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Cat. No.: HY-14977

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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 No.: 840523-39-9
Formule: C₂₁H₃₁N₂O₅P
Masse moléculaire:422.46

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (266 KB)

CS-0777-P Chemical Structure

CAS No.: 840523-39-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- Cellular Effect
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Voir tous les produits spécifiques à Isoform LPL Receptor :

Cellular Effect

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

CAS No. 840523-39-9
Masse moléculaire 422.46
Formule C₂₁H₃₁N₂O₅P
SMILES

O=P(O)(O)OC[C@](C)(N)CCC1=CC=C(C(CCCC2=CC=C(C=C2)C)=O)N1C
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (266 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Takahide Nishi *?, Shojiro Miyazaki ?, Toshiyasu Takemoto ?, Keisuke Suzuki ?, Yukiko Iio ?, Katsuyoshi Nakajima ?, Takashi Ohnuki ?, Yumi Kawase ?, Futoshi Nara ?, Shinichi Inaba §, Takashi Izumi §, Hiroshi Yuita , Keiko Oshima , Hiromi Doi , Ryotaku Inoue , Wataru Tomisato , Takashi Kagari , and Takaichi Shimozato * .Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist ACS Med. Chem. Lett., 2011, 2 (5), pp 368-372 DOI: 10.1021/ml100301k Publication Date (Web): March 2, 2011

Calculators

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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