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

GSK1059865 is a potent orexin 1 receptor antagonist.

For research use only. We do not sell to patients.

GSK1059865 Chemical Structure

GSK1059865 Chemical Structure

CAS No. : 1191044-58-2

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 215 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

GSK1059865 Related Antibodies

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OX2 Receptor OX1 Receptor

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK1059865 is a potent orexin 1 receptor antagonist.

IC50 & Target

OX1 Receptor

 

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

436.32

Formula

C20H23BrFN3O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1[C@H](CNC2=NC=C(Br)C=C2)CC[C@H](C)C1)C3=CC=CC(F)=C3OC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (458.38 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  30% SBE-β-CD in Saline

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

  • Protocol 2

    Add each solvent one by one:  30% PEG300    70% (10% HP-β-CD in Saline)

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

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.83%

COA (253 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References
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.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 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
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GSK1059865 Related Classifications

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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