AZD8797

    
98%

AZD8797

源叶(MedMol)
S87198 一键复制产品信息
911715-90-7
C19H25N5OS2
403.5647
货号 规格 价格 上海 北京 武汉 南京 购买数量
S87198-1mg 98% ¥1090.00 9 - - -
S87198-5mg 98% ¥4100.00 货期:2-3天 - - -
S87198-10mg 98% ¥6900.00 货期:2-3天 - - -
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产品介绍

AZD8797 (KAND567) is an allosteric non-competitive and orally active antagonist of the human CX3CR1 receptor; antagonizes CX3CR1 and CXCR2 with Kis of 3.9 and 2800 nM, respectively

产品描述: AZD8797 (KAND567) is an allosteric non-competitive and orally active antagonist of the human CX3CR1 receptor; antagonizes CX3CR1 and CXCR2 with Kis of 3.9 and 2800 nM, respectively
靶点: CX3CR1:3.9 nM (Ki, 125I-CX3CL-CX3CR1 in HEK293S cells);125I-IL-8-CXCR2:2800 nM (Ki, in HEK293S cells);CXCR
体外研究: In a flow adhesion assay, AZD8797 antagonizes the natural ligand, fractalkine (CX3CL1), in both human whole blood (hWB) and in a B-lymphocyte cell line with IC50 values of 300 and 6 nM respectively. AZD8797 also prevents G-protein activation in a [35S]GTPγS accumulation assay. AZD8797 positively modulates the CX3CL1 response at sub-micromolar concentrations in a β-arrestin recruitment assay. In equilibrium saturation binding experiments, AZD8797 reduces the maximal binding of 125I-CX3CL1 without affecting Kd. AZD8797 binds selectively with high affinity 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).
体内研究: AZD8797 treatment in Dark Agouti rats with myelin oligodendrocyte glycoprotein-induced EAE results in reduced paralysis, CNS pathology, and incidence of relapses. The compound is effective when starting treatment before onset, as well as after the acute phase
参考文献: 1. Cederblad L, et al. AZD8797 is an allosteric non-competitive modulator of the human CX3CR1 receptor. Biochem J. 2016 Mar 1;473(5):641-9. 2. Ridderstad Wollberg A, et al. Pharmacological inhibition of the chemokine receptor CX3CR1 attenuates disease in a chronic-relapsing rat model for multiple sclerosis. Proc Natl Acad Sci U S A. 2014 Apr 8;111(14):5409-14. 3. Sofia Karlströ, et al. Substituted 7-amino-5-thio-thiazolo[4,5-d]pyrimidines as potent and selective antagonists of the fractalkine receptor (CX3CR1). J Med Chem. 2013 Apr 25;56(8):3177-90.
溶解性: Soluble  in  DMSO
保存条件: -20℃
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 2.478 ml 12.39 ml 24.779 ml
5 mM 0.496 ml 2.478 ml 4.956 ml
10 mM 0.248 ml 1.239 ml 2.478 ml
50 mM 0.05 ml 0.248 ml 0.496 ml
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