| 货号 | 3100/50 |
| 别名 | (7S)-6-(Cyclopropylmethyl)-2-(2,4-d |
| 供应商 | Tocris |
| 生物活性 | 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. |
| 运输条件 | Ambient |
| 存放说明 | Ambient |
| 纯度 | >98 % |
| 计算分子量 | 437.79 |
| 分子式 | C21H22Cl2N4< |
| 可溶性/溶解性 | Soluble to 100 mM in water and to 100 mM in DMSO |
| 参考文献 | Grosset al (2005) Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists. J.Med.Chem. 48 5780. PMID: 16134945. Hoareet al (2003) Mechanism of corticotropin-releasing factor type I receptor regulation by non-peptide antagonists. Mol.Pharmacol. 63 751. PMID: 12606786. Millionet 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. |