GSK1059865 - CAS:1191044-58-2

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GSK1059865

目录号 : KM6201 CAS No. : 1191044-58-2 纯度 : 98%

Data Sheet 产品使用指南

GSK1059865是有效地食欲素1受体 (orexin 1 receptor) 拮抗剂。

规格	价格	是否有货
2mg		In-stock
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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生物活性

GSK1059865 is a potent orexin 1 receptor antagonist.

体内研究

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 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 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.

分子式

C₂₀H₂₃BrFN₃O₂

分子量

436.32

CAS号

1191044-58-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

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

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2919 mL	11.4595 mL	22.9190 mL
5 mM	0.4584 mL	2.2919 mL	4.5838 mL
10 mM	0.2292 mL	1.1459 mL	2.2919 mL

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

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-CD in 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