| Bioactivity | 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[1]. | ||||||||||||
| Invitro | JNJ-28583113 分别抑制不同物种中的 TRPM2，抑例如黑猩猩 (IC50=100 nM)、大鼠 (IC50=25 nM) 和人 (IC50=126 nM)[1]。JNJ-28583113 (3 nM、30 nM 和 1 μM；200 秒) 在 hTRPM2-HEK 诱导细胞中记录的 ADPR 诱导电流中表现出电物理特性[1]。JNJ-28583113 (10 μM；1 小时）防止细胞因 H2O2 诱导的细胞死亡，最高处理条件为 1mM H2O2。JNJ-28583113 (10 μM；1 小时) 还保护 HeLa 细胞免受 H2O2 (10 μM；1 小时) 诱导的形态变化[1]。 Western Blot Analysis[1] Cell Line: | ||||||||||||
| In Vivo | JNJ-28583113 (10 mg/kg，2 ml/kg；sc；单剂量) 具有脑穿透性，在脑室中可达 400 ng/mL[1]。 Animal Model: | ||||||||||||
| Name | JNJ-28583113 | ||||||||||||
| CAS | 2765255-93-2 | ||||||||||||
| Formula | C19H21F3N2O2 | ||||||||||||
| Molar Mass | 366.38 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Fourgeaud L, et al. Pharmacology of JNJ-28583113: A novel TRPM2 antagonist. Eur J Pharmacol. 2019 Jun 15;853:299-307. |
JNJ-28583113
CAS: 2765255-93-2 F: C19H21F3N2O2 W: 366.38
JNJ-28583113 is an TRPM2 antagonist with brain permeability. JNJ-28583113 inhibits TRPM2 blocked phosphorylation of GSK3
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