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

GSK1059865是有效地食欲素1受體 (orexin 1 receptor) 拮抗劑。

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GSK1059865 Chemical Structure

GSK1059865 Chemical Structure

CAS No. : 1191044-58-2

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規(guī)格 價(jià)格 是否有貨 數(shù)量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥2150
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5 mg ￥1950
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10 mg ￥3100
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25 mg 現(xiàn)貨 詢價(jià)
50 mg   詢價(jià)  
100 mg   詢價(jià)  

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Customer Review

查看 Orexin Receptor (OX Receptor) 亞型特異性產(chǎn)品:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

GSK1059865 is a potent orexin 1 receptor antagonist.

IC50 & Target

Orexin 1 receptor[1]
體內(nèi)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 號(hào)
性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 200 mg/mL (458.38 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn)：

以下溶解方案，請直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比； 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶。

  • 方案 一

    請依序添加每種溶劑： 30% SBE-β-CD in Saline

    Solubility: 3.33 mg/mL (7.63 mM); 澄清溶液; 超聲助溶

  • 方案 二

    請依序添加每種溶劑： 30% PEG300    70% (10% HP-β-CD in Saline)

    Solubility: 5 mg/mL (11.46 mM); 懸濁液; 超聲助溶

動(dòng)物溶解方案計(jì)算器
請輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.83%

參考文獻(xiàn)
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.
參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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.

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產(chǎn)品名稱：
GSK1059865
目錄號(hào)：
HY-101534
需求量：