SNT-207858 free base is a selective, blood-brain barrier penetrating, potent, and orally active melanocortin-4 (MC-4) receptor antagonist. It demonstrates high affinity and selectivity for the MC-4 receptor, with an IC50 of 22 nM (binding) and 11 nM (function), showing 170-fold selectivity over MC-3 and 40-fold over MC-5. In preclinical studies, SNT-207858 significantly reduced tumor-induced weight loss in mice.
- Selective melanocortin-4 (MC-4) receptor antagonist
- Blood-brain barrier penetrating
- Orally active
- High potency with IC50 of 22 nM (binding) and 11 nM (function) on MC-4 receptor
- Shows 170-fold selectivity versus MC-3 and 40-fold selectivity versus MC-5
- Significantly reduces tumor-induced weight loss in mice with C26 adenocarcinoma-induced cachexia