JNJ-28583113
规格
| Cas Number | 2765255-93-2 |
| 规格或纯度 | ≥98% |
| 纯度 | ≥98% |
| 包装 | 50mg 或 10mg 或 5mg 或 25mg |
产品信息
| 品牌 | 阿拉丁 |
| 过滤标签 | TRP Channel,神经元信号传导,膜转运器/离子通道 |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | JNJ-28583113 是一种具有脑渗透性的 TRPM2 拮抗剂。JNJ-28583113 可抑制 TRPM2 阻断的 GSK3α 和 β 亚基的磷酸化。JNJ-28583113 保护细胞免受氧化应激诱导的细胞死亡。JNJ-28583113 还能抑制细胞因子 i 的释放。 |
| 英文描述 |
JNJ-28583113 is an TRPM2 antagonist with brain permeability. JNJ-28583113 inhibits TRPM2 blocked phosphorylation of GSK3α and β subunits. JNJ-28583113 protects cells from oxidative stress induced cell death. JNJ-28583113 also suppresses cytokine release in response to pro-inflammatory stimuli in microglia In Vitro JNJ-28583113 inhibits TRPM2 in cells overexpressing chimpanzee (IC 50 =100 nM), rat (IC 50 =25 nM), and human (IC 50 =126 nM), respectively. JNJ-28583113 (3 nM, 30 nM, and 1 μM; 200 s) exhibits electrophysical characterization in ADPR-induced currents recorded in hTRPM2-HEK-inducible cells. JNJ-28583113 (10 μM; 1 h) prevents cells from H 2 O 2 induced cell death up to 1 mM of H 2 O 2 . JNJ-28583113 (10 μM; 1 h) also protects HeLa cells from H 2 O 2 (10 μM; 1 h) induced morphological changes. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: hTRPM2-HEK cells Concentration: 10 μM Incubation Time: 30 min Result: Recovered phosphorylation of GSK3α and β subunits which inhibited by H 2 O 2 (300 μM; 10 min). In Vivo JNJ-28583113 (10 mg/kg, 2 ml/kg; sc; single dose) is brain penetrant, and achieves 400 ng/mL in the brain compartment . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Harlan Sprague Dawley Rats (400 g) Dosage: 10 mg/kg, 2 mL/kg Administration: SC; sampled at 0.5, 2, or 6 h post dosing Result: Quickly metabolized in the plasma, while it showed high levels in plasma and low levels in the brain. Form:Solid IC50& Target:TRPM2 |