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)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P501Dispose of contents/container to..…

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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 24 United Kingdom 1 United States 7 Global 32

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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