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Submit ReviewNBI 35965 hydrochloride
Description: Potent and selective CRF1 antagonist
Chemical Name: (7S)-6-(Cyclopropylmethyl)-2-(2,4-dichlorophenyl)-7-ethyl-7,8-dihydro-4-methyl-6H-1,3,6,8a-tetraazaacenaphthylene hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for NBI 35965 hydrochloride
NBI 35965 hydrochloride is a potent and selective corticotropin-releasing factor receptor 1 (CRF1) antagonist (Ki values are 4 and > 10000 nM at CRF1 and CRF2 respectively). Inhibits cAMP accumulation and adrenocorticotropic hormone (ACTH) production in vitro (pIC50 values are 7.1 and 6.9 respectively) and attenuates CRF and ACTH production in vivo. Orally active and brain penetrant with anxiolytic activity.
Compound Libraries for NBI 35965 hydrochloride
NBI 35965 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for NBI 35965 hydrochloride
| M. Wt | 437.79 |
| Formula | C21H22Cl2N4.HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 1782228-59-4 |
| PubChem ID | 71433630 |
| InChI Key | LNYUWBPFYXPUIO-RSAXXLAASA-N |
| Smiles | CC[C@@H]3N(CC5CC5)C1=C2C(C(C4=CC=C(Cl)C=C4Cl)=NN2C3)=NC(C)=C1.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for NBI 35965 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 43.78 | 100 | |
| DMSO | 43.78 | 100 |
Preparing Stock Solutions for NBI 35965 hydrochloride
The following data is based on the product molecular weight 437.79. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.28 mL | 11.42 mL | 22.84 mL |
| 5 mM | 0.46 mL | 2.28 mL | 4.57 mL |
| 10 mM | 0.23 mL | 1.14 mL | 2.28 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
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Product Datasheets for NBI 35965 hydrochloride
References for NBI 35965 hydrochloride
References are publications that support the biological activity of the product.
Million et al (2003) 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 PMID: 12957366
Hoare et al (2003) Mechanism of corticotropin-releasing factor type I receptor regulation by non-peptide antagonists. Mol.Pharmacol. 63 751 PMID: 12606786
Gross et al (2005) Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists. J.Med.Chem. 48 5780 PMID: 16134945
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Keywords: NBI 35965 hydrochloride, NBI 35965 hydrochloride supplier, NBI35965, CRF1R, CRF, 1, receptor, antagonist, corticotropin-releasing, factor, antagonists, CRF1, Receptors, 3100, Tocris Bioscience
2 Citations for NBI 35965 hydrochloride
Citations are publications that use Tocris products. Selected citations for NBI 35965 hydrochloride include:
Abdelhamid et al (2013) Forced swim-induced musculoskeletal hyperalgesia is mediated by CRF2 receptors but not by TRPV1 receptors. Neuropharmacology 72 29 PMID: 23624287
Martinon and Dabrowska (2018) Corticotropin-Releasing Factor Receptors Modulate OXT Release in the Dorsolateral Bed Nucleus of the Stria Terminalis (BNST) in Male Rats. Front Neurosci 12 183 PMID: 29618970
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Literature in this Area
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Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.