CP 376395
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 |
CP 376395 用途与合成方法
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.
CP 376395 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-11-08 | HY-14130 | CP 376395 | 175140-00-8 | 5mg | 915 |
| 2024-11-08 | HY-14130 | CP 376395 | 175140-00-8 | 10mM * 1mLin DMSO | 1006 |
