中文名 | AZD-5069 |
英文名 | N-(2-((2,3-difluorobenzyl)thio)-6-(((2R,3S)-3,4-dihydroxybutan-2-yl)oxy)pyrimidin-4-yl)azetidine-1-sulfonamide |
别名 | 化合物AZD-5069 N-(2-((2,3-二氟苄基)硫基)-6-(((2R,3S)-3,4-二羟基丁-2-基)氧基)嘧啶-4-基)氮杂环丁烷-1-磺酰胺 |
英文别名 | CS-2808 AZD5069 AZD 5069 AZD-5069 CPDD1543 AZD 5069 ACT-281959 878385-84-3 N-(2-((2,3-difluorobenzyl)thio)-6-(((2R,3S)-3,4-dihydroxybutan-2-yl)oxy)pyrimidin-4-yl)azetidine-1-sulfonamide 1-Azetidinesulfonamide, N-[2-[[(2,3-difluorophenyl)methyl]thio]-6-[(1R,2S)-2,3-dihydroxy-1-methylpropoxy]-4-pyrimidinyl]- |
CAS | 878385-84-3 |
化学式 | C18H22F2N4O5S2 |
分子量 | 476.52 |
密度 | 1.56±0.1 g/cm3(Predicted) |
熔点 | 149-152°C |
沸点 | 680.5±65.0 °C(Predicted) |
溶解度 | DMSO (微溶) 、甲醇 (微溶) |
酸度系数 | 4.56±0.20(Predicted) |
存储条件 | Hygroscopic, -20°C Freezer, Under inert atmosphere |
外观 | 固体 |
颜色 | White to Off-White |
靶点 | CXCR2 |
参考资料 展开查看 | 1: Uddin M, Watz H, Malmgren A, Pedersen F. NETopathic Inflammation in Chronic Obstructive Pulmonary Disease and Severe Asthma. Front Immunol. 2019 Feb 5;10:47. doi: 10.3389/fimmu.2019.00047. PMID: 30804927; PMCID: PMC6370641. 2: Cullberg M, Arfvidsson C, Larsson B, Malmgren A, Mitchell P, Wählby Hamrén U, Wray H. Pharmacokinetics of the Oral Selective CXCR2 Antagonist AZD5069: A Summary of Eight Phase I Studies in Healthy Volunteers. Drugs R D. 2018 Jun;18(2):149-159. doi: 10.1007/s40268-018-0236-x. PMID: 29856004; PMCID: PMC5995788. 3: De Soyza A, Pavord I, Elborn JS, Smith D, Wray H, Puu M, Larsson B, Stockley R. A randomised, placebo-controlled study of the CXCR2 antagonist AZD5069 in bronchiectasis. Eur Respir J. 2015 Oct;46(4):1021-32. doi: 10.1183/13993003.00148-2015. Epub 2015 Sep 4. PMID: 26341987. 4: Hickey MJ, Allen PH, Caffrey M, Hansen P, Kingston LP, Wilkinson DJ. Syntheses of a radiolabelled CXCR2 antagonist AZD5069 and its major human metabolite. J Labelled Comp Radiopharm. 2016 Sep;59(11):432-8. doi: 10.1002/jlcr.3429. Epub 2016 Jul 27. PMID: 27461061. 5: Watz H, Uddin M, Pedersen F, Kirsten A, Goldmann T, Stellmacher F, Groth E, Larsson B, Böttcher G, Malmgren A, Kraan M, Rabe KF. Effects of the CXCR2 antagonist AZD5069 on lung neutrophil recruitment in asthma. Pulm Pharmacol Ther. 2017 Aug;45:121-123. doi: 10.1016/j.pupt.2017.05.012. Epub 2017 May 23. PMID: 28549850. 6: Nicholls DJ, Wiley K, Dainty I, MacIntosh F, Phillips C, Gaw A, Mårdh CK. Pharmacological charact |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.099 ml | 10.493 ml | 20.986 ml |
5 mM | 0.42 ml | 2.099 ml | 4.197 ml |
10 mM | 0.21 ml | 1.049 ml | 2.099 ml |
5 mM | 0.042 ml | 0.21 ml | 0.42 ml |
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