CAS: 266359-83-5; (R)-2-(4-Isobutylphenyl)-N-(Methylsulfonyl)Propanamide

该化合物是一种化学化合物,其特点是其作为化学受体CXCR2的选择性对抗者的作用.这种受体涉及各种煽动性过程,是慢性阻塞性肺病(COPD)和其他发炎性疾病等条件下进行治疗干预的目标.Repertaxin显示,它能够抑制化武与CXCR2的结合,从而调节炎情反应.该化合物的特点是其特定的分子结构,有助于其生物活动和选择性.在物理特性方面,Repertaxin通常在室内温度上作为固体,在有机溶剂中溶液溶性.其药性皮质特征包括吸收,分布,代谢和排泄等因素,这些因素对于其临床应用的功效和安全至关重要.

结构式图片

物理性质

MSDS等安全信息

欧盟法规

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    专利信息


    专利号:US-9333264-B2
    优先权日:2013-03-06
    标 题:Biocompatible polymeric nanoparticles degrade and release cargo in response to biologically relevant levels of hydrogen peroxide
    发明人：ALMUTAIRI ADAH; DE GRACIA LUX CAROLINE
    权利人:UNIV CALIFORNIA
    摘要:Disclosed are compositions and synthesis methods that pertain to biocompatible polymeric capsules capable of undergoing backbone degradation and cargo release upon exposure to biologically relevant concentrations of hydrogen peroxide (50-100 μM of H 2 O 2 ). In the invention, bio-responsive polyester bearing boronic ester triggers groups that degrade upon exposure to low concentrations of H 2 O 2 . The degradation is induced by transformation of a boronic ester to a phenol, which undergoes a quinone methide rearrangement to break down the polyester backbone.

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    主要参考文献


    1: Kim HY, Choi JH, Kang YJ, Park SY, Choi HC, Kim HS. Reparixin, an inhibitor of CXCR1 and CXCR2 receptor activation, attenuates blood pressure and hypertension-related mediators expression in spontaneously hypertensive rats. Biol Pharm Bull. 2011;34(1):120-7. doi: 10.1038/bjp.2008.270. Epub 2008 Jun 30.
    3: Gorio A, Madaschi L, Zadra G, Marfia G, Cavalieri B, Bertini R, Di Giulio AM. Reparixin, an inhibitor of CXCR2 function, attenuates inflammatory responses and promotes recovery of function after traumatic lesion to the spinal cord. J Pharmacol Exp Ther. 2007 Sep;322(3):973-81. Epub 2007 Jun 29.
    5: Leitner JM, Mayr FB, Firbas C, Spiel AO, Steinlechner B, Novellini R, Jilma B. Reparixin, a specific interleukin-8 inhibitor, has no effects on inflammation during endotoxemia. Int J Immunopathol Pharmacol. 2007 Jan-Mar;20(1):25-36.

    合成参考文献


    参考文献:10.1021/jm200371q
    摘要:Congreve M, Langmead CJ, Mason JS, Marshall FH. Progress in structure based drug design for G protein-coupled receptors. J Med Chem. 2011 Jul 14;54(13):4283–311.
    参考文献:10.1038/s41582-019-0217-x
    摘要:Vezzani A, Balosso S, Ravizza T. Neuroinflammatory pathways as treatment targets and biomarkers in epilepsy. Nat Rev Neurol. 2019 Aug;15(8):459–72. doi: 10.1038/s41582-019-0217-x.
    参考文献:10.1186/s13046-020-01666-z
    摘要:Zhao C, Wu M, Zeng N, Xiong M, Hu W, Lv W, Yi Y, Zhang Q, Wu Y. Cancer-associated adipocytes: emerging supporters in breast cancer. Journal of Experimental & Clinical Cancer Research. 2020 Aug 12;39(1):156. doi: 10.1186/s13046-020-01666-z.
    参考文献:10.1186/s12916-022-02248-w
    摘要:Zhang Y, Li N, Yuan G, Yao H, Zhang D, Li N, Zhang G, Sun Y, Wang W, Zeng J, Xu N, Liu M, Wu L. Upregulation of NOD1 and NOD2 contribute to cancer progression through the positive regulation of tumorigenicity and metastasis in human squamous cervical cancer. BMC Medicine. 2022 Feb 08;20(1):55. doi: 10.1186/s12916-022-02248-w.
    参考文献:10.1038/sj.bjp.0705862
    摘要:Souza DG, Bertini R, Vieira AT, Cunha FQ, Poole S, Allegretti M, Colotta F, Teixeira MM. Repertaxin, a novel inhibitor of rat CXCR2 function, inhibits inflammatory responses that follow intestinal ischaemia and reperfusion injury. British J Pharmacology. 2004 Sep;143(1):132–42. doi: 10.1038/sj.bjp.0705862.
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