NBI 35965 hydrochloride
NBI 35965 hydrochloride 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 hydrochloride does not inhibit CRF2. NBI 35965 hydrochloride reduces CRF or stress-induced adrenocorticotropic hormone (ACTH) production in vivo with pIC50 values of 7.1 and 6.9, respectively. NBI 35965 hydrochloride shows anxiolytic effects.
For research use only. We do not sell to patients.
- CAS No.: 1782228-59-4
- Formula: C21H23Cl3N4
- Molecular Weight:437.79
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
CRFR1 4 nM (Ki) |
CRFR1 8.5 (pKi) |
NBI 35965 hydrochloride displays a high affinity for CRF1 while having no binding affinity to CRF2. NBI 35965 hydrochloride also inhibits the stimulation of cAMP induced by Sauvagine in CRF1 transfected cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In rats, NBI 35965 hydrochloride (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 hydrochloride also penetrated the blood-brain barrier, resulting in a mean maximal brain concentration of 700 ng/g[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Male CD-1 mice (24-26 g) bearing restraint stress[1]
-
Dosage:20 mg/kg (10 mL/kg 5% mannitol-d (w/v) in water)
-
Administration:Oral gavage; 60 min prior to the initiation of the stressor
-
Result:Reduced stress induced ACTH production in vivo.
Chemical Information
-
CAS No. 1782228-59-4
-
Molecular Weight 437.79
-
Formula C21H23Cl3N4
-
SMILES
CC[C@H]1CN2N=C(C3=C(C=C(C=C3)Cl)Cl)C4=NC(C)=CC(N1CC5CC5)=C42.Cl
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NBI 35965 hydrochloride Related Classifications
HY-110056 Related Classifications
Powered by Bioz