| Company Name: |
Pharmacodia (Beijing) Co.,Ltd
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| Tel: |
+86-400-851-9921 |
| Email: |
sales@pharmacodia.com |
| Products Intro: |
Product Name:GSK1059865
CAS:1191044-58-2
Package:10Mg-100g
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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 |
| 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 | |
| | GSK1059865 Preparation Products And Raw materials |
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