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

Chemical Structure : Ivacaftor hydrate

CAS No.: 1134822-07-3

Ivacaftor hydrate (VX-770 hydrate;VX 770 hydrate;VX770 hydrate)

货号: PC-43327Not 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

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; 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; also potentiates CFTR-mediated Cl− secretion in primary cultures of G551D/F508del HBE and F508del HBE; demonstrates potential for treatment of cystic fibrosis with certain mutations in CFTR gene (primarily the G551D mutation).

Fibrosis

Approved

物理化学性质&存储条件

分子量 410.506
分子式 C24H30N2O4
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-, hydrate (1:1)

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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