NBI-34041  (Synonyms: SB-723620)

NBI-34041 (SB-723620) is a selective and orally active nonpeptide CRF1 receptor antagonist with an IC₅₀ of 58.9 nM and a K_i of 4.0 nM for human CRF1 receptor. NBI-34041 has no inhibitory effect on the CRF2 receptor. NBI-34041 can be used for depression and anxiety disorders research.

NBI-34041 could inhibit the production of cAMP in a concentration-dependent manner with an IC₅₀ of approximately 60 nM. At concentrations of NBI-34041 up to 10 000 nM, NBI-34041 is unable to fully inhibit sauvagine stimulated cAMP from cells expressing the human CRF2 receptor^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

NBI-34041 (3-30 mg/kg; oral gavage; a single dose) significantly attenuates the elevation in plasma ACTH induced by CRF. NBI-34041 also demonstrates efficacy in attenuating shock-induced ACTH release in a dose-dependent manner^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

417.37

C₂₂H₂₆Cl₂N₄

268545-87-5

CC1=NC2=C3C(N(C(CCC)CCC)CCN3N=C2C4=CC=C(Cl)C=C4Cl)=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Marcus Ising, et al. High-affinity CRF1 receptor antagonist NBI-34041: preclinical and clinical data suggest safety and efficacy in attenuating elevated stress response. Neuropsychopharmacology. 2007 Sep;32(9):1941-9.  [Content Brief]