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製品番号: 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 番号: 840523-39-9
分子式: C₂₁H₃₁N₂O₅P
分子量:422.46

保管条件:

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

Data Sheet (266 KB)

CS-0777-P 構造式

CAS 番号: 840523-39-9

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Use of MCE Products

Fluorescent Dye

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

生物活性

製品説明

LPL Receptor アイソフォーム固有の製品をすべて表示 :

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]

化学情報

CAS 番号 840523-39-9
分子量 422.46
分子式 C₂₁H₃₁N₂O₅P
SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (266 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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

モル濃度計算機

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

Mass Mass

濃度濃度

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分子量分子量

希釈計算機

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濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

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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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CS-0777-P

LPL Receptor アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

CS-0777-P 関連分類

HY-14977 関連分類