For research use only.

Catalog No.S8241 Synonyms: ACT-128800

3 publications

Ponesimod Chemical Structure

CAS No. 854107-55-4

Ponesimod (ACT-128800) is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator with EC50 of 5.7 nM.

Selleck's Ponesimod has been cited by 3 publications

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Biological Activity

Description Ponesimod (ACT-128800) is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator with EC50 of 5.7 nM.
S1P1 receptor [1]
(In recombinant Chinese hamster ovary cells)
5.7 nM(EC50)
In vitro

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].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO NX;tUolJTnWwY4Tpc44h[XO|YYm= MkjDRYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDy[YNwdWKrbnHueEBUOVBzIILlZ4VxfG:{IHX4dJJme3OnZDDpckBEUE9iY3XscJMh[nliR2TQ[4FudWGVIHLpcoRqdmdiYYPzZZktKEWFNUC9NE4xODl5zszN M1e1S|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNES2OlgyLz5{MES0OlY5OTxxYU6=
CHO MXvGeY5kfGmxbjDhd5NigQ>? NXrsVoNESWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBz\WOxbXLpcoFvfCCVMWCzJJJm[2WydH;yJIV5eHKnc4Pl[EBqdiCFSF:gZ4VtdHNiYomgS3RR\2GvbXHTJIJqdmSrbnegZZN{[XluIFXDOVA:OC5zMEpOwG0> NX3GSHZGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC0OFY3QDFpPkKwOFQ3PjhzPD;hQi=>
CHOK1 NGfmOWJHfW6ldHnvckBie3OjeR?= M4PhPFkxKG2rboO= M1uye2lvcGmkaYTpc44hd2ZiU{HQVlEhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iQ1jPT|Eh[2WubIOgZYZ1\XJiOUCgcYlveyCkeTDi[ZRiNWG{cnXzeIlv\yC{ZXP1bZRu\W62IHHzd4F6NCCLQ{WwQVAvODF{NUpOwG0> NIf3VoY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEG0N|QzPCd-M{CxOFM1OjR:L3G+

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In vivo 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:


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  • Animal Models: Male Wistar rats; Female BALB/c mice
  • Dosages: 5 to 10 ml/kg(Rats); 5 ml/kg(Mice)
  • Administration: Oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 92 mg/mL (199.57 mM)
Water Insoluble
Ethanol '92 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 460.97


CAS No. 854107-55-4
Storage powder
in solvent
Synonyms ACT-128800
Smiles CCCN=C1N(C(=O)C(=CC2=CC(=C(C=C2)OCC(CO)O)Cl)S1)C3=CC=CC=C3C

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02029482 Completed Drug: ACT-128800|Drug: Placebo Safety and Tolerability Actelion April 2010 Phase 1
NCT02223832 Completed Drug: ACT-128800 Healthy Actelion February 2009 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID