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Reciprocally, glyburide blocked SR-BI-mediated selective lipid uptake and efflux at a potency similar to that for its inhibition of ABCA1 (IC50 ∼275-300 μM).

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In the presence of 1 μm cytoplasmic ATP, the glyburide IC50 was 20.3 ± 7.1 nm ( n = 5, control) and it was 15.4 ± 1.4 nm (n = 5, p = n.s. vs.

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The CSS for glimepiride and glyburide (glibenclamide) was above IC50 values for all three isoforms, suggesting these drugs are non-selective.

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All these parameters except LDH release were reversed by glyburide (1 microM), the isolated rat aorta precontracted with methoxamine (IC(50): 23.5 microM).

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