CS-0777-P
CS-0777-P, the phosphorylated form of CS-0777, acts as a potent and selective modulator of the S1P receptor-1 (S1P1). It exhibits approximately 320-fold higher agonist activity for human S1P1 compared to S1P3, with an EC50 of 1.1 nM. In pharmacological studies, CS-0777-P demonstrated significant effects in vitro as an S1P1 and S1P3 agonist, leading to lowered peripheral blood lymphocyte counts and suppressive effects on experimental autoimmune encephalomyelitis (EAE) in rats. Pharmacokinetic studies in rats revealed rapid lymphocyte count reductions following oral administration, making CS-0777 a promising candidate currently undergoing clinical trials for the treatment of multiple sclerosis (MS).
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- CAS. Nr.: 840523-39-9
- Formel: C21H31N2O5P
- Molecular Weight:422.46
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | EC50 |
1.1 nM
Compound: 4, CS-0777-P
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Agonist activity at human S1P1 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
Agonist activity at human S1P1 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
|
[PMID: 24900318] |
| CHO-K1 | EC50 |
1.1 nM
Compound: 4, CS-0777-P
|
Agonist activity at human S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding
Agonist activity at human S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding
|
[PMID: 22405291] |
| CHO-K1 | EC50 |
1.8 nM
Compound: 4, CS-0777-P
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Agonist activity at rat S1P1 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
Agonist activity at rat S1P1 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
|
[PMID: 24900318] |
| CHO-K1 | EC50 |
1.8 nM
Compound: 4, CS-0777-P
|
Agonist activity at rat S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding
Agonist activity at rat S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding
|
[PMID: 22405291] |
| CHO-K1 | EC50 |
200 nM
Compound: 4, CS-0777-P
|
Agonist activity at rat S1P3R expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
Agonist activity at rat S1P3R expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
|
[PMID: 24900318] |
| CHO-K1 | EC50 |
200 nM
Compound: 4, CS-0777-P
|
Agonist activity at rat S1P3 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding
Agonist activity at rat S1P3 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding
|
[PMID: 22405291] |
| CHO-K1 | EC50 |
350 nM
Compound: 4, CS-0777-P
|
Agonist activity at human S1P3R expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
Agonist activity at human S1P3R expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
|
[PMID: 24900318] |
| CHO-K1 | EC50 |
350 nM
Compound: 4, CS-0777-P
|
Agonist activity at human S1P3 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding
Agonist activity at human S1P3 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding
|
[PMID: 22405291] |
Chemical Information
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CAS. Nr. 840523-39-9
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Molecular Weight 422.46
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Formel C21H31N2O5P
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SMILES
O=P(O)(O)OC[C@](C)(N)CCC1=CC=C(C(CCCC2=CC=C(C=C2)C)=O)N1C
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
CS-0777-P Related Classifications
HY-14977 Related Classifications
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