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1781828-85-0

中文名称 化合物 (S)-RO 32-0432
英文名称 Ro 32-0432 hydrochloride
CAS 1781828-85-0
分子式 C28H29ClN4O2
分子量 489.02
MOL 文件 1781828-85-0.mol
1781828-85-0 结构式 1781828-85-0 结构式

基本信息

中文别名
化合物 (S)-RO 32-0432

物理化学性质

溶解度Soluble to 10 mM in DMSO with gentle warming
化合物 (S)-RO 32-0432价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2025/05/22HY-108601A化合物 (S)-RO 32-0432
(S)-Ro 32-0432
1781828-85-01 mg5940元

常见问题列表

生物活性
Ro 32-0432 hydrochloride 是一种有效的,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 9.3 nM,28 nM,30 nM,36.5 nM 和 108.3 nM。Ro 32-0432 hydrochloride 也是一种选择性 GRK5 的抑制剂。Ro 32-0432 hydrochloride 可防止 T 细胞活化,并可用于慢性炎症和自身免疫性疾病的研究。
靶点

PKCα

9.3 nM (IC 50 )

PKC-βI

28 nM (IC 50 )

PKC-βII

30 nM (IC 50 )

PKCγ

36.5 nM (IC 50 )

PKCε

108.3 nM (IC 50 )

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 IC 50 of 0.15 μM.

体内研究

Ro 32-0432 (10-50 mg/kg; oral administration; once; female AHH/R rats) treatment inhibits subsequent phorbol ester-induced 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 adjuvant-induced arthritis are also inhibited by Ro 32-0432.

Animal Model: Female AHH/R rats (200-250 g) induced with phorbol ester
Dosage: 10 mg/kg, 30 mg/kg, 50 mg/kg
Administration: Oral administration; once
Result: Inhibited subsequent phorbol ester-induced edema in rats.
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