Phloretin

Phloretin is a natural phenol which inhibits a variety of transporters. It inhibits the monocarboxylate transporters MCT1 and MCT2 (IC₅₀ = 28 and 14 µM, respectively), restricting the rapid transport of monocarboxylates like lactate and pyruvate across the plasma membrane. Phloretin also blocks the sodium/D-glucose cotransporter (Ki = 86 µM) and the human concentrative nucleoside transporter 3 (Ki = 32 µM). Blocks L-type Ca²⁺ channels; activates Ca²⁺-activated K⁺ channels in amphibian myelinated nerve fibers.