Home GPCR & G Protein S1P Receptor modulator Ponesimod For research use only.

Ponesimod

Synonyms: ACT-128800

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

Ponesimod Chemical Structure

Ponesimod Chemical Structure

CAS: 854107-55-4

Selleck's Ponesimod has been cited by 6 publications

Purity & Quality Control

Batch: S824101 DMSO] 92 mg/mL] false] Ethanol] 92 mg/mL] false] Water] Insoluble] false Purity: 99.92%
99.92

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO Function assay Agonist activity at human recombinant S1P1 receptor expressed in CHO cells by GTPgammaS binding assay, EC50=0.0097μM 20446681
CHO Function assay Agonist activity at human recombinant S1P3 receptor expressed in CHO cells by GTPgammaS binding assay, EC50=0.109μM 20446681
CHOK1 Function assay 90 mins Inhibition of S1PR1 (unknown origin) expressed in CHOK1 cells after 90 mins by beta-arresting recuitment assay, IC50=0.01259μM 30143424
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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.
Targets
S1P1 receptor [1]
(In recombinant Chinese hamster ovary cells)
5.7 nM(EC50)
In vitro
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].
Kinase Assay GTPγS Binding Assay
GTPγS binding assays use membrane preparations of cells expressing recombinant S1P receptors of human, rat, or mouse origin. EC50 values were determined using IC50 Witch. Results were expressed as EC50 using the maximal response generated by S1P (percentage effect of maximal response) as an external maximum and solvent as minimum. Data are expressed as nanomoles of EC50 (geometric mean, geometric standard deviation).
In Vivo
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 Animal Models Male Wistar rats; Female BALB/c mice
Dosages 5 to 10 ml/kg(Rats); 5 ml/kg(Mice)
Administration Oral administration
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05552196 Completed Healthy Janssen Pharmaceutica N.V. Belgium October 18 2022 Phase 1
NCT02029482 Completed Safety and Tolerability Actelion April 2010 Phase 1
NCT02223832 Completed Healthy Actelion February 2009 Phase 1

Chemical lnformation & Solubility

Molecular Weight 460.97 Formula

C23H25ClN2O4S
CAS No. 854107-55-4 SDF Download Ponesimod SDF
Smiles CCCN=C1N(C(=O)C(=CC2=CC(=C(C=C2)OCC(CO)O)Cl)S1)C3=CC=CC=C3C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 92 mg/mL ( (199.57 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 92 mg/mL

Water : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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