1. GPCR/G Protein
  2. LPL Receptor
  3. Ponesimod

Ponesimod (Synonyms: ACT-128800)

Cat. No.: HY-10569 Purity: 99.72%
Handling Instructions

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.

For research use only. We do not sell to patients.

Ponesimod Chemical Structure

Ponesimod Chemical Structure

CAS No. : 854107-55-4

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Description

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].

IC50 & Target[1]

S1PR1

6 nM (IC50)

S1PR5

142 nM (IC50)

S1PR4

1956 nM (IC50)

S1PR3

2068 nM (IC50)

In Vitro

Ponesimod activates human S1P1-5 receptors with EC50s of 5.7, >10000, 105, 1108 and 59.1 nM respectively in GTPγS binding assay[2].
Ponesimod activates S1P1 receptors with EC50s of 5.7, 1.9, and 1.4 nM for human, rat, and mouse S1P receptors respectively[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Ponesimod (30 and 175 mg/kg; once daily p.o. for 8 d) prevents delayed-type hypersensitivity in mice[2].
Ponesimod (30 mg/kg by gavage 3 h before and 6 h after adjuvant injection followed by 100 mg/kg/day by administration as food admix for 18 days) prevents adjuvant-induced arthritis in rats[2].
Ponesimod (0.3-100 mg/kg; a single oral gavage) causes a dose-dependent reduction in lymphocyte count, with a plateau effect being reached at 3 mg/kg in rats[2].
Ponesimod (100 mg/kg; once daily oral gavage for 7 d) results in a lymphocyte count reduction to 1900 lymphocytes/μL, and this effect is maintained over the entire 7 days studies. Lymphocyte count returned to baseline levels within 48 h after discontinuation of dosing[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c mice (15-25 g) sensitized with DNFB[2]
Dosage: 30 and 175 mg/kg
Administration: Gavage (30 mg/kg) 19 and 3 h before sensitization, followed by administration as food admix (175 mg/kg/day) for 8 days
Result: Caused a 60 to 90% reduction of delayed-type hypersensitivity (DTH) parameters of the skin, such as edema, protein extravasation, and neutrophil myeloperoxidase (MPO) activity.
Reduced skin levels of proinflammatory cytokines, such as IL-1β, IL-6, IFNγ, TNFα, and several chemokines to different degrees ranging from -27 to -100%.
Clinical Trial
Molecular Weight

460.97

Formula

C₂₃H₂₅ClN₂O₄S

CAS No.
SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (216.93 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1693 mL 10.8467 mL 21.6934 mL
5 mM 0.4339 mL 2.1693 mL 4.3387 mL
10 mM 0.2169 mL 1.0847 mL 2.1693 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.42 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.42 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.72%

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Keywords:

PonesimodACT-128800ACT128800ACT 128800LPL ReceptorLysophospholipid ReceptorS1P1lymphocyte-mediatedinflammationInhibitorinhibitorinhibit

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