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Bafilomycin C1 is a member of a potent family of macrocyclic lactones. Bafilomycin C1 shares a similar mode of action and activity as its more accessible A1 analogue. Bafilomycin C1 is broadly active against bacteria, fungi, insects, nematodes and cestodes. Bafilomycin C1 has attracted interest as a potential agent for treating osteoporosis. The presence of the fumarate group provides an ideal ligand for affinity chromatography of V-ATPase.

Bafilomycin C1 is a selective, reversible inhibitor of vacuolar H+-ATPases (V-ATPases). It blocks these pumps in mammalian, plant, or fungal cells, preventing proton transport and compartment acidification. Bafilomycin C1 has been shown to have angiostatic activity in the chick chorioallantoic membrane assay. It has also been used, when coupled to cellulose, to purify V-ATPases.[Cayman Chemical]

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