Ivacaftor

Cat. No. 7887 提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Potent and selective CFTR potentiator

化学名： N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxo-3-quinolinecarboxamide

纯度： ≥98% (HPLC)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for Ivacaftor

Ivacaftor is a potent and selective potentiator of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) that targets F508del-CFTR and G551D-CFTR (EC₅₀ values are 25 nM and 100 nM, respectively); its potentiation activity depends on the level of CFTR phosphorylation. Ivacaftor reversibly binds to wild type (WT-CFTR) and G551D-CFTR mutants, increasing the open probability via an ATP-independent mechanism, and enhances cAMP/PKA-signaling mediated gating activity for both WT-CFTR and G551D-CFTR mutants. In cultured human CF bronchial epithelia with G551D/F508del mutations, Ivacaftor increases Forskolin (Cat. No. 1099)-induced transepithelial current (EC₅₀ = 236 nM) and increases chloride secretion by 10-fold. Also rescues endothelial CFTR expression and function and prevents endothelial barrier failure and protein leak in human pulmonary microvascular endothelial cells. Ivacaftor is orally bioavailable.

技术数据 for Ivacaftor

分子量	392.5
公式	C₂₄H₂₈N₂O₃
储存	Store at -20°C
纯度	≥98% (HPLC)
CAS Number	873054-44-5
PubChem ID	16220172
InChI Key	PURKAOJPTOLRMP-UHFFFAOYSA-N
Smiles	O=C(C1=CNC2=C(C1=O)C=CC=C2)NC3=CC(O)=C(C(C)(C)C)C=C3C(C)(C)C

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for Ivacaftor

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
	ethanol	1.96	5
	DMSO	39.25	100

制备储备液 for Ivacaftor

以下数据基于产品分子量 392.5。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

浓度/溶剂体积/质量	1 mg	5 mg	10 mg
1 mM	2.55 mL	12.74 mL	25.48 mL
5 mM	0.51 mL	2.55 mL	5.1 mL
10 mM	0.25 mL	1.27 mL	2.55 mL
50 mM	0.05 mL	0.25 mL	0.51 mL

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产品说明书 for Ivacaftor

分析证书/产品说明书

化学品安全技术说明书

参考文献 for Ivacaftor

参考文献是支持产品生物活性的出版物。

Jih et al (2013) Vx-770 potentiates CFTR function by promoting decoupling between the gating cycle and ATP hydrolysis cycle. Proc.Natl.Acad.Sci.U.S.A. 110 4404 PMID: 23440202

Cui (2019) VX-770-mediated potentiation of numerous human CFTR disease mutants is influenced by phosphorylation level. Sci.Rep. 9 13460 PMID: 31530897

Erfinanda et al (2022) Loss of endothelial CFTR drives barrier failure and edema formation in lung infection and can be targeted by CFTR potentiation. Sci.Transl.Med. 14 eabg8577 PMID: 36475904

Levring et al (2023) CFTR function, pathology and pharmacology at single-molecule resolution. Nature 616 606 PMID: 36949202

Eckford et al (2012) Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) potentiator VX-770 (Ivacaftor) opens the defective channel gate of mutant CFTR in a phosphorylation dependent but ATP-independent manner. J.Biol.Chem. 287 36639 PMID: 22942289

Nguyen et al (2021) Modulation of cAMP metabolism for CFTR potentiation in human airway epithelial cells. Sci.Rep. 11 904 PMID: 33441643

If you know of a relevant reference for Ivacaftor, please let us know.

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关键词: Ivacaftor, Ivacaftor supplier, Ivacaftor, Cystic, Fibrosis, Transmembrane, Conductance, Regulator, CFTR, potentiator, G551D, F508, 7887, Tocris Bioscience

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