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.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
---|---|---|---|---|---|
サンプルについてお問い合わせ | |||||
1 mg | 在庫あり | ¥ 8,500 | |||
2 mg | 在庫あり | ¥ 12,000 | |||
5 mg | 在庫あり | ¥ 19,500 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 33,500 |
説明 | 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. |
ターゲット&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]. |
別名 | A839977, A-839977 |
分子量 | 413.26 |
分子式 | 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), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
A 839977 870061-27-1 Membrane transporter/Ion channel Metabolism Neuroscience P2X Receptor Calcium Channel A839977 A-839977 Inhibitor inhibitor inhibit