Otenzepad

CAS No. 102394-31-0

Otenzepad( AF-DX 116 )

Catalog No. M26778 CAS No. 102394-31-0

Otenzepad is a selective antagonist of M2 mAChR with IC50s of 386 nM and 640 nM for rat heart and rabbit peripheral lung.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    Otenzepad
  • Note
    Research use only, not for human use.
  • Brief Description
    Otenzepad is a selective antagonist of M2 mAChR with IC50s of 386 nM and 640 nM for rat heart and rabbit peripheral lung.
  • Description
    Otenzepad is a selective antagonist of M2 mAChR with IC50s of 386 nM and 640 nM for rat heart and rabbit peripheral lung.(In Vivo):In rats, Otenzepad (2 mg/kg; s.c.) significantly improved retention relative to vehicle controls. Otenzepad (0.5, 1 mg/kg; s.c.) significantly improved win-stay acquisition. In mice, Otenzepad (0.3, 1.0, or 3.0 mg/kg, i.p.) reverses the effects of insulin on memory and potentiates the effects of glucose.
  • In Vitro
    ——
  • In Vivo
    Otenzepad (0.5, 1 mg/kg, s.c., in rats) significantly improved win-stay acquisition relative to vehicle-injected controls.Otenzepad (2 mg/kg, s.c., in rats) significantly improved retention relative to vehicle controls.Otenzepad (0.3, 1.0, or 3.0 mg/kg, ip, in mice) potentiates the effects of glucose and reverses the effects of insulin on memory. Animal Model:Forty-eight male Long-Evans rats (325-350 g).Dosage:0.25, 0.5, 1.0 and 2.0 mg/kg.Administration:S.C. on the dorsum of the neck once.Result:Doses of 0.5 and 1.0 mg/kg significantly improved acquisition relative to vehicle controls, while doses of 0.25 and 2.0 mg/kg had no effect.Animal Model:Adult male Swiss mice (age 60–70 days; weight 25-30 g).Dosage:0.3, 1.0, or 3.0 mg/kg.Administration:IP once.Result:Enhanced retention in an inverted-U dose–response manner, with significant enhancement seen at 1.0 mg/kg (U15,15 = 49, p < 0.02, compared with saline-saline-injected control group).
  • Synonyms
    AF-DX 116
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    AChR
  • Recptor
    CYP1A1| CYP1A2| CYP2B1
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    102394-31-0
  • Formula Weight
    421.545
  • Molecular Formula
    C24H31N5O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 25 mg/mL (59.31 mM)
  • SMILES
    CCN(CC)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc12
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1.Naijue Zhu, et al. Ethynyl and Propynylpyrene Inhibitors of Cytochrome P450. J Chem Crystallogr. 2010 Apr 1;40(4):343-352.
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