S 25585 is a potent neuropeptide Y (NPY) Y5 receptor antagonist (IC50 values are 5.4, > 1000, > 10 000 and > 10 000 nM at Y5, Y1, Y2 and Y4 receptors respectively) that displays no affinity for a wide range of other receptors. Does not produce a conditioned taste aversion, suppress sodium appetite or cause pica in rats. Significantly inhibits NPY-induced feeding but not through blockade of Y5 receptors.
Molecular Weight | 528.5 |
Formula | C22H23F3N4O6S |
CAS Number | 263849-50-9 |
Solubility (25°C) | DMSO 52.85 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Awouters, et al. Annu Rev Pharmacol Toxicol. Pharmacology of antidiarrheal drugs.
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