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- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
1191044-58-2
- 规格:
10 mM * 1 mL/5 mg/10 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥2150.0 |
|---|---|---|---|
| 规格: | 5 mg | 产品价格: | ¥1950.0 |
| 规格: | 10 mg | 产品价格: | ¥3100.0 |
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GSK1059865
CAS No. : 1191044-58-2
MCE 国际站:GSK1059865
产品活性:GSK1059865是有效地食欲素1受体 (orexin 1 receptor) 拮抗剂。
研究领域:GPCR/G Protein | Neuronal Signaling
作用靶点:Orexin Receptor (OX Receptor)
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 EC50 and a concomitant decrease of the agonist maximal response. The calculated pKB 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 EC50 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.
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