CAS NO: | 873054-44-5 |
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 |
生物活性 | Ivacaftor (VX-770) is a potent and orally bioavailableCFTRpotentiator, targeting G551D-CFTR and F508del-CFTR withEC50s of 100 nM and 25 nM, respectively. | ||||||||||||||||
IC50& Target | EC50: 100 nM (G551D-CFTR), 25 nM (F508del-CFTR)[1] | ||||||||||||||||
体外研究 (In Vitro) | Ivacaftor (10 μM) increases the PC secretion activity by 3-fold for ABCB4-G535D, 13.7-fold for ABCB4-G536R, 6.7-fold for ABCB4-S1076C, 9.4-fold for ABCB4-S1176L, and 5.7-fold for ABCB4-G1178S. Ivacaftor corrects the functional defect of ABCB4 mutants[1]. Ivacaftor (10 μM) significantly increases CFTR activity in W1282X-expressing cells compared to R1162X CFTR cells[2]. Ivacaftor shows no significant activity against 160 targets tested including the GABAAbenzodiazepine receptor. Ivacaftor increases the chloride secretion with an EC50of 0.236 ± 0.200 μM, a 10-fold shift in potency compared to the F508del HBEs[3]. In recombinant cells, VX-770 increases CFTR channel open probability (Po) in both the F508del processing mutation and the G551D gating mutation. VX-770 increases forskolin-stimulated ITin temperature-corrected F508del-FRT cells by appr 6-fold with an EC50of 25 nM[4]. | ||||||||||||||||
体内研究 (In Vivo) | Ivacaftor (1-200 mg/kg, p.o.) exhibits good oral bioavailability in rat[3]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 392.49 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C24H28N2O3 | ||||||||||||||||
CAS 号 | 873054-44-5 | ||||||||||||||||
中文名称 | 依伐卡托;依法卡托;艾伐卡托 | ||||||||||||||||
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 : 50 mg/mL(127.39 mM;Need ultrasonic) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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