BPO-27 racemate
作者：齐岳
发布时间：2023-09-15
09:03:06
点击数：
产品名称：BPO-27 racemate
产品描述：
| 产品描述 | Bpo-27 racemate is an effective CFTR inhibitor with IC50 of 8 nM. |
| 靶点活性 | CFTR:8 nM |
| 体外活性 | The R enantiomer of BPO-27 inhibits CFTR chloride conductance (IC50: 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 [1]. (R)-BPO-27 binds near the canonical ATP binding site. Whole-cell patch-clamp studies show 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 [2]. |
| 体内活性 | Following bolus intraperitoneal administration of BPO-27 in mice, serum (R)-1 decays with t1/2 ≈ 1.6 h and gives sustained therapeutic concentrations in the kidney [1]. |
| 别名 | BPO-27 (racemate) |
| 分子量 | 548.34 |
| 分子式 | C26H18BrN3O6 |
| CAS No. | 1314873-02-3 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 6 mg/mL (10.94 mM),Need ultrasonic and warming
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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