2. GPCR/G Protein
  3. LPL Receptor
  4. CS-0777-P

CS-0777-P 是 CS-0777 的磷酸化形式，是 S1P 受体-1 (S1P1) 的强效和选择性调节剂。CS-0777-P 对人 S1P1 比对 S1P3 的激动剂活性高大约 320 倍，EC50 为 1.1 nM。在药理研究中，CS-0777-P 作为 S1P1 和 S1P3 激动剂在体外表现出显著作用，导致外周血淋巴细胞计数降低并对大鼠实验性自身免疫性脑脊髓炎 (EAE) 产生抑制作用。大鼠药代动力学研究表明，口服给药后淋巴细胞计数迅速减少，这使得 CS-0777 有潜力用于多发性硬化症 (MS) 的研究。

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CS-0777-P Chemical Structure

CS-0777-P Chemical Structure

CAS No. : 840523-39-9

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CS-0777-P 相关抗体

Top Publications Citing Use of Products

查看 LPL Receptor 亚型特异性产品:

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LPAR1 LPAR2 LPAR3 LPAR5 S1PR1 S1PR2 S1PR3 S1PR4 S1PR5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)[1].

细胞效力
(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
1.8 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
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
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]
分子量

422.46

Formula

C21H31N2O5P
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

CS-0777-P 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CS-0777-P840523-39-9LPL ReceptorLysophospholipid ReceptorInhibitorinhibitorinhibit

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产品名称：
CS-0777-P
目录号：
HY-14977
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