GSK1059865 is a potentorexin 1 receptorantagonist.

Orexin 1 receptor^[1]

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^[1]. GSK1059865 (0.3 nM-10 nM) produces non-surmountable antagonism with a dose-dependent rightward shift of the OXA EC₅₀and a concomitant decrease of the agonist maximal response. The calculated pK_Bvalue 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 EC₅₀without depression of the agonist maximal response^[2]. 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^[3].

436.32

Solid

C₂₀H₂₃BrFN₃O₂

1191044-58-2

Room temperature in continental US; may vary elsewhere.

DMSO : 200 mg/mL(458.38 mM;Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 30%PEG300   70% (10%HP-β-CDin saline)

  Solubility: 5 mg/mL (11.46 mM); Suspended solution; Need ultrasonic
• 2.

  请依序添加每种溶剂： 30 %SBE-β-CD

  Solubility: 3.33 mg/mL (7.63 mM); Clear solution; Need ultrasonic