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NPY5RA-972 

Cat. No. M30096
NPY5RA-972  Structure
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Biological Activity

NPY5RA-972 is an orally active, central nervous system (CNS) penetrating, potent and selective NPY Y5 receptor antagonist that prevents feeding driven by activation of this receptor.

Chemical Information
Molecular Weight 351.44
Formula C21H25N3O2
CAS Number 439861-56-0
Form Solid
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] P Li, et al. Int J Obes (Lond). Genetic association analysis of 30 genes related to obesity in a European American population

[2] Bartolo Gabriele, et al. J Org Chem. Efficient synthesis of ureas by direct palladium-catalyzed oxidative carbonylation of amines

[3] Andrew V Turnbull, et al. Diabetes. Selective antagonism of the NPY Y5 receptor does not have a major effect on feeding in rats

[4] Michael H Block, et al. J Med Chem. Discovery and optimization of a series of carbazole ureas as NPY5 antagonists for the treatment of obesity

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Keywords: NPY5RA-972  supplier, Neuropeptide Receptor, inhibitors, activators


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