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GPCR&G protein

Ponesimod (854107-55-4)

Ponesimod is an orally available sphingosine-1-phosphate receptor 1 (S1PR1, S1P1) agonist that acts as a functional antagonist, with potential immunomodulating activity.

Not Intended for Therapeutic Use. For research use only.

CAS: 854107-55-4 Category

Ponesimod (854107-55-4) Description:

Ponesimod, also known as ACT-128800, is a potent, and orally active selective S1P(1) agonist. Ponesimod activated S1P(1)-mediated signal transduction with high potency (EC(50) of 5.7 nM) and selectivity. Ponesimod prevented edema formation, inflammatory cell accumulation, and cytokine release in the skin of mice with delayed-type hypersensitivity. Ponesimod also prevented the increase in paw volume and joint inflammation in rats with adjuvant-induced arthritis. Ponesimod may represent a new therapeutic approach in lymphocyte-mediated autoimmune diseases.

Ponesimod (854107-55-4) Specifications:

Product Name Ponesimod
Synonyms ACT-128800; ACT 128800; ACT128800; Ponesimod.
Chemical Names Ponesimod; 854107-55-4; ACT-128800; UNII-5G7AKV2MKP; 5G7AKV2MKP; CHEMBL1096146
Purity >98%
CAS Number  854107-55-4
Molecular Formula C23H25ClN2O4S
Molecular Weight 460.973 g/mol
Monoisotopic Mass 460.122 g/mol
InChIKey LPAUOXUZGSBGDU-STDDISTJSA-N
InChi Code InChI=1S/C23H25ClN2O4S/c1-3-10-25-23-26(19-7-5-4-6-15(19)2)22(29)21(31-23)12-16-8-9-20(18(24)11-16)30-14-17(28)13-27/h4-9,11-12,17,27-28H,3,10,13-14H2,1-2H3/b21-12-,25-23-/t17-/m1/s1
SMILES O=C1N(C2=CC=CC=C2C)/C(S/C1=C\C3=CC=C(OC[[email protected]](O)CO)C(Cl)=C3)=N/CCC
Form Powder
Color N/A
Solubility  may be formulated in DMSO
Storage Temp.  −20°C
Shelf life >2 years if stored properly.
Handling Dry, dark
Application  a potent, and orally active selective S1P(1) agonist

 


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RIDADR NONH for all modes of transport

References:

  • 1: Juif PE, Hoch M, D’Ambrosio D, Dingemanse J. Biocomparison of Three Formulations of the S1P1 Receptor Modulator Ponesimod in Healthy Subjects. Drugs R D. 2015 Jun;15(2):203-10. doi: 10.1007/s40268-015-0095-7. PubMed PMID: 25939333; PubMed Central PMCID: PMC4488184.
  • 2: Scherz MW, Brossard P, D’Ambrosio D, Ipek M, Dingemanse J. Three different up-titration regimens of ponesimod, an S1P1 receptor modulator, in healthy subjects. J Clin Pharmacol. 2015 Jun;55(6):688-97. doi: 10.1002/jcph.467. Epub 2015 Feb 10. PubMed PMID: 25612299.
  • 3: D’Ambrosio D, Steinmann J, Brossard P, Dingemanse J. Differential effects of ponesimod, a selective S1P1 receptor modulator, on blood-circulating human T cell subpopulations. Immunopharmacol Immunotoxicol. 2015 Feb;37(1):103-9. doi: 10.3109/08923973.2014.993084. PubMed PMID: 25519470.
  • 4: Reyes M, Hoch M, Brossard P, Dingemanse J. Effects of ethnicity and sex on the pharmacokinetics and pharmacodynamics of the selective sphingosine-1-phosphate receptor 1 modulator ponesimod: a clinical study in Japanese and Caucasian subjects. Pharmacology. 2014;94(5-6):223-9. doi: 10.1159/000368837. Epub 2014 Nov 14. PubMed PMID: 25402365.
  • 5: Hoch M, Darpo B, Brossard P, Zhou M, Stoltz R, Dingemanse J. Effect of ponesimod, a selective S1P1 receptor modulator, on the QT interval in healthy individuals. Basic Clin Pharmacol Toxicol. 2015 May;116(5):429-37. doi: 10.1111/bcpt.12336. Epub 2014 Nov 8. PubMed PMID: 25287214.
  • 6: Reyes M, Hoch M, Brossard P, Wagner-Redeker W, Miraval T, Dingemanse J. Mass balance, pharmacokinetics and metabolism of the selective S1P1 receptor modulator ponesimod in humans. Xenobiotica. 2015 Feb;45(2):139-49. doi: 10.3109/00498254.2014.955832. Epub 2014 Sep 4. PubMed PMID: 25188442.

1 review for Ponesimod (854107-55-4)

  1. Rated 5 out of 5

    Cofttek

    Never had such good experience before,The Ponesimod (854107-55-4) is high purity,also customer service is pretty nice !gotta try!!

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