PD 198306

CAS No. 212631-61-3

PD 198306( —— )

Catalog No. M27491 CAS No. 212631-61-3

PD 198306 is a selective inhibitor of MAPK/ERK-kinase (MEK) with antihyperalgesic effects. PD 198306 reduces the Streptozocin-induced increase in the level of active ERK1.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    PD 198306
  • Note
    Research use only, not for human use.
  • Brief Description
    PD 198306 is a selective inhibitor of MAPK/ERK-kinase (MEK) with antihyperalgesic effects. PD 198306 reduces the Streptozocin-induced increase in the level of active ERK1.
  • Description
    PD 198306 is a selective inhibitor of MAPK/ERK-kinase (MEK) with antihyperalgesic effects. PD 198306 reduces the Streptozocin-induced increase in the level of active ERK1.(In Vitro):PD 198306 (10 μM) reduces Tha-Crimson replication by 30% at 18 h and 50% at 36 h. PD 198306 (10 μM) significantly inhibits Tha-GFP replication by 25%.(In Vivo):In male Sprague Dawley rats bearing neuropathic pain, PD 198306 (1-30 μg/10 μL; i.t.) dose-dependently blocks static allodynia in both the chronic constriction injury and the streptozocin models.
  • In Vitro
    PD198306 significantly inhibits Tha-GFP replication by 25% at 10?μM, after 36?h.PD198306 (5?μM) reduces Tha-Crimson replication significantly by 20% at 18?h but such a result could not be confirmed at 36?h. Cell Cycle Analysis Cell Line:Human induced pluripotent stem cells (iPSC) Concentration:10? μM Incubation Time:6? hours Result:Inhibited Tha-Crimson replication at 10?μM, reducing it by 30% at 18?h and 50% at 36?h.
  • In Vivo
    Intrathecal administration of PD 198306 (1-30 μg per 10 μL) dose-dependently (1-30 μg) blocks static allodynia in both the streptozocin and the chronic constriction injury (CCI) models of neuropathic pain. Animal Model:Male Sprague Dawley rats (250-300 g) bearing neuropathic pain Dosage:1-30 μg per 10 μL and 3 mg per 100 μL (PD 198306 is suspended in cremophor:ethanol:water, 1 : 1 : 8.)Administration:Single doses of intrathecal (i.t.) or intraplantar (ipl) of PD 198306 (1-30 μg per 10 μL and 3 mg per 100 μL respectively Result:Intrathecal administration dose-dependently (1-30 μg) blocked static allodynia the streptozocin model of neuropathic pain. The minimum effective doses (MED) of 3 μg significantly blocked static allodynia 30 min after treatment. Both 10 μg and the highest dose used (30 μg) totally blocked the maintenance of static allodynia, for up to 1 h.
  • Synonyms
    ——
  • Pathway
    MAPK/ERK Signaling
  • Target
    MEK
  • Recptor
    Acidic mammalian chitinase (AMCase)|Bacterial|GH18 chitinase
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    212631-61-3
  • Formula Weight
    476.23
  • Molecular Formula
    C18H16F3IN2O2
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    O=C(NOCC1CC1)C2=CC(F)=C(F)C(F)=C2NC3=CC=C(I)C=C3C
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1.Schüttelkopf AW, et al. Bisdionin C-a rationally designed, submicromolar inhibitor of family 18 chitinases. ACS Med Chem Lett. 2011;2(6):428-432. Published 2011 Mar 23.
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