NBI 35965 hydrochloride

Cat. No. 3100

NBI 35965 hydrochloride C21H22Cl2N4.HCl [1782228-59-4]

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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.

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

Gross et al (2005) Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists. J.Med.Chem. 48 5780. PMID: 16134945.

Hoare et al (2003) Mechanism of corticotropin-releasing factor type I receptor regulation by non-peptide antagonists. Mol.Pharmacol. 63 751. PMID: 12606786.

Million et al (2003) A novel water-soluble selective CRF1 receptor antagonist, NBI 35965, blunts stress-induced visceral hyperalgesia and colonic motor function in rats. Brain Res. 985 32. PMID: 12957366.

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Keywords: NBI 35965 hydrochloride, supplier, NBI35965, CRF1R, CRF, 1, receptor, antagonist, corticotropin-releasing, factor, 1, antagonists, Tocris Bioscience, CRF1 Receptor Antagonist products

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