A 839977

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

A 839977是一种选择性 P2X7 受体拮抗剂, 可阻断人和大小鼠 P2X7 受体的 BzATP 诱发的钙内流 (IC50s=20 nM, 42 nM / 150 nM); 在体实验中, 通过阻断 IL-1β 释放产生抗痛觉过敏反应, 减弱模型动物的炎症反应与神经性疼痛.

A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockadeare mediated by blocking the release of IL-1beta.

A 839977 selectively blocks BzATP-evoked calcium influx at mammalian P2X7 receptors, (IC50=20-150 nM), which blocks agonist-evoked YO-PRO uptake and IL-1beta release from differentiated human THP-1 cells, it has been shown to reduce inflammatory and neuropathic pain in animal models.A 839977 (50 nM, pre-treatment 1 hour) significantly prevents pressure-induced rise of IL-1β priming in optic nerve astrocytes.RT-PCR Cell Line:Optic nerve astrocyte cells Concentration:50 nM Incubation Time:1 hour(pre-treatment) Result:Prevented the IL-1β priming in astrocyte cells

A 839977 (30 μmol/kg, 100 μmol/kg, 300 μmol/kg; pre-injected 30mins) dose-dependently reduces thermal hyperalgesia produced by intraplantar administration of complete Freund's adjuvant (CFA) in rats.A 839977 (10 μmol/kg, 30 μmol/kg, 100 μmol/kg; pre-injected 30mins) produces robust antihyperalgesia in the CFA model of inflammatory pain in wild-type mice, but it has no effect on IL-1alphabeta knockout mice.A 839977 attenuates dorsal horn neuronal responses in cancer bearing animals.Animal Model:Male Sprague-Dawley, BALB/c mice and IL-1 (?/?) mice for CFA-induced chronic inflammatory Dosage:30 μmol/kg, 100 μmol/kg, 300 μmol/kg (rat); 10 μmol/kg, 30 μmol/kg, 100 μmol/kg (mice)Administration:Injection; pre-injected 30mins Result:Attenuated CFA-induced thermal hyperalgesia in a dose-related manner in rat and mice, but has no effect on IL-1 (?/?) mice.

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GPCR/G Protein

Calcium Channel

Calcium Channel | P2X Receptor

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870061-27-1

413.26

C19H14Cl2N6O

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (241.98 mM; 超声助溶 )

Clc1cccc(c1Cl)-n1nnnc1NCc1ccccc1Oc1ccccn1

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(-20℃)

With Ice Pack

≥ 2 years