Ro 32-0432 hydrochloride  

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包装规格:1mg in glass bottle
产品描述:基本信息 产品编号:R10289  产品名称:Ro 32-0432 hydrochloride CAS: 1781828-85-0   储存条件 粉末 -20℃ 四年 分子式: C28H28N4O2?HCl 溶于液体 -80℃ 六个月 分子量: 452.55     化学名:      Solubility (25°C)   体外 DMSO   Ethanol   Water   体内(现配现用)     <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。   生物活性 产品描述 一种有效的,选择性的,ATP 竞争性和具有口服活性的 PKC 抑制剂,对 PKCα,PKCβI,PKCβII,PKCγ 和 PKCε 的 IC50 值分别为 9.3nM,28nM,30nM,36.5nM 和 108.3nM。Ro 32-0432 hydrochloride 也是一种选择性 GRK5 的抑制剂。 靶点/IC50 PKCα 9.3nM (IC50) PKC-βI 28nM (IC50) PKC-βII 30nM (IC50) PKCγ 36.5nM (IC50) PKCε 108.3nM (IC50) G protein-coupled receptor kinase 5 (GRK5)       体外研究 Ro 32-0432 inhibits interleukin-2 (IL-2) secretion, IL-2 receptor expression in, and proliferation of, peripheral human T-cells stimulated with phorbol ester together with phytohemagglutin or anti-CD3, but does not inhibit IL-2 induced proliferation in cells already stimulated to express IL-2 receptors. Proliferation of the influenza peptide antigen HA 307-319-specific human T-cell clone (HA27) after exposure to antigen-pulsed autologous presenting cells is also inhibited by Ro 32-0432. Ro 32-0432 inhibits HA27 proliferation with an IC50 of 0.15μM. 体内研究 Ro 32-0432 (10-50mg/kg; oral administration; once; female AHH/R rats) treatment inhibits subsequent phorbol esterinduced edema in rats demonstrating the systemic efficacy of the compound to inhibit PKC-driven responses. Induction of more physiologically T-cell driven responses such as host vs. graft responses and the secondary paw swelling in adjuvantinduced arthritis are also inhibited by Ro 32-0432. Animal Model: Female AHH/R rats (200-250g) induced with phorbol ester Dosage: 10mg/kg,30mg/kg,50mg/kg Administration: Oral administration; once Result: Inhibited subsequent phorbol ester-induced edema in rats.
保存条件:-20℃