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JNJ16259685 {[allProObj[0].p_purity_real_show]}

货号：A854175

JNJ16259685 is a selective antagonist at the mGlu1 receptors, and inhibits the synaptic activation of mGlu1 in a concentration-dependent manner with IC50 of 19 nM.

JNJ16259685 化学结构 CAS号：409345-29-5
JNJ16259685 化学结构
CAS号：409345-29-5
JNJ16259685 3D分子结构
CAS号：409345-29-5
JNJ16259685 化学结构 CAS号：409345-29-5
JNJ16259685 3D分子结构 CAS号：409345-29-5
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JNJ16259685 纯度/质量文件 产品仅供科研

货号：A854175 标准纯度： {[allProObj[0].p_purity_real_show]}
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JNJ16259685 生物活性

描述 JNJ16259685 robustly and entirely suppresses the increase in intracellular Ca2+ levels triggered by glutamate (30 μM) at the rat mGlu1a receptor, with an IC50 of 3.24±1.00 nM. JNJ16259685 also impedes the glutamate-prompted elevation in intracellular Ca2+ levels at the rat mGlu5a receptor with an IC50 of 1.31±0.39 μM. Moreover, JNJ16259685 obstructs glutamate-induced Ca2+ mobilization at the human mGlu5 receptor with an IC50 of 28.3±11.7 μM. JNJ16259685 does not show any agonist activity at any of the group I mGlu receptors[1].

JNJ16259685 动物研究

Animal study Administered intraperitoneally, JNJ16259685 at doses of 0.25, 0.5, 1, 2, 4, and 8 mg/kg notably diminishes the duration of digging behaviors, as well as threat and attack behaviors, when compared to the vehicle group[2]. At a dosage of 30 mg/kg, JNJ16259685 has a negligible impact on locomotor activity. It significantly decreases rearing behavior, exploration in new environments, and lever pressing for food rewards (in rats at 0.3 mg/kg and in mice at 1 mg/kg). When administered subcutaneously at 30 mg/kg, JNJ16259685 does not affect the reflexive startle responses to loud sounds or foot shocks in mice[3].

JNJ16259685 参考文献

[1]Lavreysen H,et al. JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist. Neuropharmacology. 2004 Dec;47(7):961-72.

[2]Navarro JF,et al. JNJ16259685, a selective mGlu1 antagonist, suppresses isolation-induced aggression in male mice. Eur J Pharmacol. 2008 May 31;586(1-3):217-20.

[3]Hodgson RA, et al. Characterization of the selective mGluR1 antagonist, JNJ16259685, in rodent models of movement and coordination. Pharmacol Biochem Behav. 2011 Apr;98(2):181-7.

JNJ16259685 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.07mL

0.61mL

0.31mL

15.37mL

3.07mL

1.54mL

30.73mL

6.15mL

3.07mL

JNJ16259685 技术信息

CAS号409345-29-5
分子式C20H23NO3
分子量 325.401
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
溶解度

DMSO: 105 mg/mL(322.68 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: JNJ16259685 | 409345-29-5 | JNJ 16259685 | JNJ-16259685 | mGlu1 Receptor Antagonist | GPCR/G Protein | Neuronal Signaling | mGluR | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | JNJ16259685 纯度/质量文件 | JNJ16259685 生物活性 | JNJ16259685 参考文献 | JNJ16259685 实验方案 | JNJ16259685 技术信息

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