Ponesimod

产品编号 T3258   CAS 854107-55-4
别名: ACT-128800

Ponesimod is an orally available sphingosine-1-phosphate receptor 1 (S1PR1, S1P1) agonist that acts as a functional antagonist, with potential immunomodulating activity.

Ponesimod结构式
Ponesimod , CAS 854107-55-4
规格 库存 价格/RMB 数量
1 mg 上海现货 367.00
2 mg 上海现货 660.00
5 mg 上海现货 960.00
10 mg 上海现货 1560.00
25 mg 上海现货 3631.00
50 mg 上海现货 6500.00
100 mg 上海现货 10767.00
1 mL * 10 mM (in DMSO) 上海现货 1056.00
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产品描述 Ponesimod is an orally available sphingosine-1-phosphate receptor 1 (S1PR1, S1P1) agonist that acts as a functional antagonist, with potential immunomodulating activity.
靶点活性 S1P1 : 5.7nM(EC50),  
体外活性 Relative to the potency of S1P, the potency of ponesimod at human recombinant receptors was 4.4-fold higher for S1P1 and 150-fold lower for human S1P3. Therefore, ponesimod was ∼650-fold more selective for human S1P1 over S1P3 than the natural ligand[1].
体内活性 Ponesimod is a new, potent, and selective S1P1 receptor agonist with pharmacokinetic properties allowing rapid restoration of lymphocyte count in peripheral blood upon discontinuation. Ponesimod prevents edema formation, inflammatory cell accumulation, and cytokine release in the skin of mice with delayed-type hypersensitivity. Ponesimod also prevents the increase in paw volume and joint inflammation in rats with adjuvant-induced arthritis. Selective activation of S1P1 using ponesimod leads to blood lymphocyte count reduction and prevention in models of lymphocyte-mediated tissue inflammation. It has the potential to be as effective in animal models of autoimmunity and human autoimmune disease via its effect on T and B cell blood count. Thus, ponesimod may represent a new therapeutic option for the treatment of autoimmune diseases[1]. Ponesimod is eliminated within 1 week of discontinuation and its pharmacological effects are rapidly reversible [2].
Animal Research
Animal Model: Wistar rats; FeBALB/c mice
别名 ACT-128800
纯度 98.01%
分子量 460.97
分子式 C23H25ClN2O4S
CAS No. 854107-55-4

存储

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

溶解度

DMSO: 10 mM

Ethanol: 92 mg/mL (199.58 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

文献引用

参考文献
1. Piali L. et al. J Pharmacol Exp Ther. 2011, 337(2):547-556. 2. D'Ambrosio D, et al. Ther Adv Chronic Dis. 2016, 7(1):18-33. 3. Fauzyah Y, Ono C, Torii S, et al. Ponesimod suppresses hepatitis B virus infection by inhibiting endosome maturation[J]. Antiviral Research. 2020: 104999.

Related Compound Libraries

This product is contained In the following compound libraries:
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