GSK1059865 manufacturers
- GSK1059865
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- $0.00 / 1removed
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2026-02-25
- CAS:1191044-58-2
- Min. Order:
- Purity:
- Supply Ability: 10g
- GSK1059865
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- $108.00 / 2mg
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2025-07-20
- CAS:1191044-58-2
- Min. Order:
- Purity:
- Supply Ability: 10g
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| | GSK1059865 Basic information |
| Product Name: | GSK1059865 | | Synonyms: | 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 | | CAS: | 1191044-58-2 | | MF: | C20H23BrFN3O2 | | MW: | 436.32 | | EINECS: | | | Product Categories: | | | Mol File: | 1191044-58-2.mol |  |
| | GSK1059865 Chemical Properties |
| 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 |
| | GSK1059865 Usage And Synthesis |
| 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 | | | 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 |
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