CP 376395
| 中文名称 | CP 376395 |
|---|---|
| 中文同义词 | 化合物CP 376395;2-(均三甲苯基氧基)-3,6-二甲基-N-(戊-3-基)吡啶-4-胺 |
| 英文名称 | CP 376395 |
| 英文同义词 | CP 376395;CP 376395 hydrochloride;N-(1-Ethylpropyl)-3,6-dimethyl-2-(2,4,6-trimethylphenoxy)-4-pyridinaminehydrochloride;CP376395;CP-376395;CP 376395;4-Pyridinamine, N-(1-ethylpropyl)-3,6-dimethyl-2-(2,4,6-trimethylphenoxy)-;inhibit,CP376395,Inhibitor,Corticotropin-releasing Factor Receptor,CRFR,CP 376395,CP-376395;2-(Mesityloxy)-3,6-dimethyl-N-(pentan-3-yl)pyridin-4-amine;3,6-dimethyl-N-(pentan-3-yl)-2-(2,4,6-trimethylphenoxy)pyridin-4-amine |
| CAS号 | 175140-00-8 |
| 分子式 | C21H30N2O |
| 分子量 | 326.48 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 175140-00-8.mol |
| 结构式 |  |
CP 376395 性质
| 熔点 | 224 °C |
|---|---|
| 沸点 | 434.9±45.0 °C(Predicted) |
| 密度 | 1.018±0.06 g/cm3(Predicted) |
| 储存条件 | Desiccate at RT |
| 溶解度 | DMF：30mg/mL； DMSO：15mg/mL；乙醇：30mg/mL |
| 形态 | 结晶固体 |
| 酸度系数(pKa) | 7.23±0.48(Predicted) |
| 颜色 | 白色至米白色 |
CRF1
CP 376395 fully antagonizes oCRF-stimulated adenylate cyclase activity in rat cerebral cortex and at human CRF1 receptors with an apparent K i value of 12 nM, indicating antagonist functional activity. It is highly selective for the human CRF1 receptor subtype; affinity for the CRF2 receptor is >10000 nM. It shows affinities greater than 1 µM against 40 neurotransmitter receptor and ion channels.
In the CNS, systemically administered CP 376395 blocks the effects of both exogenous and endogenous CRF. Pretreatment with CP 376395 reverses the excitation of locus coeruleus neurons induced by icv CRF (3 µg) with an ID 50 of completely blocked the enhanced startle response induced by icv CRF (1 µg) at 17.8 mg/kg, p.o. and partially blocked at 10 mg/kg, p.o. without significantly altering baseline startle. The attenuation of fear-potentiated startle is statistically significant at lower doses (0.32-3.2 mg/kg, p.o., with 62-83% blockade) and completely reversed by CP 376395 at 10 mg/kg, p.o.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/08/19 | HY-14130 | CP 376395 CP 376395 | 175140-00-8 | 5mg | 915元 |
| 2024/08/19 | HY-14130 | CP 376395 CP 376395 | 175140-00-8 | 10mM * 1mLin DMSO | 1006元 |