CAS NO: | 936727-05-8 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Lumacaftor (VX-809; VRT 826809) is aCFTRmodulator that corrects the folding and trafficking ofCFTRprotein. | ||||||||||||||||
IC50& Target | EC50: 0.1 μM (CFTR)[1] | ||||||||||||||||
体外研究 (In Vitro) | In fischer rat thyroid (FRT) cells, Lumacaftor improves F508del-CFTR maturation by 7.1±0.3 fold (n=3) compared with vehicle-treated cells (EC50, 0.1±0.1 μM; n=3) and enhances F508del-CFTR-mediated chloride transport by approximately fivefold (EC50, 0.5±0.1 μM; n=3). At Lumacaftor concentrations greater than 10 μM, the response is reduced, resulting in a bell-shaped dose-response relationship with an IC50of approximately 100 μM. Lumacaftor is orally bioavailable in rats and achieved in vivo plasma levels significantly above concentrations required for in vitro efficacy[1]. Lumacaftor produces a concentration-dependent increase in the HRP luminescence signal after incubation with cells at 37℃ or 27℃ in both cell lines, with a similar EC50value of approximately 0.3 μM. In F508-HRP CFBE41o-cells at 37℃, Lumacaftor increases the signal maximally to approximately 250 luminescence arbitrary units (a.u.) over the DMSO control baseline of approximately 60 a.u., representing an approximately 4-fold signal increase. Similarly, with the R1070W-HRP CFBE41o-cells, Lumacaftor increases the signal maximally to approximately 220 a.u. over the DMSO control baseline of approximately 85 a.u., representing an approximately 2.5-fold signal increase. Therefore, both cell lines produced robust signals with a good dynamic range for high-throughput screening[2]. | ||||||||||||||||
体内研究 (In Vivo) | Oral dosing of 1 mg/kg Lumacaftor in male Sprague-Dawley rats results in a Cmaxof 2.4±1.3 μM with a t1/2of 7.7±0.4 h (mean±SD; n=3), indicating that that Lumacaftor is orally bioavailable and able to reach plasma levels that significantly exceeded EC50s for F508del-CFTR correction[1]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 452.41 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C24H18F2N2O5 | ||||||||||||||||
CAS 号 | 936727-05-8 | ||||||||||||||||
中文名称 | 鲁玛卡托 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 25 mg/mL(55.26 mM;ultrasonic and warming and heat to 60℃) 配制储备液
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