| Name | AZD8797 |
| Description | 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. |
| In vitro | 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]. |
| In vivo | 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]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 100 mg/mL (247.79 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (9.91 mM), Sonication is recommended.
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| Keywords | CXCR2 | CX3CR1 | AZD-8797 | AZD8797 | AZD 8797 | 125I-IL-8-CXCR2 | [125I]-CX3CL1-CX3CR1 |
| Inhibitors Related | AZD8309 | rac-NBI-74330 | Delmetacin | Tannic acid | Artemotil | CXCR2-IN-1 | Soquelitinib | Plerixafor octahydrochloride | Tanimilast | 3-Indoleglyoxylic acid | Nicotinamide N-oxide | CXCL-CXCR1/2-IN-1 |
| Related Compound Libraries | Bioactive Compound Library | Cytokine Inhibitor Library | Membrane Protein-targeted Compound Library | Anti-Viral Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Orally Active Compound Library | Immuno-Oncology Compound Library | Immunology/Inflammation Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | GPCR Compound Library |
United States
