2. GPCR/G Protein Neuronal Signaling
  3. Orexin Receptor (OX Receptor)
  4. GSK1059865

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

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GSK1059865 Chemical Structure

GSK1059865 Chemical Structure

CAS No. : 1191044-58-2

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规格 价格 是否有货 数量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥2150
In-stock
5 mg ￥1950
In-stock
10 mg ￥3100
In-stock
25 mg 现货 询价
50 mg   询价  
100 mg   询价  

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Customer Review

GSK1059865 相关抗体

Top Publications Citing Use of Products

查看 Orexin Receptor (OX Receptor) 亚型特异性产品:

查看所有亚型
OX2 Receptor OX1 Receptor

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

GSK1059865 is a potent orexin 1 receptor antagonist.

IC50 & Target

Orexin 1 receptor[1]
体内研究
(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[1]. 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[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

436.32

Formula

C20H23BrFN3O2
CAS 号
性状

固体

颜色

White to off-white

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 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 200 mg/mL (458.38 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 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。

  • 方案 一

    请依序添加每种溶剂： 30% SBE-β-CD in Saline

    Solubility: 3.33 mg/mL (7.63 mM); 澄清溶液; 超声助溶

  • 方案 二

    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); 悬浊液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.83%

COA (197 KB) LCMS (93 KB)

产品使用指南 (1538 KB)
参考文献
Animal Administration
[1][2]

Rats: GSK1059865 is dissolved in 0.5% HPMC (w/v) in distilled water and administered by gavage at doses of 10 and 30 mg/kg to rats. Drug or vehicle is administered 1 h before access to highly palatable food[2].

Mice: During baseline and the first 5 test cycles following chronic intermittent ethanol (or air) exposure, mice receive vehicle (saline) injections (i.p.; 0.01 ml/g body weight) 30 minutes before drinking ethanol. On test cycles 6 and 7 mice receive vehicle or GSK1059865 (10, 25, 50 mg/kg) before given access to ethanol 15% v/v (Test 6) or sucrose 5% w/v (Test 7) versus water. GSK1059865 is dissolved in saline and TWEEN 80 (0.5 % v/v) as vehicle[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

GSK1059865 相关分类

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2919 mL 11.4595 mL 22.9190 mL 57.2974 mL
5 mM 0.4584 mL 2.2919 mL 4.5838 mL 11.4595 mL
10 mM 0.2292 mL 1.1459 mL 2.2919 mL 5.7297 mL
15 mM 0.1528 mL 0.7640 mL 1.5279 mL 3.8198 mL
20 mM 0.1146 mL 0.5730 mL 1.1459 mL 2.8649 mL
25 mM 0.0917 mL 0.4584 mL 0.9168 mL 2.2919 mL
30 mM 0.0764 mL 0.3820 mL 0.7640 mL 1.9099 mL
40 mM 0.0573 mL 0.2865 mL 0.5730 mL 1.4324 mL
50 mM 0.0458 mL 0.2292 mL 0.4584 mL 1.1459 mL
60 mM 0.0382 mL 0.1910 mL 0.3820 mL 0.9550 mL
80 mM 0.0286 mL 0.1432 mL 0.2865 mL 0.7162 mL
100 mM 0.0229 mL 0.1146 mL 0.2292 mL 0.5730 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK10598651191044-58-2GSK 1059865GSK-1059865Orexin Receptor (OX Receptor)Hypocretin ReceptorHCRT ReceptorInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-101534
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