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.
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- CAS No.: 1782228-59-4
- 화학식: C21H23Cl3N4
- 분자량:437.79
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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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.
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Animal Model:Male CD-1 mice (24-26 g) bearing restraint stress[1]
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Dosage:20 mg/kg (10 mL/kg 5% mannitol-d (w/v) in water)
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Administration:Oral gavage; 60 min prior to the initiation of the stressor
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Result:Reduced stress induced ACTH production in vivo.
Chemical Information
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CAS No. 1782228-59-4
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분자량 437.79
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화학식 C21H23Cl3N4
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SMILES
CC[C@H]1CN2N=C(C3=C(C=C(C=C3)Cl)Cl)C4=NC(C)=CC(N1CC5CC5)=C42.Cl
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
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
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