A selective CRF1 antagonist (Ki = 4 nM); inhibits cAMP accumulation and ACTH production in vitro (pIC50s = 7.1 and 6.9

NBI 35965 (mesylate) – 25 mg

Brand:
Cayman
CAS:
603151-83-3
Storage:
-20
UN-No:
Non-Hazardous - /

Corticotropin-releasing hormone, also known as corticotropin-releasing factor (CRF) or corticoliberin, is a peptide hormone and neurotransmitter involved in the stress response. It is secreted from the hypothalamus and is the major regulator of pituitary corticotropin-release and consequent glucocorticoid secretion. NBI 35965 is a selective CRF receptor 1 (CRF1) antagonist with a Ki value of 4 nM.{29749,29750} It does not inhibit CRF2 (Ki = >10,000 nM).{29750} NBI 35965 inhibits cAMP accumulation and adrenocorticotropic hormone (ACTH) production in vitro (pIC50s = 7.1 and 6.9, respectively) and reduces CRF- and stress-induced ACTH production in vivo.{29748} In animal models of stress, NBI 35965 administration produces anxiolytic effects.{29750}  

 

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Description

A selective CRF1 antagonist (Ki = 4 nM); inhibits cAMP accumulation and ACTH production in vitro (pIC50s = 7.1 and 6.9, respectively) and reduces CRF- and stress-induced ACTH production in vivo

Formal name: (7S)-6-(cyclopropylmethyl)-2-(2,4-dichlorophenyl)-7-ethyl-7,8-dihydro-4-methyl-6H-1,3,6,8a-tetraazaacenaphthylene, monomethanesulfonate

Synonyms: 

Molecular weight: 497.4

CAS: 603151-83-3

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Glucocorticoids & Mineralocorticoids||Research Area|Neuroscience|Behavioral Neuroscience|Anxiety||Research Area|Neuroscience|Neuroendocrinology

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