Biological Activity
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.
Technical Data
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 43.78 | 100 | |
| water | 43.78 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 437.79. Batch specific molecular weights may vary from batch to batch due to solvent 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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References
References are publications that support the products' biological activity.
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
Keywords: NBI 35965 hydrochloride, supplier, NBI35965, CRF1R, CRF, 1, receptor, antagonist, corticotropin-releasing, factor, 1, antagonists, CRF1, Receptors, CRF1, Receptors, Tocris Bioscience
