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CAS No. : 1064662-40-3
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|Name:||SNT-207707; Imidazo[1,2-a]pyridine-6-carboxamide, 2-(4-cyanophenyl)-N,N-bis(3-methylbutyl)-3-[3-(1-pyrrolidinyl)propyl]-, hydrochloride (1:1)|
|Cat. No. :||CS-0003000|
|CAS No. :||1064662-40-3|
|M. Wt. :||550.18|
SNT-207707 is a selective, potent and orally active melanocortin MC-4 receptor antagonist with 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 Vitro: SNT-207707 binds to the MC-4 receptor with an affinity of 8 nM and shows a more than 200-fold selectivity vs. MC-3 and MC-5. SNT207858 is a 22 nM MC-4 antagonist with a 170-fold selectivity vs. MC-3 and a 40-fold selectivity versus MC-5. In Vivo: Single subcutaneous injection of 20 mg/kg of SNT-207707 distinctly increases food intake of the mice. Once daily oral administration of both compounds SNT207858 and SNT-207707 starting the day after tumor implantation significantly reduces the tumor induced weight loss.
Protocol:Animal Administration: SNT-207707 is freshly dissolved and administered by oral gavage in a volume of 10 mL/kg of 10% Hydroxypropyl-β-cyclodextrin in 100 mM saline solution.Mice
Twelve weeks old male CD-1 mice are dosed by gavage with either SNT-207707 or SNT207858 at 60 mg/kg (n=9 per compound). At 1, 3, and 6 hrs post-dose, 3 mice from each compound group are euthanized with CO2. Blood is collected by cardiac puncture, plasma is isolated immediately and then kept on dry ice until analysis.
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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