GSK 962040
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- CAS号:
- 923565-21-3
- 英文名:
- GSK962040
- 英文别名:
- Camicil;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]-
- 中文名:
- GSK 962040
- 中文别名:
- 化合物 T11508
- CBNumber:
- CB02627933
- 分子式:
- C25H33FN4O
- 分子量:
- 424.55
- MOL File:
- 923565-21-3.mol
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GSK 962040化学性质
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熔点:
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144℃
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沸点:
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610.0±55.0 °C(Predicted)
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密度:
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1.175±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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形态:
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Solid
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酸度系数(pKa):
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9.21±0.40(Predicted)
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颜色:
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White to off-white
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GSK 962040性质、用途与生产工艺
Camicinal (GSK962040) 是胃动素受体激动剂,pEC50为7.9。
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].
GSK 962040
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/04/30 | HY-10922 | Camicinal | | 1 mg | 980元 |
2024/04/30 | HY-10922 | GSK 962040 Camicinal | 923565-21-3 | 5mg | 2450元 |
923565-21-3, GSK 962040 相关搜索:
- C25H33FN4O
- 化合物 T11508
- 923565-21-3
- Ethanone, 1-[4-[(3-fluorophenyl)amino]-1-piperidinyl]-2-[4-[[(3S)-3-methyl-1-piperazinyl]methyl]phenyl]-
- Camicil
- GSK962040
(Camicinal
- Lopixibat chloride
- Camicinal
- 1-[4-[(3-Fluorophenyl)amino]-1-piperidinyl]-2-[4-[[(3S)-3-methyl-1-piperazinyl]methyl]phenyl]ethanone
- GSK962040