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CAS: | 2109704-99-4 | Cat No: | JKN02922 | Purity: | 98% |
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Product Description
CAS | 2109704-99-4 | Cat No | JKN02922 | |
Name | Belumosudil Mesylate | |||
Synonyms | KD025 mesylate | |||
Smiles | CC(C)NC(=O)COC1=CC=CC(=C1)C2=NC=C3C(=N2)C=CC=C3NC4=CC5=C(C=C4)NN=C5.CS(=O)(=O)O | |||
Chemical Name | 2-[3-[5-(1H-indazol-5-ylamino)quinazolin-2-yl]phenoxy]-N-propan-2-ylacetamide;methanesulfonic acid | |||
Formula | C27H28N6O5S | MWt | 548.6 | |
Purity | 98% | Storage | Store at 4--8℃ | |
Description | Belumosudil Mesylate is the mesylate salt form of belumosudil, an orally bioavailable inhibitor of Rho-associated coiled-coil kinase 2 (ROCK2; ROCK-II), with potential immunomodulating activity. Upon oral administration, belumosudil binds to and inhibits the serine/threonine kinase activity of ROCK2. This inhibits ROCK2-mediated signal transduction pathways and modulates various pro- and anti-inflammatory immune cell responses through the regulation of signal transducer and activator of transcription 3 and 5 (STAT3/STAT5) phosphorylation. This downregulates pro-inflammatory Th17 cells and increases regulatory T (Treg) cells. Belumosudil also inhibits ROCK2-mediated fibrotic processes, including stress fiber formation, myofibroblast activation and pro-fibrotic gene transcription. ROCK2 is upregulated in various diseases, including various fibrotic, neurodegenerative and autoimmune diseases. |
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