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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-CFTR-Ivacaftor
Ivacaftor

Chemical Structure : Ivacaftor

CAS No.: 873054-44-5

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Ivacaftor (VX-770, VX770)

货号: PC-43325Not For Human Use, Lab Use Only.

Ivacaftor (VX-770, VX770) is a potent, orally bioavailable CFTR potentiator, increases G551D- and F508del CFTR-mediated Cl- secretion with EC50 of 100 nM.

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25 mg ￥1880 In stock
50 mg ￥2980 In stock
100 mg ￥4580 In stock
250 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Ivacaftor (VX-770, VX770) is a potent, orally bioavailable CFTR potentiator, increases G551D- and F508del CFTR-mediated Cl- secretion with EC50 of 100 nM.
Ivacaftor (VX-770) increases CFTR channel open probability (Po) in both the F508del processing mutation and the G551D gating mutation in recombinant cells, increases the Po of G551D CFTR by 6-fold, the Po of F508del- and wild-type CFTR by 5-fold and 2-fold, respectively.
Ivacaftor (VX-770) also potentiates CFTR-mediated Cl− secretion in primary cultures of G551D/F508del HBE and F508del HBE.
Ivacaftor (VX-770) demonstrates potential for treatment of cystic fibrosis with certain mutations in CFTR gene (primarily the G551D mutation).

物理化学性质&存储条件

分子量 392.4907
分子式 C24H28N2O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

3-Quinolinecarboxamide, N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxo-

参考文献

1. Van Goor F, et al. Proc Natl Acad Sci U S A. 2009 Nov 3;106(44):18825-30.

2. Accurso FJ, et al. N Engl J Med. 2010 Nov 18;363(21):1991-2003.

3. Yu W, et al. J Biol Chem. 2011 Jul 15;286(28):24714-25.

4. Hadida S, et al. J Med Chem. 2014 Dec 11;57(23):9776-95.

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