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PAT-505 B

CAS No. 1782070-22-7

PAT-505 B( —— )

Catalog No. M33056 CAS No. 1782070-22-7

PAT-505 is an orally available, selective and potent inhibitor of autologous epidermal growth factor (IC50 2 nM in Hep3B cells, 9.7 nM in human blood, 62 nM in mouse plasma).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    PAT-505 B
  • Note
    Research use only, not for human use.
  • Brief Description
    PAT-505 is an orally available, selective and potent inhibitor of autologous epidermal growth factor (IC50 2 nM in Hep3B cells, 9.7 nM in human blood, 62 nM in mouse plasma).
  • Description
    PAT-505 is a potent, selective, noncompetitive and orally available autotaxin inhibitor, with an IC50 of 2 nM in Hep3B cells, 9.7 nM in human blood and 62 nM in mouse plasma.
  • In Vitro
    PAT-505 is a potent, selective, noncompetitive and orally available autotaxin inhibitor, with an IC50 of 2 nM in Hep3B cells, 9.7 nM in human blood and 62 nM in mouse plasma. PAT-505 is selective for ATX versus other ENPP proteins, and shows marginal inhibition of radiolabeled agonist or antagonist binding to the adenosine A3 receptor, MT1 melatonin receptor, prostaglandin E2 EP4 receptor, 5-HT5a serotonin receptor, and GABA-gated Cl- channel with 50%-70% inhibition at 10 μM.
  • In Vivo
    PAT-505 suppresses ATX lysoPLD activity with an average IC50 value of 62 nM and an average IC90 value of 630 nM in mouse plasma, and the IC90 in rat plasma is ～770 nM. PAT-505 (30 mg/kg, p.o.) significantly reduces fibrotic score, the percentage of PSR-positive area, and α-SMA immunoreactivity in mouse model of nonalcoholic steatohepatitis (NASH).
  • Synonyms
    ——
  • Pathway
    Angiogenesis
  • Target
    EGFR
  • Recptor
    EGFR
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1782070-22-7
  • Formula Weight
    473.92
  • Molecular Formula
    C23H18ClF2N3O2S
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 48.33 mg/mL (101.98 mM; Ultrasonic )
  • SMILES
    CCn1cc(cn1)-n1c(C2CC2)c(Sc2cccc(C(O)=O)c2F)c2ccc(Cl)c(F)c12
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Bain G, et al. Selective Inhibition of Autotaxin Is Efficacious in Mouse Models of Liver Fibrosis. J Pharmacol Exp Ther. 2017 Jan;360(1):1-13. Epub 2016 Oct 17.?
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