BMS-520
BMS-520 is a potent, orally active and selective sphingosine-1-phosphate 1 (S1P1) agonist with an EC50 of 0.47nM. BMS-520 shows ~3400-fold selectivity over S1P3. BMS-520 demonstrates impressive efficacy in a rat model of arthritis and in a mouse experimental autoimmune encephalomyelitis (EAE) model of multiple sclerosis. BMS-520 can be used for arthritis and EAE research.
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- No. CAS: 1236188-38-7
- Fòrmula: C23H17F3N4O4
- Peso molecular:470.40
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Actividad biológica
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S1PR1 0.47 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
0.27 nM
Compound: 6d; BMS-520
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Induction of internalization of C-terminal GFP-fused human S1P1 receptor expressed in CHO cell membranes after 50 mins
Induction of internalization of C-terminal GFP-fused human S1P1 receptor expressed in CHO cell membranes after 50 mins
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[PMID: 26924461] |
| CHO | EC50 |
0.47 nM
Compound: 3; BMS-520
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Agonist activity at human S1P1 receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgamma binding incubated for 45 mins by liquid scintillation counting method
Agonist activity at human S1P1 receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgamma binding incubated for 45 mins by liquid scintillation counting method
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[PMID: 27055941] |
| CHO | EC50 |
0.47 nM
Compound: 6d; BMS-520
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Agonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assay
Agonist activity at human S1P1 receptor expressed in CHO cell membranes after 45 mins by [35S]-GTPgammaS binding assay
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[PMID: 26924461] |
| HEK-293T | EC50 |
1600 nM
Compound: 3; BMS-520
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Agonist activity at human S1P3 receptor expressed in EDG3-Ga15-bla HEK293T cell membranes assessed as stimulation of [35S]GTPgamma binding incubated for 45 mins by liquid scintillation counting method
Agonist activity at human S1P3 receptor expressed in EDG3-Ga15-bla HEK293T cell membranes assessed as stimulation of [35S]GTPgamma binding incubated for 45 mins by liquid scintillation counting method
|
[PMID: 27055941] |
| HEK-293T | EC50 |
1600 nM
Compound: 6d; BMS-520
|
Agonist activity at human S1P3 receptor expressed in EDG3-Ga15-bla HEK293T cell membranes after 45 mins by [35S]-GTPgammaS binding assay
Agonist activity at human S1P3 receptor expressed in EDG3-Ga15-bla HEK293T cell membranes after 45 mins by [35S]-GTPgammaS binding assay
|
[PMID: 26924461] |
Chemical Information
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No. CAS 1236188-38-7
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Peso molecular 470.40
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Fòrmula C23H17F3N4O4
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SMILES
O=C(O)C1CN(C1)CC2=CC=C(C=C2)C3=NOC(C4=C(C(C5=CC=CC=C5)=NO4)C(F)(F)F)=N3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BMS-520 Related Classifications
HY-120615 Related Classifications
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