GSK1059865

Product Name: GSK1059865
CAS No.: 1191044-58-2
Chemical Name: GSK1059865
Synonyms: GSK1059865;GSK1059865 HCl;GSK-1059865 (GSK 1059865;((2S,5S)-2-(((5-Bromopyridin-2-yl)amino)methyl)-5-methylpiperidin-1-yl)(3-fluoro-2-methoxyphenyl)methanone;Methanone, [(2S,5S)-2-[[(5-bromo-2-pyridinyl)amino]methyl]-5-methyl-1-piperidinyl](3-fluoro-2-methoxyphenyl)-
CBNumber: CB63067549
Molecular Formula: C20H23BrFN3O2
Formula Weight: 436.32
MOL File: 1191044-58-2.mol

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GSK1059865 Property

Boiling point:: 575.8±50.0 °C(Predicted)
Density: 1.376±0.06 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO : ≥ 50 mg/mL (114.59 mM)
form: Solid
pka: 4.89±0.10(Predicted)
color: White to off-white

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-7915
Product name: GSK1059865
Purity: 99.55%
Packaging: 5mg
Price: $192
Updated: 2021/12/16

ChemScene

Product number: CS-7915
Product name: GSK1059865
Purity: 99.55%
Packaging: 10mg
Price: $324
Updated: 2021/12/16

AK Scientific

Product number: SYN5019
Product name: GSK1059865
Packaging: 10mg
Price: $335
Updated: 2021/12/16

ChemScene

Product number: CS-7915
Product name: GSK1059865
Purity: 99.55%
Packaging: 25mg
Price: $684
Updated: 2021/12/16

ChemScene

Product number: CS-7915
Product name: GSK1059865
Purity: 99.55%
Packaging: 50mg
Price: $1152
Updated: 2021/12/16

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GSK1059865 Chemical Properties,Usage,Production

Uses

GSK1059865 is a potent orexin 1 receptor antagonist.

Biological Activity

GSK1059865 is a potent orexin 1 receptor antagonist.

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. GSK1059865 (0.3 nM-10 nM) produces non-surmountable antagonism with a dose-dependent rightward shift of the OXA EC ₅₀ 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 EC ₅₀ without depression of the agonist maximal response. Intraperitoneal The 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 ani mals exhibit slightly higher baseline mean arterial blood pressure values than controls.

target

Orexin 1 receptor

IC 50

OX₁ Receptor

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. DOI:10.1016/j.brainres.2016.01.049
[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. DOI:10.1038/npp.2012.48
[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. DOI:10.1038/npp.2013.109

GSK1059865 Preparation Products And Raw materials

Raw materials

Preparation Products

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GSK1059865 Suppliers

China 23 United Kingdom 1 United States 7 Global 31

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1191044-58-2, GSK1059865Related Search:

GSK1059865

GSK-1059865 (GSK 1059865

Methanone, [(2S,5S)-2-[[(5-bromo-2-pyridinyl)amino]methyl]-5-methyl-1-piperidinyl](3-fluoro-2-methoxyphenyl)-

GSK1059865 HCl

((2S,5S)-2-(((5-Bromopyridin-2-yl)amino)methyl)-5-methylpiperidin-1-yl)(3-fluoro-2-methoxyphenyl)methanone

1191044-58-2

C20H23BrFN3O2