AZD-5069 is a potent and selective CXCR2 antagonist with the potential to inhibit neutrophil migration into the airways in patients with COPD. AZD-5069 was shown to inhibit binding of radiolabeled CXCL8 to human CXCR2 with a pIC50 value of 9.1. Furthermore, AZD5069 inhibited neutrophil chemotaxis, with a pA2 of approximately 9.6, and adhesion molecule expression, with a pA2 of 6.9, in response to CXCL1. AZD5069 was a slowly reversible antagonist of CXCR2 with effects of time and temperature evident on the pharmacology and binding kinetics. AZD-5069 is also potential useful for patient in inflammatory conditions.
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名称 | AZD-5069 |
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Iupac 化学名称 | N-(2-((2,3-difluorobenzyl)thio)-6-(((2R,3S)-3,4-dihydroxybutan-2-yl)oxy)pyrimidin-4-yl)azetidine-1-sulfonamide |
同义词 | AZD 5069 ; AZD5069 |
英文同义词 | AZD 5069 ; AZD5069 |
分子式 | C18H22F2N4O5S2 |
分子量 | 476.51 |
Smile | O=S(N1CCC1)(NC2=NC(SCC3=CC=CC(F)=C3F)=NC(O[C@@H]([C@@H](O)CO)C)=C2)=O |
InChiKey | QZECRCLSIGFCIO-RISCZKNCSA-N |
InChi | InChI=1S/C18H22F2N4O5S2/c1-11(14(26)9-25)29-16-8-15(23-31(27,28)24-6-3-7-24)21-18(22-16)30-10-12-4-2-5-13(19)17(12)20/h2,4-5,8,11,14,25-26H,3,6-7,9-10H2,1H3,(H,21,22,23)/t11-,14+/m1/s1 |
Cas号 | 878385-84-3 |
相关CAS号 | 878385-84-3 |
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