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hDDAH-1-IN-1 (compound 8a) is a potent and selective non-amino acid catalytic site inhibitor of human dimethylarginine dimethylaminohydrolase-1 (hDDAH-1), with a Ki of 18 μM. DDAH mediates ADMA metabolism, thereby regulating nitric oxide production in a variety of disease states[1][2]. | [References]
[1] Tran CT, et al. The DDAH/ADMA/NOS pathway. Atheroscler Suppl. 2003 Dec;4(4):33-40. DOI:10.1016/s1567-5688(03)00032-1 [2] Lunk I, et al. Discovery of N-(4-Aminobutyl)-N'-(2-methoxyethyl)guanidine as the First Selective, Nonamino Acid, Catalytic Site Inhibitor of Human Dimethylarginine Dimethylaminohydrolase-1 (hDDAH-1). J Med Chem. 2019 Dec 31. DOI:10.1021/acs.jmedchem.9b01230 |
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