2. GPCR/G Protein
  3. CRFR
  4. NBI 35965 methanesulfonate

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.

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NBI 35965 methanesulfonate Chemical Structure

NBI 35965 methanesulfonate Chemical Structure

CAS No. : 603151-83-3

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Other Forms of NBI 35965 methanesulfonate:

NBI 35965 methanesulfonate Related Antibodies

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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[1][2].

IC50 & Target[1][2]

CRFR1

4 nM (Ki)

CRFR1

8.5 (pKi)

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].

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

NBI 35965 methanesulfonate Related Antibodies
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; 10mg/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.

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.
Molecular Weight

497.44

Formula

C22H26Cl2N4O3S
CAS No.
SMILES

CC1=CC2=C3N(N=C(C4=CC=C(Cl)C=C4Cl)C3=N1)C[C@H](CC)N2CC5CC5.OS(=O)(C)=O
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
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NBI 35965 methanesulfonate Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NBI 35965603151-83-3NBI35965NBI-35965CRFRCorticotropin-releasing Factor ReceptorCRHRCRF1 AntagonistACTHorally activebrain-penetrantanxiolytic effectsInhibitorinhibitorinhibit

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