Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK1059865 is a potent antagonist of the orexin 1 receptor.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
2 mg | 6-8 weeks | $ 108.00 | |
25 mg | 6-8 weeks | $ 736.00 | |
50 mg | 6-8 weeks | $ 956.00 | |
100 mg | 6-8 weeks | $ 1,690.00 |
Description | GSK1059865 is a potent antagonist of the orexin 1 receptor. |
In vivo | GSK1059865 (0.3?nM-10?nM) produces non-surmountable antagonism with a dose-dependent rightward shift of the OXA EC50 and a concomitant decrease of the agonist maximal response.?The calculated pKB 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 EC50 without depression of the agonist maximal response.?Intraperitoneal 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 animals exhibit slightly higher baseline mean arterial blood pressure values than controls.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. |
Molecular Weight | 436.32 |
Formula | C20H23BrFN3O2 |
CAS No. | 1191044-58-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (114.59 mM)
You can also refer to dose conversion for different animals. More
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GSK1059865 1191044-58-2 Others GSK 1059865 GSK-1059865 inhibitor inhibit