PROTAC AR Degrader-9

PROTAC AR Degrader-9 (compound C6) (0.4 mg/mouse; topical; single dose) shows excellent skin retention properties with a C_max of 86701.15 ng/g and an AUC_0-t of 651924.91 ng/g·h, and exhibits minimal systemic plasma exposure (C_max = 707.90 ng/mL; AUC_0-t = 992.42 ng/mL·h) in male ICR mice^[1].
PROTAC AR Degrader-9 (0.4 mg/mouse; topical; single dose) distributes to heart, liver, spleen, lung and kidney tissues, accumulates most abundantly in spleen and lung, and maintains markedly higher concentrations in skin than in plasma and all other tissues at all detection time points in male ICR mice^[1].
PROTAC AR Degrader-9 (0.1%, 0.4% solution; topical; once daily for 14 days) promotes hair regeneration in a dose-dependent manner and delivers therapeutic efficacy comparable to 5% Minoxidil (HY-B0112) in terms of hair coverage and pigment indicators in testosterone-induced male C57BL/6 AGA mice^[1].
PROTAC AR Degrader-9 (0.4% solution; topical; once daily for 14 days) degrades more than 50% of AR protein in dorsal skin tissue, upregulates β-catenin and Ki67 expression while downregulating TGF-β1 in hair follicles, thickens hair shafts, elevates hair density, improves hair cuticle integrity, raises hair cycle scores and facilitates more telogen hair follicles to enter the anagen phase in male C57BL/6 mice^[1].