Belumosudil mesylate

SKU: orb1691224

Description

Belumosudil mesylate

Research Area

Cell Biology, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 2109704-99-4
• MW: 548.61
• Purity: 99.36% (May vary between batches)
• Formula: C₂₇H₂₈N₆O₅S
• SMILES: O=C(NC(C)C)COC1=CC=CC(=C1)C=2N=C3C=CC=CC3=C(N2)NC=4C=CC=5NN=CC5C4.O=S(=O)(O)C
• Target: ROCK
• Solubility: H2O:1 mg/mL (1.82 mM);DMSO:20 mg/mL (36.46 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (1.82 mM)

Bioactivity

• Target IC50:
  ROCK2:105 nM (IC50)|ROCK1:24 μM (IC50)
• In Vivo:
  Intraperitoneal injection of 100, 200, or 300 mg/kg Belumosudil mesylate dose-dependently reduced infarct volume after transient middle cerebral artery occlusion. Belumosudil mesylate was at least as effective in aged, diabetic, or female mice as in normal adult male mice.
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• In Vitro:
  Belumosudil mesylate is a selective inhibitor of ROCK2, with IC50s of 105 nM and 24 μM for ROCK2 and ROCK1, respectively. 40 μM Belumosudil mesylate significantly down-regulated the levels of Tsp-1 and CTGF mRNA in pulmonary artery smooth muscle cells (PASMC).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

KD 025 mesylate, KD025 mesylate, KD-025 Mesylate, Rezurock Rezurock, SLx2119 mesylate, SLx-2119 mesylate, SLx-2119mesylate, SAR445761

Compound Identifiers

PubChem CID

146681181