Catalog Number: 3100
Chemical Name: (7S)-6-(Cyclopropylmethyl)-2-(2,4-dichlorophenyl)-7-ethyl-7,8-dihydro-4-methyl-6H-1,3,6,8a-tetraazaacenaphthylene hydrochloride
Biological Activity
Potent and selective corticotropin-releasing factor receptor 1 (CRF1) antagonist (Ki values are 4 and > 10000 nM at CRF1 and CRF2 respectively). Inhibits cAMP accumulation and adrenocorticotropic hormone (ACTH) production in vitro (pIC50 values are 7.1 and 6.9 respectively) and attenuates CRF and ACTH production in vivo. Orally active and brain penetrant with anxiolytic activity.
Technical Data
  • M.Wt:
    437.79
  • Formula:
    C21H22Cl2N4.HCl
  • Solubility:
    Soluble to 100 mM in water and to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Desiccate at RT
  • CAS No:
    1782228-59-4
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Mechanism of corticotropin-releasing factor type I receptor regulation by non-peptide antagonists.
    Hoare et al.
    Mol.Pharmacol., 2003;63:751
  2. Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists.
    Gross et al.
    J.Med.Chem., 2005;48:5780
  3. A novel water-soluble selective CRF1 receptor antagonist, NBI 35965, blunts stress-induced visceral hyperalgesia and colonic motor function in rats.
    Million et al.
    Brain Res., 2003;985:32

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