NBI 35965 (methanesulfonate)

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].

Product Specifications

CAS Number

[603151-83-3]

UNSPSC

12352005

Hazard Statement

H315-H319-H335

Target

CRFR

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/nbi-35965-methanesulfonate.html

Solubility

10 mM in DMSO

Smiles

CC1=CC2=C3N(N=C(C4=CC=C(Cl)C=C4Cl)C3=N1)C[C@H](CC)N2CC5CC5.OS(=O)(C)=O

Molecular Formula

C22H26Cl2N4O3S

Molecular Weight

497.44

Precautions

P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P362+P364-P403+P233-P405-P501

References & Citations

[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.