生物活性：Ivacaftor-d9 is a potent CFTR modulator and exhibits an EC50 value of 255 nM for CFTR potentiation in G551D/F508del HBE Cells. Ivacaftor-D9 acts as an orally active and improved deuterated Ivacaftor analog for cystic fibrosis research[1].
体内研究(In Vivo)
In PK study, CTP-656 (oral gavage; 10 mg/kg; single dose) shows a superior pharmacokinetic profile, The plasma levels of compound were measured over 72 hours,exhibits the parameters Cmax, AUC0-24 hr, C24hr and t1/2 of 1970 ng/ml (15%), 24,260 hr*ng/ml(17%), 413 ng/ml (19%) and 13.9 hours, respectively in Male Sprague-Dawley rats.CTP-656 (oral gavage; 3 mg/kg; single dose) exhibits the parameters Cmax, AUC0-24 hr, C24hr and t1/2 of 3643 ng/ml (9%), 49,782 hr*ng/ml(31%), 1418 ng/ml (31%) and 22.8 hours, respectively in Male Beagle Dogs (3.0 mg/kg).
瑞禧生物 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
NCT NumberSponsorConditionStart DatePhaseNCT02680249Concert PharmaceuticalsHealthyFebruary 2016Phase 1NCT02599792Concert PharmaceuticalsHealthyNovember 2015Phase 1
分子量：401.55
Formula：C24H19D9N2O3
CAS 号：1413431-07-8
非标记 CAS：873054-44-5
性状：固体
颜色：White to off-white
中文名称：依伐卡托 d9
运输条件：Room temperature in continental US; may vary elsewhere.
储存方式：Powder：-20°C：3 years，4°C：2 years
In solvent：-80°C：6 months，-20°C：1 month