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编 号：F213796
分子式：C28H29ClN4O2
分子量：489.01
分子式：C28H29ClN4O2
分子量：489.01
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CAS No: 1781828-85-0
产品详情
生物活性：
(S)-Ro 32-0432 is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of (S)-Ro 32-0432 for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. (S)-Ro 32-0432 is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. (S)-Ro 32-0432 prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research.
体内研究：
(S)-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.
体外研究：
(S)-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 (S)-Ro 32-0432. (S)-Ro 32-0432 inhibits HA27 proliferation with an IC50 of 0.15 μM.
(S)-Ro 32-0432 is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of (S)-Ro 32-0432 for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. (S)-Ro 32-0432 is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. (S)-Ro 32-0432 prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research.
体内研究：
(S)-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.
体外研究：
(S)-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 (S)-Ro 32-0432. (S)-Ro 32-0432 inhibits HA27 proliferation with an IC50 of 0.15 μM.
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