PF-06700841 tosylate

PF-06700841 tosylate Chemische Eigenschaften,Einsatz,Produktion Methoden

• Chemische Eigenschaften

  The p-toluenesulfonic acid salt of brepocitinib exhibits good aqueous solubility (4.84 mg/mL at pH 7.64; >7 mg/mL in simulated gastric fluids). This compound also displayed high passive membrane permeability (mean PAPP = 18.8 × 10?6 cm/s as determined using Ralph Russ canine kidney cells (RRCK)).

• Charakteristisch

  Class: non-receptor tyrosine kinase
  Treatment: immunological disorders
  Other name: PF-06700841; Brepocitinib
  Elimination half-life = 3.8–7.5 h
  Protein binding = 39%
  

• Verwenden

  PF-06700841 tosylate salt has been used as an inhibitor of Janus kinase1 (JAK1) to study its therapeutic effect on the adjuvant induced arthritis (AIA) rat model. It has also been used as an inhibitor of interferon-α/β receptor alpha chain (IFNAR1) signaling adaptor tyrosine kinase (2TYK2) in mice.

• Biochem/physiol Actions

  PF-06700841 prevents IL-23 (interleukin 23) signaling through TYK2 (Tyrosine-protein kinase 2)/JAK1 (Janus kinase 1) inhibition.

• Pharmakokinetik

  The high oral bioavailability of brepocitinib obtained from rats (83%) is consistent with its high passive permeability and good solubility. The elimination half-life of brepocitinib ranged from 3.8 to 7.5 h after a single oral dose and from 4.9 to 10.7 h after multiple-dose administration. It was eliminated from the body by CYP450-mediated hepatic metabolism (84%) (mainly via CYP3A4) and renal clearance (16%). Oxidation of the N-methyl pyrazole (2) is the major metabolic pathway, followed by N-demethylation (3) and N-dealkylation with loss of pyrazole (4).
  

PF-06700841 tosylate Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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