store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
A 839977 is a selective P2X7 receptor antagonist with anti-inflammatory and analgesic activity that inhibits BzATP-induced calcium efflux from the P2X7 receptor for the study of renal fibrosis.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
2 mg | In stock | $ 63.00 | |
5 mg | In stock | $ 102.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 158.00 |
Description | A 839977 is a selective P2X7 receptor antagonist with anti-inflammatory and analgesic activity that inhibits BzATP-induced calcium efflux from the P2X7 receptor for the study of renal fibrosis. |
Targets&IC50 | P2X7 receptor:150 nM (Mouse), P2X7 receptor:42 nM (Rat), P2X7 receptor:20 nM (Human) |
In vitro |
A 839977 selectively blocks BzATP-evoked calcium influx at mammalian P2X7 receptors (IC50=20-150 nM). A 839977 inhibits agonist-evoked YO-PRO uptake and IL-1beta release from differentiated human THP-1 cells. Furthermore, A 839977 has demonstrated efficacy in reducing inflammatory and neuropathic pain in animal models[1]. In optic nerve astrocytes, pre-treatment with A 839977 (50 nM for 1 hour) significantly prevents the pressure-induced rise of IL-1β priming[3]. |
In vivo | In rats, A 839977 (30 μmol/kg, 100 μmol/kg, 300 μmol/kg; pre-injected 30 mins) dose-dependently reduces thermal hyperalgesia induced by intraplantar administration of complete Freund's adjuvant (CFA)[1].In the CFA model of inflammatory pain in wild-type mice, A 839977 (10 μmol/kg, 30 μmol/kg, 100 μmol/kg; pre-injected 30 mins) elicits robust antihyperalgesia, while it shows no effect in IL-1alphabeta knockout mice[1].Furthermore, A 839977 attenuates dorsal horn neuronal responses in cancer-bearing animals[2]. |
Synonyms | A839977, A-839977 |
Molecular Weight | 413.26 |
Formula | C19H14Cl2N6O |
CAS No. | 870061-27-1 |
store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 80 mg/mL (193.58 mM), Sonification is recommended.
You can also refer to dose conversion for different animals. More
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A 839977 870061-27-1 Membrane transporter/Ion channel Metabolism Neuroscience P2X Receptor Calcium Channel A839977 A-839977 inhibitor inhibit