NBI 35965 (mesylate)

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. It does not inhibit CRF2 (Ki = >10,000 nM). 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. In animal models of stress, NBI 35965 administration produces anxiolytic effects.Formal Name: (7S)-6-(cyclopropylmethyl)-2-(2,4-dichlorophenyl)-7-ethyl-7,8-dihydro-4-methyl-6H-1,3,6,8a-tetraazaacenaphthylene, monomethanesulfonate. CAS Number: 603151-83-3. Molecular Formula: C21H22Cl2N4 . CH3SO3H. Formula Weight: 497.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 25 mg/ml, Ethanol: 10 mg/ml. lambdamax: 237, 329 nm. SMILES: CC1=CC(N(CC2CC2)[C@@H](CC)CN3N=C4C5=CC=C(Cl)C=C5Cl)=C3C4=N1.CS(=O)(O)=O. InChi Code: InChI=1S/C21H22Cl2N4.CH4O3S/c1-3-15-11-27-21-18(26(15)10-13-4-5-13)8-12(2)24-20(21)19(25-27)16-7-6-14(22)9-17(16)23,1-5(2,3)4/h6-9,13,15H,3-5,10-11H2,1-2H3,1H3,(H,2,3,4)/t15-,/m0./s1. InChi Key: ARENHXRYYRAMQA-RSAXXLAASA-N.