Belumosudil

Belumosudil (KD025) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 µM for ROCK2 and ROCK1, respectively.

Belumosudil (40 µM) elicits notable suppressions of Tsp-1 and CTGF mRNA concentrations in PASMC. Hybridization of the microarray with aRNA from HMVEC, following Belumosudil treatment, displays a quintuple increase in background compared to other arrays¹.

Administration of Belumosudil (KD-025; doses of 100, 200, or 300mg/kg, intraperitoneally) results in a dose-proportional diminution of infarct size post-transient middle cerebral artery obstruction. Moreover, Belumosudil demonstrates comparable effectiveness in aged, diabetic, or female mice to that observed in standard adult male subjects².

Administration of Belumosudil (KD-025; doses of 100, 200, or 300mg/kg, intraperitoneally) results in a dose-proportional diminution of infarct size post-transient middle cerebral artery obstruction. Moreover, Belumosudil demonstrates comparable effectiveness in aged, diabetic, or female mice to that observed in standard adult male subjects².

溶解方案(细胞实验)

DMSO 中的溶解度 : 23.33 mg/mL (51.56 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)|H₂O 中的溶解度 : < 0.1 mg/mL (insoluble)

溶解方案(动物实验)

"方案一": "请依序添加每种溶剂：10% DMSO 40% PEG300 5% Tween-80 45% SalineSolubility: ≥ 2.08 mg/mL (4.60 mM); 澄清溶液 此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。"

"方案一": "请依序添加每种溶剂：50% PEG300 50% SalineSolubility: 3.33 mg/mL (7.36 mM); 悬浊液; 超声助溶"