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MK-0249 B

CAS No. 862309-06-6

MK-0249 B( —— )

Catalog No. M33026 CAS No. 862309-06-6

MK-0249 is an orally active, selective and potent histamine H3 receptor antagonist (IC50: 1.7 nM) for the study of attention-deficit and hyperactivity disorders.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    MK-0249 B
  • Note
    Research use only, not for human use.
  • Brief Description
    MK-0249 is an orally active, selective and potent histamine H3 receptor antagonist (IC50: 1.7 nM) for the study of attention-deficit and hyperactivity disorders.
  • Description
    MK-0249 (Compound 1) is a potent, selective and orally active histamine H3 receptor antagonist, with anIC50 of 1.7 nM for human H3.
  • In Vitro
    MK-0249 (Compound 1) shows very good hepatic clearance values (CLh e 11 mL/min/kg), and is a substrate for rat P-gp but not for human P-gp.MK-0249 displays potent binding affinity to human, rat, and rhesus H3 receptors with Ki values of 6.8 ± 1.3 nM, 33 ± 3 nM, and 4.3 ± 1.2 nM, respectively. MK-0249 shows high intrinsic activity.
  • In Vivo
    ——
  • Synonyms
    ——
  • Pathway
    GPCR/G Protein
  • Target
    Histamine Receptor
  • Recptor
    Histamine Receptor
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    862309-06-6
  • Formula Weight
    431.45
  • Molecular Formula
    C23H24F3N3O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 50 mg/mL (115.89 mM; Ultrasonic )
  • SMILES
    Cc1nc2cccc(c2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1)C(F)(F)F
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1. Nagase T, et al. Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists. J Med Chem. 2008 Aug 14;51(15):4780-9.?
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