货号	规格	价格	上海	北京	珠海	重庆	武汉
S82814-1mg	≥98%	￥420.00 S82814-1mg ￥420.00 3-5天	0 货期：3-5天	-	-	-	-
S82814-5mg	≥98%	￥1310.00 S82814-5mg ￥1310.00 3-5天	0 货期：3-5天	-	-	-	-
S82814-10mg	≥98%	￥1840.00 S82814-10mg ￥1840.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

BPO-27 racemate is a potent CFTR inhibitor with an IC50 of 8 nM

靶点：

IC50: 8 nM;CFTR; Autophagy

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

参考文献：

1. Snyder DS, et al. Absolute Configuration And Biological Properties of Enantiomers of CFTR Inhibitor BPO-27. ACS Med Chem Lett. 2013 May 9;4(5):456-459. 2. Kim Y, et al. Benzopyrimido-pyrrolo-oxazine-dione (R)-BPO-27 Inhibits CFTR Chloride Channel Gating by Competition with ATP. Mol Pharmacol. 2015 Oct;88(4):689-96.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.824 ml	9.118 ml	18.237 ml
5 mM	0.365 ml	1.824 ml	3.647 ml
10 mM	0.182 ml	0.912 ml	1.824 ml
50 mM	0.036 ml	0.182 ml	0.365 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

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计算重置

BPO-27 (racemate)