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MedChemExpress - Model NBI 35965 methanesulfonate -603151-83-3
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].MCE products for research use only. We do not sell to patients.
NBI 35965 methanesulfonate
MCE China：NBI 35965 methanesulfonate
Brand：MedChemExpress (MCE)
Cat. No.HY-103378
CAS：603151-83-3
Storage：Please store the product under the recommended conditions in the Certificate of Analysis.
Shipping：Room temperature in continental US; may vary elsewhere.
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.
In Vitro：NBI 35965 methanesulfonate displays a high affinity for CRF1 while having no binding affinity to CRF2. NBI 35965 methanesulfonate also inhibits the stimulation of cAMP induced by Sauvagine in CRF1 transfected cells[2].
In Vivo：NBI 35965 methanesulfonate (20 mg/kg; oral gavage; once) reduces stress induced ACTH production in mice[1]. In rats, NBI 35965 methanesulfonate (Compound 12a; 10 mg/kg) has a volume of distribution 17.8 L/kg, a plasma clearance of 17 mL/min/kg, and a half-life of 12 h. The estimated oral bioavailability is 34% with a mean maximal plasma concentration at 1 h of 560 ng/mL. NBI 35965 methanesulfonate also penetrated the blood-brain barrier, resulting in a mean maximal brain concentration of 700 ng/g[1].
IC50 & Target：CRFR1 4 nM (Ki) CRFR1 8.5 (pKi)
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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. [Content Brief]
[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. [Content Brief]
Brand introduction:
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