Ponesimod

Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM) . Ponesimod can protect against lymphocyte-mediated tissue inflammation[1][2][3].

Product Specifications

CAS Number

[854107-55-4]

Product Name Alternative

ACT-128800

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

LPL Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/Ponesimod.html

Purity

99.78

Solubility

DMSO : ≥ 100 mg/mL

Smiles

O=C1N(C2=CC=CC=C2C)/C(S/C1=C\C3=CC=C(OC[C@H](O)CO)C(Cl)=C3)=N/CCC

Molecular Formula

C23H25ClN2O4S

Molecular Weight

460.97

Precautions

H302, H315, H319, H335

References & Citations

[1]Piali L, et al. The selective sphingosine 1-phosphate receptor 1 agonist ponesimod protects against lymphocyte-mediated tissue inflammation. J Pharmacol Exp Ther. 2011 May;337 (2) :547-56.|[2]Bolli MH, et al. 2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists. J Med Chem. 2010 May 27;53 (10) :4198-211.|[3]Brossard P, et al. Pharmacokinetics and pharmacodynamics of ponesimod, a selective S1P1 receptor modulator, in the first-in-human study. Br J Clin Pharmacol. 2013 Dec;76 (6) :888-96.