Bioactivity | SNT207858 free base is a selective, blood brain barrier penetrating, potent and orally active melanocortin-4 (MC-4) receptor antagonist. SNT207858 free base has an IC50 of 22 nM (binding) and 11 nM (function) on the MC-4 receptor[1]. | ||||||||||||
Target | MC-4 receptor | ||||||||||||
Invitro | SNT207858 binds to the MC-4 receptor with an affinity of 22 nM and shows a 170-fold selectivity vs. MC-3 and a 40-fold selectivity vs. MC-5[1]. | ||||||||||||
In Vivo | SNT207858 (30 mg/kg; oral administration; once daily; 15 days) significantly reduces the tumor induced weight loss in mice[1]. Animal Model: | ||||||||||||
Name | SNT-207858 free base | ||||||||||||
CAS | 1104662-66-9 | ||||||||||||
Formula | C32H43Cl2N5O3 | ||||||||||||
Molar Mass | 616.62 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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. |