| 名称 | AZD8797 |
| 描述 | AZD8797 (KAND567) is an orally available, selective and potent human CX3CR1-converting antagonist with inhibitory effects on CX3CR1 and CXCR2, and potentially protects against SARS-CoV-2-induced neuronal damage, preventing worsening of nociceptive sensitization and microglial activation in a migraine model of rats following seizures. |
| 体外活性 | In a flow adhesion assay, AZD8797, with IC50 values of 300 nM in human whole blood (hWB) and 6 nM in a B-lymphocyte cell line, antagonizes the natural ligand fractalkine (CX3CL1). AZD8797 also prevents G-protein activation in a [35S]GTPγS accumulation assay and positively modulates the CX3CL1 response in a β-arrestin recruitment assay at sub-micromolar concentrations. In equilibrium saturation binding experiments, AZD8797 reduces the maximal binding of 125I-CX3CL1 without affecting Kd[1]. AZD8797 selectively and with high affinity binds to human and rat CX3CR1 (Ki of hCX3CR1, 4 nM; Ki of rCX3CR1, 7 nM, respectively). The equilibrium dissociation constant, KB, demonstrates that AZD8797 is a very potent inhibitor for human CX3CR1 (10 nM), with reduced potency for rat CX3CR1 (29 nM) and even lower for mouse CX3CR1 (54 nM)[3]. |
| 体内活性 | Treatment with AZD8797 in Dark Agouti rats with myelin oligodendrocyte glycoprotein-induced EAE results in reduced paralysis, CNS pathology, and incidence of relapses. The compound is effective both when starting treatment before onset and after the acute phase[3]. |
| 存储条件 | store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 100 mg/mL (247.79 mM)
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| 关键字 | AZD 8797 | AZD8797 | AZD-8797 |
| 相关产品 | AZD8309 | rac-NBI-74330 | Delmetacin | Tannic acid | Artemotil | CXCR2-IN-1 | LIT927 | Reparixin | Plerixafor octahydrochloride | Nicotinamide N-oxide | Plerixafor | CXCL-CXCR1/2-IN-1 |
| 相关库 | 经典已知活性库 | 膜蛋白靶向化合物库 | 药物功能重定位化合物库 | 已知活性化合物库 | GPCR靶点分子库 |
United States
