID: 27958732] |
| HEK293 | EC50 |
>100 μM
Compound: 57; BMS 902483
|
Agonist activity at rat alpha3beta4 nAChR expressed in HEK293 cells for 2 mins by FLIPR assay
Agonist activity at rat alpha3beta4 nAChR expressed in HEK293 cells for 2 mins by FLIPR assay
|
[PMID: 27958732] |
| HEK293 | EC50 |
>100 μM
Compound: 57; BMS 902483
|
Agonist activity at rat alpha4beta2 nAChR expressed in HEK293 cells for 2 mins by FLIPR assay
Agonist activity at rat alpha4beta2 nAChR expressed in HEK293 cells for 2 mins by FLIPR assay
|
[PMID: 27958732] |
| HEK293 | EC50 |
140 nM
Compound: 1a; BMS-902483
|
Agonist activity at rat alpha7 nAChR expressed in HEK293 cells co-expressing human RIC3 assessed as area under current curve at holding potential of -90 mV by whole-cell voltage clamp electrophysiology method
Agonist activity at rat alpha7 nAChR expressed in HEK293 cells co-expressing human RIC3 assessed as area under current curve at holding potential of -90 mV by whole-cell voltage clamp electrophysiology method
|
[PMID: 28337332] |
| HEK293 | EC50 |
140 nM
Compound: 57; BMS 902483
|
Partial agonist activity at rat alpha7 nAChR expressed in HEK293 cells co-expressing human RIC3 at holding potential of -90 mV by whole-cell voltage clamp technique
Partial agonist activity at rat alpha7 nAChR expressed in HEK293 cells co-expressing human RIC3 at holding potential of -90 mV by whole-cell voltage clamp technique
|
[PMID: 27958732] |
| HEK293 | EC50 |
240 nM
Compound: 1a; BMS-902483
|
Agonist activity at human alpha7 nAChR expressed in HEK293 cells co-expressing human RIC3 assessed as area under current curve at holding potential of -90 mV by whole-cell voltage clamp electrophysiology method
Agonist activity at human alpha7 nAChR expressed in HEK293 cells co-expressing human RIC3 assessed as area under current curve at holding potential of -90 mV by whole-cell voltage clamp electrophysiology method
|
[PMID: 28337332] |
| HEK293 | EC50 |
9.3 nM
Compound: 57; BMS 902483
|
Agonist activity at rat alpha7 nAChR expressed in HEK293 cells co-expressing human RIC3 measured for 2 mins by FLIPR assay
Agonist activity at rat alpha7 nAChR expressed in HEK293 cells co-expressing human RIC3 measured for 2 mins by FLIPR assay
|
[PMID: 27958732] |
| HEK293 | IC50 |
480 nM
Compound: 3
|
Antagonist activity at 5-HT3A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of Ca2+ flux by Fluo-4-AM dye based FLIPR assay
Antagonist activity at 5-HT3A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of Ca2+ flux by Fluo-4-AM dye based FLIPR assay
|
[PMID: 28105289] |
| HEK293 | IC50 |
480 nM
Compound: 57; BMS 902483
|
Antagonist activity at human 5-HT3A expressed in HEK293 cells assessed as reduction in acetylcholine-induced activity preincubated for 30 mins followed by addition of acetylcholine measured for 2 mins by Fluo-4AM dye based FLIPR assay
Antagonist activity at human 5-HT3A expressed in HEK293 cells assessed as reduction in acetylcholine-induced activity preincubated for 30 mins followed by addition of acetylcholine measured for 2 mins by Fluo-4AM dye based FLIPR assay
|
[PMID: 27958732] |
| HEK293 | IC50 |
480 nM
Compound: 1a; BMS-902483
|
Antagonist activity at human 5-HT3A receptor expressed in HEK293 cells
Antagonist activity at human 5-HT3A receptor expressed in HEK293 cells
|
[PMID: 28337332] |
Chemical Information
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CAS No. 1192810-88-0
-
Molecular Weight 308.38
-
Formula C18H20N4O
-
SMILES
C12CCN(CC2)C[C@]13OC(NC4=CC5=C(C=CC=C5)C=N4)=NC3
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Shipping
Room temperature in continental US; may vary elsewhere.
-
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)