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175140-00-8

中文名称 CP 376395
英文名称 CP 376395
CAS 175140-00-8
分子式 C21H30N2O
分子量 326.48
MOL 文件 175140-00-8.mol
更新日期 2023/08/30 13:34:15
175140-00-8 结构式 175140-00-8 结构式

基本信息

中文别名
化合物CP 376395
英文别名
CP 376395
CP 376395 hydrochloride
CP376395
CP-376395
CP 376395
4-Pyridinamine, N-(1-ethylpropyl)-3,6-dimethyl-2-(2,4,6-trimethylphenoxy)-
N-(1-Ethylpropyl)-3,6-dimethyl-2-(2,4,6-trimethylphenoxy)-4-pyridinaminehydrochloride

物理化学性质

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: 30 mg/ml; DMSO: 15 mg/ml; Ethanol: 30 mg/ml
酸度系数(pKa)7.23±0.48(Predicted)
形态A crystalline solid
颜色White to off-white
CP 376395价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/08/19HY-14130CP 376395
CP 376395
175140-00-85mg915元
2024/08/19HY-14130CP 376395
CP 376395
175140-00-810mM * 1mLin DMSO1006元
2024/08/19HY-14130CP 376395
CP 376395
175140-00-810mg1457元

常见问题列表

生物活性
CP 376395是有效和选择性的 CRF1 受体拮抗剂。
靶点

CRF1

体外研究

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.

体内研究

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.

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