SNT-207707 is a potent, selective and orally active antagonist of melanocortin MC-4 receptor(IC50 of 8 nM (binding) and 5 nM (function) on the MC-4 receptor).
SNT-207858 is a selective, blood brain barrier penetrating, potent and orally active antagonist of melanocortin-4 (MC-4) receptor. SNT207858 has an IC50 of 22 nM (binding) and 11 nM (function) on the MC-4 receptor.
Vepdegestrant (ARV-471) 是一种具有选择性和高效性的雌激素受体(ER,ESR1)PROTAC 降解剂,对 ER 蛋白具有强效降解能力。Vepdegestrant 通过直接降解 ER 蛋白而非单纯拮抗其活性,有效抑制 ER 信号通路,在 ER 阳性(ER⁺)乳腺癌中表现出显著的抗肿瘤活性,DC50 值约为 2 nM,尤其对 ESR1 突变型肿瘤同样具有良好效果。