Ivacaftor

SKU: orb1305294

描述

Ivacaftor (VX-770) is a CFTR potentiator effective on G551D and F508del mutants, with EC50 values of 100 nM and 25 nM, respectively, in Fisher rat thyroid cell assays. It is a key research tool for studying CFTR channel function and rescue in cellular models of cystic fibrosis, supporting both in vitro and preclinical in vivo research.

研究领域

Cell Biology, Pharmacology & Drug Discovery

图片与验证

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关键属性

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CAS 号	873054-44-5
MW	392.4907
纯度	99.98% (May vary between batches)
分子式	C₂₄H₂₈N₂O₃
SMILES	CC(C)(C)C1=CC(=C(O)C=C1NC(=O)C1=CNC2=C(C=CC=C2)C1=O)C(C)(C)C
靶点	Autophagy,CFTR
溶解性	H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:252 mg/mL (642.05 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (12.74 mM)

生物活性

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靶点 IC50	F508del CFTR:25 nM(EC50, Fisher rat thyroid cells)\|CFTR (G551D):100 nM(EC50, Fisher rat thyroid cells)
体内	In a rat dose proportionality study, the AUC and Cmax were increased linearly after oral administration of Ivacaftor in a suspension vehicle at doses from 1 to 200 mg/kg (3, 10, 30, and 100 were the intermediate doses). A similar trend was observed in beagle dogs increasing the oral dose from 3 to 80 mg/kg (10, 30, and 60 were the intermediate doses), confirming high levels of oral absorption. The predicted human hepatic clearance of Ivacaftor using allometric scaling from four species was 4.7 mL min 1 kg 1, which is approximately 23% of hepatic blood flow .
体外	VX-770 increased the forskolin-stimulated IT in temperature-corrected F508del-FRT cells by ~6-fold with an EC50 of 25 ± 5 nM. Before the addition of VX-770, the CFTR channel was exposed to maximally effective concentrations of PKA (75 nM) and ATP (1 mM). Under these conditions, 10 μM VX-770 increased the Po of G551D CFTR by ~6-fold . HEK293 cells transiently expressing ABCB4-wt or the mutants were treated with 10 μmol/L of ivacaftor (VX-770), for 24 hours. Treatment with ivacaftor increased 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 .
细胞研究	HEK293 cells were seeded on poly-lysine precoated six-well plates at a density of 1.3 x 10^6 cells/well. Six hours after seeding, cells were transiently transfected with 1μg of ABCB4-encoding plasmids using Turbofect, following the manufacturer's instructions. Twenty-four hours post-transfection, cells were washed twice with HBSS, then the medium was replaced by phenol red-free DMEM containing 0.5 mmol/L sodium taurocholate and 0.02% fatty acid–free bovine serum albumin (BSA) in the presence or absence of 10 μmol/L of ivacaftor, 50 μM/L of UDCA, and 10 μmol/L of ivacaftor plus 50 μM/L of UDCA. Media were collected after 24 hours .
动物研究	Male mouse,Sprague Dawley rats,beagle dog,and cynomolgus monkeys (n = 3/group) were administered a single iv dose of compound formulated in dimethyl isosorbide/ethanol/PEG400/5% dextrose in water (D5W) (10%/15%/35%/40%) at the nominal dose indicated in a dose volume of 1 mL/kg.Blood samples (0.3 mL,sodium heparin anticoagulant) were collected from an indwelling carotid cannula at the following nominal time points: at predose,5,15,30,and 45 min and 1,2,4,6,8,12,24,36,and 48 h following iv administration and at predose,0.25,0.50,1,1.5,2,4,8,12,and 24 h following oral administration.The concentration of compound in the plasma samples was determined with a liquid chromatography/tandem mass spectrometry (LC/MS/MS) method,which had a lowest limit of quantitation (LLOQ) of 1 ng/mL and a linearity range between 1 and 2500 ng/mL .

储存与操作

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储存	-20°C
有效期	12 months from date of receipt.
免责声明	For research use only

别名

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inhibit, Ivacaftor, Ivacaftor (VX-770), G551D-CFTR, F508del-CFTR, Inhibitor, Autophagy, Cystic fibrosis transmembrane conductance regulator, CFTR, VX770, VX-770, VX 770

相似产品

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N-[5-(Methoxycarbonyloxy)-2,4-di(tert-butyl)phenyl]-4-oxo-1H-quinoline-3-carboxamide [orb3144226]
CAS 号：
1246213-45-5
MW:
450.53
分子式：
C₂₆H₃₀N₂O₅
可选规格： 10 mg, 50 mg
Ivacaftor hydrate [orb1707921]
CAS 号：
1134822-07-3
MW:
410.514
分子式：
C₂₄H₃₀N₂O₄
可选规格： 50 mg, 100 mg, 25 mg
Ivacaftor benzenesulfonate [orb1707922]
CAS 号：
1134822-09-5
MW:
550.67
分子式：
C₃₀H₃₄N₂O₆S
可选规格： 50 mg, 100 mg, 25 mg
Ivacaftor [orb1223783]
纯度：
>98% (HPLC)
CAS 号：
873054-44-5
MW:
392.4907
分子式：
C₂₄H₂₈N₂O₃
可选规格： 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 500 mg, 1 g

质量保证

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化合物标识

PubChem CID

16220172 ↗

关键属性

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暂无计算属性。

实验方案信息

查看更多实验方案

CAS 号：	1246213-45-5
MW:	450.53
分子式：	C₂₆H₃₀N₂O₅

CAS 号：	1134822-07-3
MW:	410.514
分子式：	C₂₄H₃₀N₂O₄

CAS 号：	1134822-09-5
MW:	550.67
分子式：	C₃₀H₃₄N₂O₆S

纯度：	>98% (HPLC)
CAS 号：	873054-44-5
MW:	392.4907
分子式：	C₂₄H₂₈N₂O₃

Ivacaftor

描述

研究领域

图片与验证

关键属性

生物活性

储存与操作

别名

相似产品

N-[5-(Methoxycarbonyloxy)-2,4-di(tert-butyl)phenyl]-4-oxo-1H-quinoline-3-carboxamide [orb3144226]

Ivacaftor hydrate [orb1707921]

Ivacaftor benzenesulfonate [orb1707922]

Ivacaftor [orb1223783]

质量保证

化合物标识

关键属性

实验方案信息

可选规格