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Belumosudil (SLx-2119), also known as KD-025, is an orally bioavailable inhibitor of ROCK-II that is greater than 200-fold selective over ROCK-I (IC50s = 105 nM and 24 µM, respectively). SLx-2119 (40 µM) induces significant down-regulations of Tsp-1 and CTGF mRNA levels in PASMC.
In vivo, SLx-2119 (KD-025) (100, 200 or 300 mg/kg, orogastric gavage) dose-dependently reduces infarct volume after transient middle cerebral artery occlusion.
| Cell Experiment | |
|---|---|
| Cell lines | Cultured neurons and N2a cells |
| Preparation method | Cultured neurons and N2a cells were treated with belumosudil (KD025, 10 μmol/L) for 36–48 h, followed by immunofluorescence examination. |
| Concentrations | 10 μmol/L |
| Incubation time | 36–48 h |
| Animal Experiment | |
|---|---|
| Animal models | lentivirus-injected mice |
| Formulation | 0.5% CMC-Na |
| Dosages | 3 consecutive days at doses of 150 mg/kg, twice daily |
| Administration | orogastric gavage |
| Molecular Weight | 452.51 |
| Formula | C26H24N6O2 |
| CAS Number | 911417-87-3 |
| Solubility (25°C) | DMSO 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] Lee JH, et al. Ann Clin Transl Neurol. Selective ROCK2 Inhibition In Focal Cerebral Ischemia.
| Related ROCK Products |
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| Thiazovivin
Thiazovivin is a selective small molecule Rho-associated kinase (ROCK) inhibitor which significantly improves (200-fold) the efficiency of iPSC generation from human fibroblasts. |
| Fasudil hydrochloride
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| RKI-1447
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| GSK429286A
GSK429286A is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively. |
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