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1781828-85-0

英文名稱 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 結(jié)構(gòu)式 1781828-85-0 結(jié)構(gòu)式

物理化學(xué)性質(zhì)

溶解度Soluble to 10 mM in DMSO with gentle warming

常見問題列表

生物活性
Ro 32-0432 hydrochloride 是一種有效的,選擇性的,ATP 競爭性和具有口服活性的 PKC 抑制劑,對 PKCα,PKCβI,PKCβII,PKCγ 和 PKCε 的 IC50 值分別為 9.3 nM,28 nM,30 nM,36.5 nM 和 108.3 nM。Ro 32-0432 hydrochloride 也是一種選擇性 GRK5 的抑制劑。Ro 32-0432 hydrochloride 可防止 T 細(xì)胞活化,并可用于慢性炎癥和自身免疫性疾病的研究。
靶點(diǎn)

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)

體外研究

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.

體內(nèi)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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