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MK-571 is a potent, selective, and orally active small molecule that acts as a competitive antagonist and inverse agonist of the cysteinyl leukotriene receptor 1 (CysLT1), also known as the leukotriene D4 (LTD4) receptor. It exhibits high affinity for CysLT1 with Ki values in the low nanomolar range in both human and guinea pig lung membranes. In addition to its primary action on CysLT1, MK-571 is widely used as an inhibitor of multidrug resistance-associated proteins ABCC1 (MRP1) and ABCC4 (MRP4). Originally developed for its anti-inflammatory properties targeting leukotriene pathways, it has been extensively utilized in research settings to study allergic inflammation, pulmonary diseases, drug transport mechanisms, and more recently demonstrated antiviral activity against hepatitis C virus by antagonizing CysLT1[1][2][3][5][6].
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