A selective CRF1 antagonist
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NBI 35965 (mesylate)

Item No. 18524

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 25 mg/mlEthanol: 10 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    1 mg

    $33

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    5 mg

    $98

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    10 mg

    $163

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    25 mg

    $367

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    Product Description

    NBI 35965 is a selective CRF receptor 1 (CRF1) antagonist with a Ki value of 4 nM.1,2 It does not inhibit CRF2 (Ki = >10,000 nM).2 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.3 In animal models of stress, NBI 35965 administration produces anxiolytic effects.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hoare, S.R.J., Sullivan, S.K., Ling, N., et al. Mechanism of corticotropin-releasing factor type I receptor regulation by nonpeptide antagonists. Mol. Pharmacol. 63(3), 751-765 (2003).

    2. Million, M., Grigoriadis, D.E., Sullivan, S., 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. 985, 32-42 (2003).

    3. Gross, R.S., Guo, Z., Dyck, B., et al. Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists. J. Med. Chem. 48, 5780-5793 (2005).