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CB1 inverse agonist 1

CAS No. 852315-00-5

CB1 inverse agonist 1( —— )

Catalog No. M32826 CAS No. 852315-00-5

CB1 inverse agonist 1 (MRL-650) is an orally active and selective CB1 agonist. The IC50s for CB1 and CB2 are 7.5 nM and 4100 nM, respectively.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    CB1 inverse agonist 1
  • Note
    Research use only, not for human use.
  • Brief Description
    CB1 inverse agonist 1 (MRL-650) is an orally active and selective CB1 agonist. The IC50s for CB1 and CB2 are 7.5 nM and 4100 nM, respectively.
  • Description
    MRL-650 (CB1 inverse agonist 1) is a highly potent, orally active, and specific inverse agonist of CB1 receptor with IC50s of 7.5 nM and 4100 nM for CB1 and CB2 receptors, respectively. Anorexigenic effects.
  • In Vitro
    ——
  • In Vivo
    MRL-650 (Compound 14; 0.3, 1, or 3 mg/kg）inhibits feeding in a dose-dependent manner. The pharmacokinetic profile of CB1 inverse agonist 1 is evaluated in Sprague-Dawley rats, C57BL/6 mice, beagles, and rhesus macaques with t1/2 of >8, >8, >24, and 22 h, respectively.Animal Model:Rat Dosage:0.3, 1, or 3 mg/kg Administration:PO Result:Inhibited feeding in a dose-dependent manner. 3 mg/kg decreased cumulative food intake from 2 h post-dosing. Decreased overnight body weight gain compared to vehicle treatment at all dosing levels.
  • Synonyms
    ——
  • Pathway
    GPCR/G Protein
  • Target
    Cannabinoid Receptor
  • Recptor
    Cannabinoid Receptor
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    852315-00-5
  • Formula Weight
    514.79
  • Molecular Formula
    C25H18Cl3N3O3
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    N(C(C)=O)C=1C=2C(=NC(=C(C2)C3=CC=C(Cl)C=C3)C4=C(Cl)C=C(Cl)C=C4)N(C)C(=O)C1C(C)=O
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1. Debenham JS, et al. Synthesis of functionalized 1,8-naphthyridinones and their evaluation as novel, orally active CB1 receptor inverse agonists.Bioorg Med Chem Lett. 2006 Feb;16(3):681-5.?
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