store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AZD8797 (KAND567) 是一种可口服且具有选择性和有效性的人 CX3CR1 变构拮抗剂,对 CX3CR1 和 CXCR2 具有抑制作用,对SARS-CoV-2诱导的神经元损伤有潜在的保护作用,可防止癫痫发作后偏头痛模型大鼠痛觉过敏和小胶质细胞活化的恶化。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,090 | 现货 | ||
5 mg | ¥ 2,380 | 现货 | ||
10 mg | ¥ 3,970 | 现货 | ||
25 mg | ¥ 5,970 | 现货 | ||
50 mg | ¥ 7,880 | 现货 | ||
100 mg | ¥ 10,800 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,630 | 现货 |
产品描述 | 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. |
靶点活性 | [125I]-IL8-CXCR2:2800 nM (Ki, HEK293S cells), [125I]-CX3CL1-CX3CR1:3.9 nM (Ki, HEK293S cells), CX3CR1 (human):4 nM (Ki), CX3CR1:10 nM (human), B-lymphocyte cell lines:6 nM, CX3CR1 (rat):7 nM (Ki), CX3CR1:29 nM (Rat), CX3CR1:54 nM (mouse), WB (human):300 nM |
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. In a β-arrestin recruitment assay, AZD8797 positively modulates the CX3CL1 response 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). The potency is threefold lower for rat CX3CR1 (29 nM) and decreases even further at 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]. |
别名 | KAN-0440567, KAND567 |
分子量 | 403.56 |
分子式 | C19H25N5OS2 |
CAS No. | 911715-90-7 |
store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (247.79 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.4779 mL | 12.3897 mL | 24.7795 mL | 61.9487 mL |
5 mM | 0.4956 mL | 2.4779 mL | 4.9559 mL | 12.3897 mL | |
10 mM | 0.2478 mL | 1.239 mL | 2.4779 mL | 6.1949 mL | |
20 mM | 0.1239 mL | 0.6195 mL | 1.239 mL | 3.0974 mL | |
50 mM | 0.0496 mL | 0.2478 mL | 0.4956 mL | 1.239 mL | |
100 mM | 0.0248 mL | 0.1239 mL | 0.2478 mL | 0.6195 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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