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GSK1059865

    级别和纯度:
  • 10mM in DMSO
  • CAS编号: 1191044-58-2
  • 分子式: C20H23BrFN3O2
  • 分子量: 436.33
有货

库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
G654590-1ml
1ml 期货 Stock Image

基本描述

规格或纯度 10mM in DMSO
英文名称 GSK1059865
生化机理 GSK1059865 是一种强效的奥曲肽 1 受体拮抗剂。
储存温度 -80℃储存
运输条件 超低温冰袋运输
产品介绍


GSK1059865 is a potent orexin 1 receptor antagonist.

In Vivo

Treatment with GSK1059865 significantly decreases ethanol drinking in a dose-dependent manner in CIE-exposed mice. In contrast GSK1059865 decreases drinking in air-exposed mice only at the highest dose used. There is no effect of GSK1059865 on sucrose intake . GSK1059865 (0.3 nM-10 nM) produces non-surmountable antagonism with a dose-dependent rightward shift of the OXA EC 50 and a concomitant decrease of the agonist maximal response. The calculated pK B value is 8.77±0.12 for GSK1059865. GSK1059865 (0.1-3.3 μM) produces a classical surmountable profile with parallel rightward shift of the OXA EC 50 without depression of the agonist maximal response. Intraperitoneal administration of GSK1059865 produces a region-dependent inhibition of yohimbine-induced relative cerebral blood volume response. The administration of GSK1059865 per se produces a weak relative cerebral blood volume increase in several brain regions. GSK1059865-pretreated animals exhibit slightly higher baseline mean arterial blood pressure values than controls. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:Orexin 1 receptor

关联靶点(人)

HCRTR1 Tclin 食欲素受体 1 型(Orexin receptor type 1) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
HCRTR2 Tclin 食欲素受体 2 型(Orexin receptor type 2) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

Isomeric SMILES C[C@H]1CC[C@H](N(C1)C(=O)C2=C(C(=CC=C2)F)OC)CNC3=NC=C(C=C3)Br
PubChem CID 44463491
分子量 436.33

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
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