GR 125743

目录号: PL02499 纯度: ≥99%
GR 125743 是一种选择性的 5-HT1B/1D 受体拮抗剂,与野生型的人 h5-HT1B 和 5-HT1D 结合的 pKi 分别为 8.85 和 8.31。GR 125743 可用于帕金森病和心血管疾病的研究。
CAS No. :148547-33-5
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中文名称
GR 125743
英文名称
GR 125743
英文别名
Benzamide,N-[4-methoxy-3-(4-methyl-1-piperazinyl)phenyl]-3-methyl-4-(4-pyridinyl)-;GR 125743
Cas No.
148547-33-5
分子式
C25H28N4O2
分子量
416.52
包装储存
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
详情描述
GR 125743 是一种选择性的 5-HT1B/1D 受体拮抗剂,与野生型的人 h5-HT1B 和 5-HT1D 结合的 pKi 分别为 8.85 和 8.31。GR 125743 可用于帕金森病和心血管疾病的研究。
产品详情
GR 125743 是一种选择性的 5-HT1B/1D 受体拮抗剂,与野生型的人 h5-HT1B 和 5-HT1D 结合的 pKi 分别为 8.85 和 8.31。GR 125743 可用于帕金森病和心血管疾病的研究。
生物活性
GR 125743 is a selective 5-HT 1B/1D receptor antagonist, with pK i s of 8.85 and 8.31 for wild-type h5-HT 1B and wild-type h5-HT 1D , respectively. GR 125743 is used for the research of Parkinsons disease and cardiovascular diseases.
性状
Solid
IC50 & Target[1][2]
human 5-HT1B Receptor 8.85 (pKi) human 5-HT1D Receptor
体外研究(In Vitro)
GR 125743 has a Kd of 0.61 nM for h5-HT1B.
has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
GR 125743 (0.3 mg/kg; i.p.) produces significant decreases in extracellular 5-HT in the frontal cortex of the conscious guinea pig.
has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献
[1]. T Wurch, et al. Induction of a high-affinity ketanserin binding site at the 5-Hydroxytryptamine(1B) receptor by modification of its carboxy-terminal intracellular portion. Characterization of human serotonin 1D and 1B receptors using [3H]-GR-125743, a nov
[2]. Roberts, C., et al. The role of 5-HT1B/1D receptors in the modulation of 5-hydroxytryptamine levels in the frontal cortex of the conscious guinea pig. European Journal of Pharmacology. 1997 May 12;326(1):23-30.
溶解度数据
In Vitro: DMSO : 100 mg/mL (240.08 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)
[1]. T Wurch, et al. Induction of a high-affinity ketanserin binding site at the 5-Hydroxytryptamine(1B) receptor by modification of its carboxy-terminal intracellular portion. Characterization of human serotonin 1D and 1B receptors using [3H]-GR-125743, a nov
[2]. Roberts, C., et al. The role of 5-HT1B/1D receptors in the modulation of 5-hydroxytryptamine levels in the frontal cortex of the conscious guinea pig. European Journal of Pharmacology. 1997 May 12;326(1):23-30.

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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