923565-21-3
基本信息
Camicinal
GSK962040
Lopixibat chloride
GSK962040 (Camicinal
1-[4-[(3-Fluorophenyl)amino]-1-piperidinyl]-2-[4-[[(3S)-3-methyl-1-piperazinyl]methyl]phenyl]ethanone
Ethanone, 1-[4-[(3-fluorophenyl)amino]-1-piperidinyl]-2-[4-[[(3S)-3-methyl-1-piperazinyl]methyl]phenyl]-
物理化学性质
| 熔点 | 144℃ |
| 沸点 | 610.0±55.0 °C(Predicted) |
| 密度 | 1.175±0.06 g/cm3(Predicted) |
| 储存条件 | -20°C储存 |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 9.21±0.40(Predicted) |
| 形态 | Solid |
| 颜色 | White to off-white |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H302 |
| 防范说明 | P264-P270-P301+P312-P330-P501 |
常见问题列表
pEC50: 7.9 (Motilin Receptor).
Camicinal (GSK962040) had no significant activity at a range of other receptors (including ghrelin), ion channels and enzymes. In rabbit gastric antrum, Camicinal (GSK962040) 300 nmol L 1-10 μmol L 1 caused a prolonged facilitation of the amplitude of cholinergically mediated contractions, to a maximum of 248 ± 47% at 3 μmol L 1. The pEC50 values for motilin, erythromycin and Camicinal (GSK962040) were, respectively, 10.4 ± 0.01 (n = 770), 7.3 ± 0.29 (n = 4) and 7.9 ± 0.09 (n = 17) [1]. Camicinal (GSK962040) activated the dog motilin receptor (pEC50 5.79; intrinsic activity 0.72, compared with [Nle13]-motilin) [2]. Camicinal (GSK962040) was preferred because its initial IC 50 values at CYP3A4 were significantly higher than our preferred threshold of 10 μM [3].
Camicinal (GSK962040) (5 mg free base kg 1) also produced an increase in total faecal weight over the 2-h postdose period (21.2 ± 4.5 g; P < 0.05) [1]. Camicinal (GSK962040) induced phasic contractions, the duration of which was dose-related (48 and 173 min for 3 and 6 mg kg 1), driven by mean plasma concentrations >1.14 μmol L 1. After the effects of GSK962040 faded, migrating motor complex (MMC) activity returned. Migrating motor complex restoration was unaffected by 3 mg kg 1 GSK962040 but at 6 mg kg 1, MMCs returned 253 min after dosing, compared with 101 min after saline (n = 5 each) [2]. he oral bioavailability (Fpo) of Camicinal (GSK962040) was found to be 48 ( 13%. Camicinal (GSK962040) shows a long lasting effect (T1/2 ) 46.9 ( 5.0 min at 3 μM) when compared with the short-lived effect of [Nle13]motilin (T1/2 ) 11.4 ( 1.5 min at 0.3 μM) [3]. Camicinal (GSK962040) strongly facilitated cholinergic activity in the antrum, with lower activity in fundus and small intestine only [4].