生物活性 靶点 体外研究 体内研究 GSK 962040 试剂级价格
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GSK 962040

GSK 962040,923565-21-3,结构式
GSK 962040
  • CAS号:923565-21-3
  • 英文名:GSK962040
  • 中文名:GSK 962040
  • CBNumber:CB02627933
  • 分子式:C25H33FN4O
  • 分子量:424.55
  • MOL File:923565-21-3.mol
GSK 962040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 :Store at -20°C
  • 溶解度 :Soluble in DMSO
  • 酸度系数(pKa) :9.21±0.40(Predicted)

GSK 962040性质、用途与生产工艺

  • 生物活性 Camicinal (GSK962040) 是胃动素受体激动剂,pEC50为7.9。
  • 靶点

    pEC50: 7.9 (Motilin Receptor).

  • 体外研究

    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].

  • 体内研究

    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
GSK 962040 试剂级价格
  • 更新日期:2024/04/30
  • 产品编号:HY-10922
  • 产品名称:Camicinal
  • CAS编号:
  • 包装:1 mg
  • 价格:980元
  • 更新日期:2024/04/30
  • 产品编号:HY-10922
  • 产品名称:GSK 962040 Camicinal
  • CAS编号:923565-21-3
  • 包装:5mg
  • 价格:2450元
GSK 962040生产厂家
  • 公司名称:Musechem
  • 联系电话:+1-800-259-7612
  • 电子邮件:info@musechem.com
  • 国家:美国
  • 产品数:4662
  • 优势度:60
  • 公司名称:TargetMol Chemicals Inc.
  • 联系电话:+1-781-999-5354 +1-00000000000
  • 电子邮件:marketing@targetmol.com
  • 国家:美国
  • 产品数:19892
  • 优势度:58
  • 公司名称:InvivoChem
  • 联系电话:+1-708-310-1919 +1-13798911105
  • 电子邮件:sales@invivochem.cn
  • 国家:美国
  • 产品数:6393
  • 优势度:58
  • 公司名称:河南科锐化工有限公司
  • 联系电话:+86-0371-86658258 15093356674;
  • 电子邮件:laboratory@coreychem.com
  • 国家:中国
  • 产品数:30255
  • 优势度:58