Powder: -20°C for 3 years | In solvent: -80°C for 1 year
(S)-Ro 32-0432是一种高效、选择性的ATP竞争性PKC抑制剂,具备口服活性,对PKCα、PKCβI、PKCβII、PKCγ和PKCε的IC50值分别为9.3 nM、28 nM、30 nM、36.5 nM和108.3 nM。此外,(S)-Ro 32-0432也能选择性地抑制GRK5。它能够防止T细胞活化,适用于慢性炎症和自身免疫性疾病的研究。
产品描述 | (S)-Ro 32-0432 is a potent, selective inhibitor of protein kinase C (PKC) and G protein-coupled receptor kinase 5 (GRK5), demonstrating ATP-competitive and oral activity. It presents IC50 values of 9.3 nM for PKCα, 28 nM for PKCβI, 30 nM for PKCβII, 36.5 nM for PKCγ, and 108.3 nM for PKCε, showcasing its effectiveness against multiple PKC isoforms. Additionally, (S)-Ro 32-0432 inhibits T-cell activation, indicating its potential application in the research of chronic inflammatory and autoimmune diseases [1] [2]. |
体外活性 | (S)-Ro 32-0432 effectively suppresses interleukin-2 (IL-2) secretion, IL-2 receptor expression, and proliferation in human peripheral T-cells when activated with phorbol ester alongside phytohemagglutin or anti-CD3. However, it does not affect IL-2 induced proliferation in cells that have already been stimulated to express IL-2 receptors. Furthermore, this compound hinders the proliferation of the influenza peptide antigen HA 307-319-specific human T-cell clone (HA27) when these cells encounter antigen-presenting cells. Specifically, (S)-Ro 32-0432 demonstrates an inhibitory concentration (IC 50) of 0.15 μM [1], indicating its potency in blocking HA27 proliferation. |
体内活性 | Administration of (S)-Ro 32-0432 (10-50 mg/kg; oral; once; female AHH/R rats) effectively inhibits phorbol ester-induced edema, showcasing the compound's systemic efficacy in suppressing PKC-mediated responses. Additionally, this treatment hampers more physiological T-cell driven reactions, including host vs. graft responses and secondary paw swelling in adjuvant-induced arthritis [1]. |
别名 | Ro 32-0432 hydrochloride |
分子量 | 489.01 |
分子式 | C28H29ClN4O2 |
CAS No. | 1781828-85-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
(S)-Ro 32-0432 1781828-85-0 Others Ro 32-0432 hydrochloride Inhibitor inhibitor inhibit