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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 |
Powder |
-20°C |
3 years |
|
4°C |
2 years |
In solvent |
-80°C |
6 months |
|
-20°C |
1 month |
|
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. |