Product Description: NBI 35965 methanesulfonate is a selective, orally active and brain-penetrant corticotropin-releasing factor receptor 1 (CRF1) antagonist with a Ki value of 4 nM and a pKi value of 8.5. NBI 35965 methanesulfonate does not inhibit CRF2. NBI 35965 methanesulfonate reduces CRF or stress-induced adrenocorticotropic hormone (ACTH) production in vivo with pIC50 values of 7.1 and 6.9, respectively. NBI 35965 methanesulfonate shows anxiolytic effects[1][2].
Applications: Neuroscience-Neuromodulation
Formula: C22H26Cl2N4O3S
References: [1]Gross RS, et al. Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists. J Med Chem. 2005 Sep 8;48(18):5780-93./[2]Mulugeta Million, et al. A novel water-soluble selective CRF1 receptor antagonist, NBI 35965, blunts stress-induced visceral hyperalgesia and colonic motor function in rats. Brain Res. 2003 Sep 19;985(1):32-42.
CAS Number: 603151-83-3
Molecular Weight: 497.44
Research Area: Neurological Disease
Solubility: 10 mM in DMSO
Target: CRFR
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