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Oxfenicine is a small molecule inhibitor of carnitine palmitoyltransferase 1 (CPT1), specifically the CPT1b isoform. It acts as a prodrug that is transaminated to its active form, 4-hydroxyphenyl-glyoxylate, which competitively inhibits CPT1 by preventing the formation of acylcarnitine. This inhibition selectively reduces fatty acid oxidation in tissues expressing CPT1b, such as cardiac muscle. By inhibiting myocardial metabolism of nonesterified fatty acids (NEFA), oxfenicine has been investigated for potential use in conditions characterized by elevated fatty acid levels and obesity, including noninsulin-dependent diabetes mellitus and preclinical models of angina pectoris and ischemia[1][2][3][5].
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