NBI 35965 methanesulfonate
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 96.43%
- CAS No.: 603151-83-3
- Formula: C22H26Cl2N4O3S
- Molecular Weight:497.44
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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CRFR1 4 nM (Ki) |
CRFR1 8.5 (pKi) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
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. 603151-83-3
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Appearance Solid
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Molecular Weight 497.44
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Formula C22H26Cl2N4O3S
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Color White to off-white
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SMILES
CC1=CC2=C3N(N=C(C4=CC=C(Cl)C=C4Cl)C3=N1)C[C@H](CC)N2CC5CC5.OS(=O)(C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Purity & Documentation
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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 methanesulfonate Related Classifications
HY-103378 Related Classifications
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