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).
For research use only. We do not sell to patients.
- CAS No.: 840523-39-9
- Formula: C21H31N2O5P
- Molecular Weight:422.46
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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
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | EC50 |
1.1 nM
Compound: 4, CS-0777-P
|
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
|
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 No. 840523-39-9
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Molecular Weight 422.46
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Formula 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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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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