1428327-31-4|JNJ 47965567|CsnPharm

CAS No.: 1428327-31-4

JNJ-47965567 Catalog No. CSN19839

Synonyms: Jnj 47965567

JNJ 47965567 is a potent and selective P2X7 antagonist (pIC50 values are 8.3, 7.5 and 7.2 for human, mouse and rat receptors respectively).

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技术信息

生物活性

描述The purinergic receptor P2X, ligand-gated ion channel, 7 (P2X7) is an ATP-gated ion channel that plays an essential role in neuropsychiatry, neurodegeneration, and chronic pain. JNJ 47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist with high affinity binding at both the human (pKi=7.9±0.07) and rat (pKi=8.7±0.07) P2X7 ion channel. The potency (pIC50) of JNJ 47965567 to attenuate Bz-ATP-induced calcium flux at human, macaque, dog, rat, and mouse P2X7 was 8.3±0.08, 8.6±0.1, 8.5±0.2, 7.2±0.08, and 7.5±0.1, respectively. JNJ 47965567 reduced LPS primed BZ-ATP-induced IL-1β release with a pIC50 of 6.7±0.07 in human whole blood and a pIC50 of 7.5±0.07 in freshly isolated human monocytes from the blood. JNJ 47965567 also inhibited IL-18 release with a pIC50 value of 7.3 ± 0.1. JNJ-47965567 at a concentration of 100nM rapidly inhibited Bz-ATP-evoked currents in 1321N1 cells expressing hP2X7 (93.9% inhibition). Subcutaneous dosing of JNJ 47965567 at 100mg/kg significantly attenuated IL-1β release in rats challenged with Bz-ATP, a P2X7 agonist. In a rat model of neuropathic pain, subcutaneous administration of JNJ 47965567 at a dose of 30mg/kg resulted in a significant increase in tactile thresholds lasting from 30–60min post-administration^[3].
参考文献

[1] Bhattacharya A, Wang Q, et al. Pharmacological characterization of a novel centrally permeable P2X7 receptor antagonist: JNJ-47965567. Br J Pharmacol. 2013 Oct;170(3):624-40.
[2] Letavic MA, Lord B, et al. Synthesis and Pharmacological Characterization of Two Novel, Brain Penetrating P2X7 Antagonists. ACS Med Chem Lett. 2013 Mar 12;4(4):419-22.
[3] Bhattacharya A, Wang Q, Ao H, Shoblock JR, Lord B, Aluisio L, Fraser I, Nepomuceno D, Neff RA, Welty N, Lovenberg TW, Bonaventure P, Wickenden AD, Letavic MA. Pharmacological characterization of a novel centrally permeable P2X7 receptor antagonist: JNJ-47965567. Br J Pharmacol. 2013 Oct;170(3):624-40.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0465 mL
- 10.2324 mL
- 20.4648 mL
- 5 mM
- 0.4093 mL
- 2.0465 mL
- 4.0930 mL
- 10 mM
- 0.2046 mL
- 1.0232 mL
- 2.0465 mL

技术信息

CAS号

1428327-31-4

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H32N4O2S

运输

蓝冰

分子量

488.64

别名

Jnj 47965567

溶解度

DMSO	25.0 mg/mL (51.2 mM)

动物实验配方

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JNJ-47965567 Catalog No. CSN19839

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