计算溶液所需的质量、体积或浓度。
概述
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
规格
规格或纯度
≥98%
英文名称
JNJ-28583113
生化机理
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。
储存条件
-20°C储存
运输条件
超低温运输
作用类型
抑制剂
纯度
≥98%
名称和识别符
分子类型
小分子
分子量
366.38
高级数据
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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溶液计算器
常见问题
本产品的纯度是多少？
本产品的化学纯度（含量）为 ≥98%。批次的具体数值以分析证书（COA）为准。
本产品应如何储存？
请于?20 °C条件下保存。需冷冻保存以维持规定的有效期。
本产品如何运输？
本产品采用保温箱配冰袋运输。收货后请立即拆包，并按上述储存条件保存。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 2765255-93-2，分子式为 C19H21F3N2O2，分子量为 366.38 g/mol。
如何获取批次专用COA？
每个订单都会随附分析证书（COA），您也可以从账户订单历史中下载。如需订购前的COA，请联系您的客户代表，或使用PDP上的"申请COA"按钮——我们将提供代表性批次的COA。
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