Product Details
| Product Name:
AZD8797 |
CAS No.:
911715-90-7 |
| Purity:
99.68% |
Supply Ability:
10g |
| Release date:
2024/11/18 |
Product Introduction
Bioactivity
| 名稱 | 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. |
| 體外活性 | 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]. |
| 體內(nèi)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]. |
| 存儲(chǔ)條件 | 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)
|
| 關(guān)鍵字 | AZD 8797 | AZD8797 | AZD-8797 |
| 相關(guān)產(chǎn)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 |
| 相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 膜蛋白靶向化合物庫(kù) | 藥物功能重定位化合物庫(kù) | 已知活性化合物庫(kù) | GPCR靶點(diǎn)分子庫(kù) |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$83.00/1mg |
VIP3Y
|
TargetMol Chemicals Inc.
|
2024-11-18 |
United States