| Bioactivity | AZD5904 is a selective and irreversible inhibitor of human Myeloperoxidase (MPO) with an IC50 of 140 nM and has similar potency in mouse and rat. | ||||||||||||
| Target | IC50: 140 nM (human MPO) | ||||||||||||
| Invitro | AZD5904 is a pselective and irreversible inhibitor of human Myeloperoxidase (MPO) with an IC50 of 140 nM and has similar potency in mouse and rat. It is 10 to 19-fold selective compare to the closely related lactoperoxidase and thyroid peroxidase; >70-fold to a broad panel of other enzymes, ion channels, and receptors. In isolated human neutrophils, 1 µM AZD5904 inhibits PMA stimulated HOCl by >90%[1]. | ||||||||||||
| Name | AZD5904 | ||||||||||||
| CAS | 618913-30-7 | ||||||||||||
| Formula | C10H12N4O2S | ||||||||||||
| Molar Mass | 252.29 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Myeloperoxidase (MPO) inhibitor. [2]. Tidén AK, Sjögren T, Svensson M, et al. 2-thioxanthines are mechanism-based inactivators of myeloperoxidase that block oxidative stress during inflammation. J Biol Chem. 2011;286(43):37578-37589. [3]. Chai W, Aylor K, Liu Z, Gan LM, Michaëlsson E, Barrett E. Inhibiting myeloperoxidase prevents onset and reverses established high-fat diet-induced microvascular insulin resistance. Am J Physiol Endocrinol Metab. 2019;317(6):E1063-E1069. [4]. Ramachandra CJA, Kp MMJ, Chua J, et al. Inhibiting cardiac myeloperoxidase alleviates the relaxation defect in hypertrophic cardiomyocytes. Cardiovasc Res. 2022;118(2):517-530. |