化合物 (S)-RO 32-0432
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- CAS號(hào):
- 1781828-85-0
- 英文名:
- Ro 32-0432 hydrochloride
- 英文別名:
- (S)-Ro 32-0432
- 中文名:
- 化合物 (S)-RO 32-0432
- 中文別名:
- 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化學(xué)性質(zhì)
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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性質(zhì)、用途與生產(chǎn)工藝
Ro 32-0432 hydrochloride 是一種有效的,選擇性的,ATP 競(jìng)爭(zhēng)性和具有口服活性的 PKC 抑制劑,對(duì) 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。
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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
上下游產(chǎn)品信息
上游原料
下游產(chǎn)品
| 更新日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS編號(hào) | 包裝 | 價(jià)格 |
|---|
| 2026/06/05 | HY-108601A | 化合物 (S)-RO 32-0432 (S)-Ro 32-0432 | 1781828-85-0 | 1 mg | 6960元 |
化合物 (S)-RO 32-0432
生產(chǎn)廠家
1781828-85-0, 化合物 (S)-RO 32-0432 相關(guān)搜索:
- 抑制劑
- 化合物 (S)-RO 32-0432
- 1781828-85-0
- (S)-Ro 32-0432