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CAS No. : 1104080-42-3
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|Name:||SNT-207858; 1-Pyrrolidinecarboxamide, N-[(1R)-1-[(2,4-dichlorophenyl)methyl]-2-oxo-2-[4-[3-[(2R)-2-(1-pyrrolidinyl)butoxy]-2-pyridinyl]-1-piperidinyl]ethyl]-, hydrochloride (1:2)|
|Cat. No. :||CS-0003001|
|CAS No. :||1104080-42-3|
|M. Wt. :||689.54|
|Solubility:||10 mM in DMSO|
SNT-207858 is a selective and orally available melanocortin MC-4 receptor antagonist with a 170-fold selectivity vs. MC-3 and a 40-fold selectivity versus MC-5. SNT-207858 has an IC50 of 8 nM (binding) and 5 nM (function) on the MC-4 receptor. IC50 & Target: IC50: 8 nM (binding, MC-4), 5 nM (function, MC-4) In Vivo: Subcutaneous injection or oral treatment by gavage of SNT-207858 distinctly increase food intake in healthy mice. In mice subcutaneously implanted with C26 adenocarcinoma cells, repeated oral administration (starting the day after tumor implantation) of SNT-207858 almost completely prevents tumor induced weight loss, and diminished loss of lean body mass and fat mass.
Protocol:Animal Administration: SNT-207858 is dissolved and administered by oral gavage at the indicated doses in a volume of 10 mL/kg of 10% Hydroxypropyl-β-cyclodextrin.Mice
Twelve weeks old male CD-1 mice are dosed by gavage with SNT207858 at 60 mg/kg. At 1, 3, and 6 hrs post-dose, mice are euthanized and blood is collected.
Weyermann P, et al. Orally available selective melanocortin-4 receptor antagonists stimulate food intake and reduce cancer-induced cachexia in mice. PLoS One. 2009;4(3):e4774.
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