(R)-BPO-27

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抑制剂描述：

产品名称：(R)-BPO-27

产品别名：见爱必信官网

英文别名：(R)-BPO-27

靶点：CFTR

CAS：1415390-47-4

纯度：

外观：见爱必信官网

保存方法：

描述：(R)-BPO-27 is a potent CFTR inhibitor with an IC50 of 4 nM.

溶解性：DMSO

体外研究：

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.

体内研究：Following bolus interperitoneal administration in mice, serum (R)-1 decays with t1/2 ≈ 1.6 h and gives sustained therapeutic concentrations in kidney.

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