产品描述: | Lumacaftor (VX-809; VRT 826809) is a CFTR modulator that corrects the folding and trafficking of CFTR protein. |
靶点: |
EC50: 0.1 μM (CFTR);CFTR; Autophagy |
体内研究: |
Oral dosing of 1 mg/kg Lumacaftor in male Sprague-Dawley rats results in a Cmax of 2.4±1.3 μM with a t1/2 of 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 |
参考文献: |
1. Van Goor F, et al. Correction of the F508del-CFTR protein processing defect in vitro by the investigational drug VX-809. Proc Natl Acad Sci U S A. 2011 Nov 15;108(46):18843-8. 2. Phuan PW, et al. Synergy-based small-molecule screen using a human lung epithelial cell line yields ΔF508-CFTR correctors that augment VX-809 maximal efficacy. Mol Pharmacol. 2014 Jul;86(1):42-51. |
溶解性: |
DMSO : 25 mg/mL (55.26 mM; ultrasonic and warming and heat to 60°C) |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.21 ml |
11.052 ml |
22.104 ml |
5 mM |
0.442 ml |
2.21 ml |
4.421 ml |
10 mM |
0.221 ml |
1.105 ml |
2.21 ml |
50 mM |
0.044 ml |
0.221 ml |
0.442 ml |
|
注意: |
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