SNT-207858
CAS No. : 1104080-42-3

SNT-207858
Cat. No. : CS-0003001
M. Wt. : 689.54
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  • Data Sheet

  • Introduction

  • SDS

  • COA & Spectra

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
Formula: C32H45Cl4N5O3
M. Wt. : 689.54
Solubility: DMSO

Activity:

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)[1] 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[1].

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[1].[1]Mice[1]

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[1].

References:

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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