SNT-207858

Names

[ CAS No. ]:
1104080-42-3

[ Name ]:
SNT-207858

[Synonym ]:
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

Biological Activity

[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.


[Related Small Molecules]

Setmelanotide | Bremelanotide Acetate | JNJ-10229570 | ACTH [1-17] | MC-4R Agonist 1 | PF-00446687 | SNT-207707 | β-MSH (human) trifluoroacetate salt

Chemical & Physical Properties

[ Molecular Formula ]:
C32H45Cl4N5O3

[ Molecular Weight ]:
689.543

[ Exact Mass ]:
687.227661

Related Compounds