Belumosudil (KD025) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 µM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties.
IC50&Target
ROCK2
105 nM (IC50)
ROCK1
24 μM (IC50)
体外研究
Belumosudil (SLx-2119; 40 µM) induces significant down-regulations of Tsp-1 and CTGF mRNA levels in PASMC. The microarray hybridized with aRNA from HMVEC treated with Belumosudil, shows a 5-times higher background than the other arrays.
体内研究
Belumosudil (KD-025; 100, 200 or 300 mg/kg, i.p.) dose-dependently reduces infarct volume after transient middle cerebral artery occlusion. Belumosudil is at least as efficacious in aged, diabetic or female mice, as in normal adult males.
分子式
C26H24N6O2
分子量
452.51
CAS号
911417-87-3
运输条件
Room temperature in continental US; may vary elsewhere.