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GSK1059865

رقم الكتالوجGC30832

GSK1059865 هو مضاد قوي لمستقبلات الأوركسين 1

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GSK1059865 التركيب الكيميائي

Cas No.: 1191044-58-2

الحجم السعر المخزون الكميّة
10mM (in 1mL DMSO)
168٫00
متوفر
2mg
110٫00
متوفر
5mg
175٫00
متوفر
10mg
304٫00
متوفر
25mg
634٫00
متوفر
50mg
1103٫00
متوفر
100mg
1930٫00
متوفر

Tel:(909) 407-4943 Email: sales@glpbio.com

مراجعات العميل

بناء على آراء العملاء.

  • GlpBio Citations

    GlpBio Citations
  • Bioactive Compounds Premium Provider

    Bioactive Compounds Premium Provider

Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Animal experiment:

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].

References:

[1]. Lopez MF, et al. The highly selective orexin/hypocretin 1 receptor antagonist GSK1059865 potently reduces ethanol drinking in ethanol dependent mice. Brain Res. 2016 Apr 1;1636:74-80.
[2]. Piccoli L, et al. Role of orexin-1 receptor mechanisms on compulsive food consumption in a model of binge eating in female rats. Neuropsychopharmacology. 2012 Aug;37(9):1999-2011.
[3]. Gozzi A, et al. Differential effect of orexin-1 and CRF-1 antagonism on stress circuits: a fMRI study in the rat with the pharmacological stressor Yohimbine. Neuropsychopharmacology. 2013 Oct;38(11):2120-30.

Background

GSK1059865 is a potent orexin 1 receptor antagonist.

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].

[1]. Lopez MF, et al. The highly selective orexin/hypocretin 1 receptor antagonist GSK1059865 potently reduces ethanol drinking in ethanol dependent mice. Brain Res. 2016 Apr 1;1636:74-80. [2]. Piccoli L, et al. Role of orexin-1 receptor mechanisms on compulsive food consumption in a model of binge eating in female rats. Neuropsychopharmacology. 2012 Aug;37(9):1999-2011. [3]. Gozzi A, et al. Differential effect of orexin-1 and CRF-1 antagonism on stress circuits: a fMRI study in the rat with the pharmacological stressor Yohimbine. Neuropsychopharmacology. 2013 Oct;38(11):2120-30.

Chemical Properties

Cas No. 1191044-58-2 SDF
Canonical SMILES O=C(N1[C@H](CNC2=NC=C(Br)C=C2)CC[C@H](C)C1)C3=CC=CC(F)=C3OC
Formula C20H23BrFN3O2 M.Wt 436.32
الذوبان DMSO : ≥ 50 mg/mL (114.59 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.2919 mL 11.4595 mL 22.919 mL
5 mM 0.4584 mL 2.2919 mL 4.5838 mL
10 mM 0.2292 mL 1.1459 mL 2.2919 mL
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