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Ponesimod

Catalog No. T3258   CAS 854107-55-4
Synonyms: ACT-128800

Ponesimod (ACT-128800) is an orally available sphingosine-1-phosphate receptor 1 (S1PR1, S1P1) agonist with potential immunomodulating activity.

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Ponesimod Chemical Structure
Ponesimod, CAS 854107-55-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 38.00
2 mg In stock $ 54.00
5 mg In stock $ 85.00
10 mg In stock $ 133.00
25 mg In stock $ 246.00
50 mg In stock $ 425.00
100 mg In stock $ 628.00
500 mg In stock $ 1,350.00
1 mL * 10 mM (in DMSO) In stock $ 98.00
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Purity: 99.42%
Purity: 98.22%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Ponesimod (ACT-128800) is an orally available sphingosine-1-phosphate receptor 1 (S1PR1, S1P1) agonist with potential immunomodulating activity.
Targets&IC50 S1P1 receptor: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].
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].
Kinase Assay The enzymatic reactions are conducted in duplicate at room temperature for 1 hour in a 50 μL mixture containing PKMT assay buffer, substrate coated plate, 10 M SAM, a HMT enzyme (EZH2 (800 ng/reaction), MLL (300 ng/reaction), PRMT1 (0.5 ng/reaction), SUV39H1 (75 ng/reaction) and UNC0638 (0-1.25 μM). After enzymatic reactions, 100 μL of first antibody is added to each well and the plate is incubated at room temperature for an additional 1 h. 100 μL of secondary antibody is added to each well and the plate is incubated at room temperature for an additional 30 min. 100 μL of developer reagents are added to wells and luminescence is measured using a BioTek SynergyTM 2 microplate reader. Enzyme activity assays are performed in duplicates at each concentration. The luminescence data are analyzed using the computer software, Graphpad Prism[1].
Synonyms ACT-128800
Molecular Weight 460.97
Formula C23H25ClN2O4S
CAS No. 854107-55-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55 mg/mL (119.31 mM)

Ethanol: 92 mg/mL (199.58 mM)

TargetMolReferences and Literature

1. Piali L. et al. J Pharmacol Exp Ther. 2011, 337(2):547-556. 2. D'Ambrosio D, et al. Ther Adv Chronic Dis. 2016, 7(1):18-33. 3. Fauzyah Y, Ono C, Torii S, et al. Ponesimod suppresses hepatitis B virus infection by inhibiting endosome maturation[J]. Antiviral Research. 2020: 104999.

TargetMolCitations

1. Fauzyah Y, Ono C, Torii S, et al. Ponesimod suppresses hepatitis B virus infection by inhibiting endosome maturation. Antiviral Research. 2021 Feb;186:104999

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Clinical Compound Library Clinical Compound Library Inhibitor Library Bioactive Compounds Library Max Orally Active Compound Library CNS-Penetrant Compound Library Anti-Obesity Compound Library

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Keywords

Ponesimod 854107-55-4 GPCR/G Protein S1P Receptor LPL Receptor S1P1 Lysophospholipid Receptor inflammation Inhibitor inhibit ACT-128800 ACT128800 lymphocyte-mediated ACT 128800 inhibitor

 

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