| 名称 | A 839977 |
| 描述 | 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. |
| 体外活性 | A 839977 selectively blocks BzATP-evoked calcium influx at mammalian P2X7 receptors (IC50=20-150 nM) and inhibits agonist-evoked YO-PRO uptake and IL-1beta release from differentiated human THP-1 cells. It has demonstrated efficacy in reducing inflammatory and neuropathic pain in animal models[1]. Pre-treatment with A 839977 (50 nM for 1 hour) significantly prevents the pressure-induced rise of IL-1β priming in optic nerve astrocytes[3]. |
| 体内活性 | 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]. |
| 存储条件 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 80 mg/mL (193.58 mM), Sonication is recommended.
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| 关键字 | A 839977 |
| 相关产品 | Nisoldipine | Nimodipine | 2,5-Di-tert-butylhydroquinone | Diltiazem hydrochloride | Levetiracetam | L-Ascorbic acid | Lanthanum(III) chloride heptahydrate | Butamben | Ethyl cinnamate | 1-Octanol | 1,2,4-Trihydroxybenzene | Otilonium bromide |
| 相关库 | 经典已知活性库 | 疼痛相关化合物库 | 膜蛋白靶向化合物库 | 抗衰老化合物库 | 已知活性化合物库 | 离子通道库 |
United States
