AZD2098 - CCR 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAZD2098Cat. No.: HY-U00064CAS No.: 566203-88-1分式: CHClNOS分量: 334.18作靶点: CCR作通路: GPCR/G Protein; Immunology/Inflammation储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (299.24 mM;

2、Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.48 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.48 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 AZD2098种有效、选择性的 CCR4 抑制剂，作于类、狗的 CCR4 pIC50s

3、值分别为 7.8、8.0、8.0、7.6，可于治疗哮喘研究 1 2。IC50 & Target CCR4体外研究 AZD2098 potently inhibits chemokine-induced cellular responses, with pIC50 of 7.5 and 6.3 against CCL22-induced Ca2+ influx in hCCR4-expressing CHO cells and CCL17- or CCL22-induced chemotaxis of primaryhuman Th2 cells respectively 1.体内研究 AZD2

4、098 (0.22-7.5 mol/kg; p.o.; 1 hour before and every 12 hours after antigen challenge) exhibits efficacyagainst antigen-induced inflammatory response among ovalbumin-sensitized rats, and the changes are firstvisible at a dose of 0.22 mol/kg and maximal at 7.5 mol/kg 1.Animal Model: Brown-Norway rats

5、1Dosage: 0.22 mol/kg, 0.75 mol/kg, 2.2 mol/kg, 3.0 mol/kg,7.5 mol/kg, 15 mol/kgAdministration: Oral administration; 1 hour before and every 12 hours after antigen challengeResult: Exhibits efficacy against antigen-induced inflammatory response among ovalbumin-sensitized rats.REFERENCES1. Kindon N, e

6、t al. Discovery of AZD-2098 and AZD-1678, Two Potent and Bioavailable CCR4 Receptor Antagonists. ACS Med Chem Lett.2017 Sep 1;8(9):981-986.2. Asher Mullard. Cancer charity sees success re-prioritizing industrys shelved compounds. Nat Rev Drug Discov. 2014 May;13(5):319-21.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400