| Bioactivity | Belumosudil (KD025) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 µM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties[1]. | ||||||||||||
| Invitro | 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[1]. | ||||||||||||
| In Vivo | 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[2]. | ||||||||||||
| Name | Belumosudil | ||||||||||||
| CAS | 911417-87-3 | ||||||||||||
| Formula | C26H24N6O2 | ||||||||||||
| Molar Mass | 452.51 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Boerma, M., et al. Comparative gene expression profiling in three primary human cell lines after treatment with a novel inhibitor of Rho kinase. Blood Coagul Fibrinolysis. 2008 Oct;19(7):709-18. [2]. Lee, J.H., et al. Selective ROCK2 Inhibition In Focal Cerebral Ischemia. Ann Clin Transl Neurol. 2014 Jan 1;1(1):2-14. |