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GSK962040

CAS No. 923565-21-3

GSK962040 ( Camicinal | GSK 962040 | GSK-962040 )

产品货号. M16615 CAS No. 923565-21-3

一种有效的、选择性的小分子胃动素受体激动剂,pEC50 为 7.9 (hMTL-R)。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
5MG ¥2811 有现货
50MG ¥12069 有现货
100MG ¥16119 有现货
200MG 获取报价 有现货
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    GSK962040
  • 注意事项
    本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
  • 产品简述
    一种有效的、选择性的小分子胃动素受体激动剂,pEC50 为 7.9 (hMTL-R)。
  • 产品描述
    A potent, selective, small molecule motilin receptor agonist with pEC50 of 7.9 (hMTL-R); displays selectivity over closely related human ghrelin acceptor (pEC50< 6.0) and no liabilities at the hERG.channel; possesses highly excellent pharmacokinetic profiles in both rat and dog.Other indication Phase 2 Clinical.
  • 体外实验
    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) . Camicinal (GSK962040) activated the dog motilin receptor (pEC50 5.79; intrinsic activity 0.72, compared with [Nle13]-motilin) . Camicinal (GSK962040) was preferred because its initial IC50 values at CYP3A4 were significantly higher than our preferred threshold of 10 μM .
  • 体内实验
    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) . 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) . 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) . Camicinal (GSK962040) strongly facilitated cholinergic activity in the antrum, with lower activity in fundus and small intestine only .
  • 同义词
    Camicinal | GSK 962040 | GSK-962040
  • 通路
    GPCR/G Protein
  • 靶点
    Motilin Receptor
  • 受体
    Motilin Receptor
  • 研究领域
    Other Indications
  • 适应症
    Other Disease

化学信息

  • CAS Number
    923565-21-3
  • 分子量
    424.5541
  • 分子式
    C25H33FN4O
  • 纯度
    >98% (HPLC)
  • 溶解度
    DMSO: 12.73 mg/mL (Need ultrasonic)
  • SMILES
    CC1CN(CCN1)CC2=CC=C(C=C2)CC(=O)N3CCC(CC3)NC4=CC(=CC=C4)F
  • 化学全称
    Ethanone, 1-[4-[(3-fluorophenyl)amino]-1-piperidinyl]-2-[4-[[(3S)-3-methyl-1-piperazinyl]methyl]phenyl]-

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

参考文献

1. Westaway SM, et al. J Med Chem. 2009 Feb 26;52(4):1180-9. 2. Sanger GJ, et al. Neurogastroenterol Motil. 2009 Jun;21(6):657-64, e30-1. 3. Broad J, et al. Br J Pharmacol. 2012 Oct;167(4):763-74.
产品手册
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