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BPO-27 racemate

CAS No. : 1314873-02-3

MCE 国际站：BPO-27 racemate

产品活性：BPO-27 racemate是有效的CFTR抑制剂，IC₅₀值为8 nM。

研究领域：Membrane Transporter/Ion Channel  |  Autophagy

作用靶点：CFTR  |  Autophagy

In Vitro: The benzopyrimido-pyrrolo-oxazinedione BPO-27 is an analogue of PPQ-102, which inhibits CFTR with an IC₅₀ of 8 nM. The R enantiomer of BPO-27 inhibits CFTR chloride conductance with an IC₅₀ of 4 nM, while S enantiomer is inactive. In vitro metabolic stability in hepatic microsomes shows both enantiomers as stable, with less than 5% metabolism in 4 h. (R)-BPO-27 binds near the canonical ATP binding site. Whole-cell patch-clamp studies shows linear CFTR currents with a voltage-independent (R)-BPO-27 block mechanism. At a concentration of (R)-BPO-27 that inhibits CFTR chloride current by 50%, the EC₅₀ for ATP activation of CFTR increases from 0.27 to 1.77 mM.

In Vivo: Following bolus interperitoneal administration in mice, serum (R)-1 decays with t_1/2 ≈ 1.6 h and gives sustained therapeutic concentrations in kidney.

相关产品：Bioactive Compound Library Plus  |  K41498 TFA  |  Kobusin  |  PG01

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