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Ro 32-0432 hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Ro 32-0432 hydrochloride图片
CAS NO:1781828-85-0
包装:1mg
市场价:8500元

产品介绍
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PKCαPKCβIPKCβIIPKCγPKCεIC50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。
生物活性

Ro 32-0432 hydrochloride is a potent, selective, ATP-competitive and orally activePKCinhibitor. TheIC50values of Ro 32-0432 hydrochloride forPKCα,PKCβI,PKCβII,PKCγandPKCεare 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. Ro 32-0432 hydrochloride is also a selectiveG protein-coupled receptor kinase5 (GRK5)inhibitor. Ro 32-0432 hydrochloride prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research[1][2].

IC50& Target[1][2]

PKCα

9.3 nM (IC50)

PKC-βI

28 nM (IC50)

PKC-βII

30 nM (IC50)

PKCγ

36.5 nM (IC50)

PKCε

108.3 nM (IC50)

G protein-coupled receptor kinase 5 (GRK5)

 

体外研究
(In Vitro)

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 IC50of 0.15 μM[1].

体内研究
(In Vivo)

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[1].

Animal Model:Female AHH/R rats (200-250 g) induced with phorbol ester[1]
Dosage:10 mg/kg, 30 mg/kg, 50 mg/kg
Administration:Oral administration; once
Result:Inhibited subsequent phorbol ester-induced edema in rats.
分子量

489.01

Formula

C28H29ClN4O2

CAS 号

1781828-85-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.