A 839977

Research use only, not for human use.

A-839977 is a selective P2X7 receptor antagonist with anti-inflammatory and analgesic properties, inhibiting BzATP-induced calcium efflux from the P2X7 receptor, and is used in the study of renal fibrosis.

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 : 100 mg/mL (241.98 mM; Ultrasonic )

Clc1cccc(c1Cl)-n1nnnc1NCc1ccccc1Oc1ccccn1

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(-20℃)

With Ice Pack

≥ 2 years