化合物 (S)-RO 32-0432
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- CAS号:
- 1781828-85-0
- 英文名:
- Ro 32-0432 hydrochloride
- 英文别名:
- (S)-Ro 32-0432
- 中文名:
- 化合物 (S)-RO 32-0432
- 中文别名:
- 化合物 (S)-RO 32-0432
- CBNumber:
- CB78326130
- 分子式:
- C28H29ClN4O2
- 分子量:
- 489.02
- MOL File:
- 1781828-85-0.mol
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化合物 (S)-RO 32-0432化学性质
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溶解度:
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Soluble to 10 mM in DMSO with gentle warming
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化合物 (S)-RO 32-0432性质、用途与生产工艺
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。
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PKCα
9.3 nM (IC
50
)
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PKC-βI
28 nM (IC
50
)
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PKC-βII
30 nM (IC
50
)
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PKCγ
36.5 nM (IC
50
)
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PKCε
108.3 nM (IC
50
)
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G protein-coupled receptor kinase 5 (GRK5)
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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.
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.
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Animal Model:
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Female AHH/R rats (200-250 g) induced with phorbol ester
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Dosage:
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10 mg/kg, 30 mg/kg, 50 mg/kg
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Administration:
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Oral administration; once
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Result:
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Inhibited subsequent phorbol ester-induced edema in rats.
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化合物 (S)-RO 32-0432
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| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2025/05/22 | HY-108601A | 化合物 (S)-RO 32-0432
(S)-Ro 32-0432 | 1781828-85-0 | 1 mg | 5940元 |
1781828-85-0, 化合物 (S)-RO 32-0432 相关搜索:
- 抑制剂
- 化合物 (S)-RO 32-0432
- 1781828-85-0
- (S)-Ro 32-0432