Ponesimod

SKU: orb1304376

Description

Ponesimod (ACT-128800) is a selective, orally active S1P1 receptor agonist that functions as an immunomodulator. It is used in research to investigate mechanisms of lymphocyte trafficking and has been studied in models of autoimmune diseases such as multiple sclerosis.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 854107-55-4
• MW: 460.97
• Purity: 99.96%
• Formula: C₂₃H₂₅ClN₂O₄S
• SMILES: CCC\N=C1/S\C(=C/c2ccc(OC[C@H](O)CO)c(Cl)c2)C(=O)N1c1ccccc1C
• Target: S1P Receptor,LPL Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.34 mM);DMSO:235 mg/mL (509.79 mM);Ethanol:92 mg/mL (199.58 mM)

Bioactivity

• Target IC50:
  S1P5 receptor:142 nM|S1P1 receptor:5.7 nM (EC50)|S1P1 receptor:6 nM|S1P4 receptor:1956 nM|S1P3 receptor:2068 nM
• 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. Ponesimod is eliminated within 1 week of discontinuation and its pharmacological effects are rapidly reversible .
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ACT 128800, ACT128800, ACT-128800, Inhibitor, lymphocyte-mediated, Lysophospholipid Receptor, inhibit, inflammation, LPL, LPL Receptor, LPLReceptor, S1PReceptor, S1P Receptor, S1P1, Ponesimod

Compound Identifiers

PubChem CID

11363176