Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Belumosudil (Rezurock) 是一种选择性的ROCK2抑制剂,对 ROCK1 和 ROCK2 的IC50值分别为 24 µM 和 105 nM,具有抗纤维化作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 293 | 现货 | ||
2 mg | ¥ 416 | 现货 | ||
5 mg | ¥ 697 | 现货 | ||
10 mg | ¥ 947 | 现货 | ||
25 mg | ¥ 1,720 | 现货 | ||
50 mg | ¥ 2,890 | 现货 | ||
100 mg | ¥ 4,280 | 现货 | ||
500 mg | ¥ 9,270 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 798 | 现货 |
产品描述 | Belumosudil (Rezurock) is an orally available, and specific ROCK2 inhibitor (IC50/Ki: 60/41 nM). |
靶点活性 | ROCK2:41 nM(Ki), ROCK2:60 nM |
体外活性 | KD025 down-regulates the IL-17 and IL-21 secretion in human PBMCs, and leads to down-regulation of STAT3 phosphorylation, IRF4, and RORγt expression in CD4+ T cells. [2] KD025 inhibits the secretion of IL-21, IL-17, and IFNγ along with decreasing phosphorylated STAT3 and reduced protein expression of IRF4 and BCL6 in human peripheral blood mononuclear cells. [3] |
体内活性 | In mice, KD025 (200 mg/kg, p.o.) inhibits ROCK activity in brain and heart, as measured by the degree of MYPT1 phosphorylation. KD025 (200 mg/kg, p.o.) significantly reduces the area of perfusion defect, and reduces tissue loss in the ipsilateral hemisphere. [1] In a collagen-induced arthritis (CIA) mouse model, KD025 (200 mg/kg, i.p.) downregulates the progression of collagen-induced arthritis via targeting of the Th17-mediated pathway. [2] KD025 ()150 mg/kg, i.p. or p.o.) effectively ameliorates cGVHD in a full MHC-mismatch model of multi-organ system cGVHD with bronchiolitis obliterans syndrome and a minor MHC-mismatch model of sclerodermatous GVHD. [3] |
激酶实验 | Cell-free enzyme assays are performed to determine the selective inhibition of ROCK1 and ROCK2 by SLx-2119. Reactions are performed on non-binding surface microplates. Four mU of human ROCK1 and ROCK2 are used to phosphorylate 30 μM of the synthetic ROCK peptide substrate S6 Long, prepared at American Peptide with the addition of 10 μM ATP, containing?33P-ATP in the presence of 10 mM Mg2+, 50 mM Tris, pH 7.5, 0.1 mM EGTA and 1 mM DTT at room temperature. One unit is the amount of kinase needed to catalyze the transfer of 1 nmol phosphate/min to the peptide. The reactions are allowed to proceed for 45 minutes and then stopped with 3% phosphoric acid to a final concentration of 1%. The reactions are captured on phospho cellulose filtration microplates and washed with 75 mM phosphoric acid and methanol using a vacuum manifold. Phosphorylation is measured on a Perkin-Elmer MicroBeta 1450. |
细胞实验 | SLx-2119 is dissolved in DMSO to obtain a stock solution of 20 mM. Western blots are used to determine whether HMVEC, NHDF and PASMC express ROCK1 and ROCK2. The cells are incubated for 24 hours in 3 mL culture media containing SLx-2119. All cells are collected at passage 3 and lysed on ice in 25 mM Tris-HCl pH 7.5, 150 mM NaCl, 0.5% tritonX-100, 10% glycerol, 10 mM NaF and a protease inhibitor cocktail. Protein concentration is determined using a BCA protein assay reagent. Cell lysates (35 μg) are separated on 7.5% or 12.5% SDS-PAGE polyacrylamide gels and transferred to PVDF membrane filters. Membranes are blocked in 5% non-fat milk in TBS containing 0.1% Tween 20. Blots are probed with antibodies to ROCK1, ROCK2 or actin and washed well before incubation with HRP-conjugated secondary antibodies and visualization with an enhanced chemiluminescence (ECL) kit. |
别名 | KD025, Rezurock, ROCK inhibitor, SLx-2119 |
分子量 | 452.51 |
分子式 | C26H24N6O2 |
CAS No. | 911417-87-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 83 mg/mL (183.4 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2099 mL | 11.0495 mL | 22.099 mL | 55.2474 mL |
5 mM | 0.442 mL | 2.2099 mL | 4.4198 mL | 11.0495 mL | |
10 mM | 0.221 mL | 1.1049 mL | 2.2099 mL | 5.5247 mL | |
20 mM | 0.1105 mL | 0.5525 mL | 1.1049 mL | 2.7624 mL | |
50 mM | 0.0442 mL | 0.221 mL | 0.442 mL | 1.1049 mL | |
100 mM | 0.0221 mL | 0.1105 mL | 0.221 mL | 0.5525 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Belumosudil 911417-87-3 Cell Cycle/Checkpoint Cytoskeletal Signaling Stem Cells ROCK inhibit KD 025 Rho-kinase Rho-associated protein kinase ROCK2 KD025 Anti-fibrotic SLx 2119 ROK Rezurock ROCK inhibitor SLx2119 SLx-2119 Rho-associated kinase KD-025 Inhibitor inhibitor