Belumosudil mesylate

Modify Date: 2024-01-10 15:30:50

Belumosudil mesylate Structure
Belumosudil mesylate structure
Common Name Belumosudil mesylate
CAS Number 2109704-99-4 Molecular Weight 548.61
Density N/A Boiling Point N/A
Molecular Formula C27H28N6O5S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Belumosudil mesylate


Belumosudil mesylate (KD025 mesylate) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 µM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties[1].

 Names

Name Belumosudil mesylate

 Belumosudil mesylate Biological Activity

Description Belumosudil mesylate (KD025 mesylate) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 µM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties[1].
Related Catalog
Target

ROCK2:105 nM (IC50)

ROCK1:24 μM (IC50)

In Vitro 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].
References

[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.

 Chemical & Physical Properties

Molecular Formula C27H28N6O5S
Molecular Weight 548.61
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