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S 25585

Cat. No. M7237
S 25585 Structure
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Biological Activity

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.

Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Awouters, et al. Annu Rev Pharmacol Toxicol. Pharmacology of antidiarrheal drugs.

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Keywords: S 25585 supplier, Neuropeptide Receptor, inhibitors, activators


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