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GSK1059865

Catalog No: 24131
CAS Number: 1191044-58-2
Purity: 98% Min.

GSK1059865 is a potent orexin 1 receptor antagonist.

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

Chemical Information

NameGSK1059865
Iupac Chemical Name((2S,5S)-2-(((5-bromopyridin-2-yl)amino)methyl)-5-methylpiperidin-1-yl)(3-fluoro-2-methoxyphenyl)methanone
SynonymsGSK1059865; GSK 1059865; GSK-1059865
Molecular FormulaC20H23BrFN3O2
Molecular Weight436.32
SmileO=C(N1[C@H](CNC2=NC=C(Br)C=C2)CC[C@H](C)C1)C3=CC=CC(F)=C3OC
InChiKeyTWCRHJLMMAYSTE-ZFWWWQNUSA-N
InChiInChI=1S/C20H23BrFN3O2/c1-13-6-8-15(11-24-18-9-7-14(21)10-23-18)25(12-13)20(26)16-4-3-5-17(22)19(16)27-2/h3-5,7,9-10,13,15H,6,8,11-12H2,1-2H3,(H,23,24)/t13-,15-/m0/s1
CAS Number1191044-58-2
Related CAS

Ordering Information

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FormulationOff-white solid
Purity98% Min.
StorageDry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years).
SolubilitySoluble in DMSO
Handling
Shipping ConditionShipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
HS Code
Coming soon.
Targets
Mechanism
Cell study
Animal study
Clinical study

1: Lopez MF, Moorman DE, Aston-Jones G, Becker HC. 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. Epub 2016 Feb 4. PMID: 26851547; PMCID:
PMC4808605.

2: Merlo Pich E, Melotto S. Orexin 1 receptor antagonists in compulsive behavior
and anxiety: possible therapeutic use. Front Neurosci. 2014 Feb 13;8:26. doi:
10.3389/fnins.2014.00026. PMID: 24592206; PMCID: PMC3923148.

3: Gozzi A, Turrini G, Piccoli L, Massagrande M, Amantini D, Antolini M,
Martinelli P, Cesari N, Montanari D, Tessari M, Corsi M, Bifone A. Functional
magnetic resonance imaging reveals different neural substrates for the effects
of orexin-1 and orexin-2 receptor antagonists. PLoS One. 2011 Jan
28;6(1):e16406. doi: 10.1371/journal.pone.0016406. PMID: 21307957; PMCID:
PMC3030585.

4: Piccoli L, Micioni Di Bonaventura MV, Cifani C, Costantini VJ, Massagrande M,
Montanari D, Martinelli P, Antolini M, Ciccocioppo R, Massi M, Merlo-Pich E, Di
Fabio R, Corsi M. 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. Epub 2012 May 9. PMID:
22569505; PMCID: PMC3398727.

5: Gozzi A, Lepore S, Vicentini E, Merlo-Pich E, Bifone A. 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. Epub 2013 May 8. PMID: 23736277;
PMCID: PMC3773661.

Chemical Structure

24131 - GSK1059865 | CAS 1191044-58-2

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