1104080-42-3

1104080-42-3 structure

Name: SNT-207858
Chemical Name: N-[(2R)-3-(2,4-Dichlorophenyl)-1-oxo-1-(4-{3-[(2R)-2-(1-pyrrolidinyl)butoxy]-2-pyridinyl}-1-piperidinyl)-2-propanyl]-1-pyrrolidinecarboximidic acid dihydrochloride
CAS Number: 1104080-42-3
Molecular Formula: C₃₂H₄₅Cl₄N₅O₃
Molecular Weight: 689.543
Catalog: Research Areas Cancer
Create Date: 2018-07-01 05:55:37
Modify Date: 2024-01-11 20:20:44
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.

Name	N-[(2R)-3-(2,4-Dichlorophenyl)-1-oxo-1-(4-{3-[(2R)-2-(1-pyrrolidinyl)butoxy]-2-pyridinyl}-1-piperidinyl)-2-propanyl]-1-pyrrolidinecarboximidic acid dihydrochloride
Synonyms	1-Pyrrolidinecarboximidic acid, 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) N-[(2R)-3-(2,4-Dichlorophenyl)-1-oxo-1-(4-{3-[(2R)-2-(1-pyrrolidinyl)butoxy]-2-pyridinyl}-1-piperidinyl)-2-propanyl]-1-pyrrolidinecarboximidic acid dihydrochloride SNT-207858

Description	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.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Melanocortin Receptor Research Areas >> Metabolic Disease Research Areas >> Cancer
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].
Animal Admin	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	[1]. 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.