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Ivacaftor (VX-770) Sale

(Synonyms: 依伐卡托; VX-770) 目录号 : GC10296

A CFTR potentiator

Ivacaftor (VX-770) Chemical Structure

Cas No.:873054-44-5

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5mg
¥350.00
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10mg
¥525.00
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25mg
¥867.00
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50mg
¥1,213.00
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100mg
¥1,698.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment [1]:

Cell lines

CHO-G551D cells

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 °C for several months.

Reaction Conditions

10 μM; 0 ~ 8 mins

Applications

In CHO-G551D cells, VX-770 activated G551D-CFTR channel, and OAG + VX-770 increased G551D-CFTR activity by 58%.

References:

[1]. Vachel L1, Norez C, Becq F, Vandebrouck C. Effect of VX-770 (ivacaftor) and OAG on Ca2+ influx and CFTR activity in G551D and F508del-CFTR expressing cells. J Cyst Fibros. 2013 Dec;12(6):584-91.

产品描述

Ivacaftor (VX-770) is a potent and orally bioavailable small molecule potentiator of cystic fibrosis transmembrane conductance regulator (CFTR). Studies in both G551D- and F508del-CFTR expressing cells have shown VX-700 combined with forskolin, but not VX-700 alone, has significantly increased CFTR-mediated Cl-secretion. The EC50 values of VX-700 in G551D- and F508del-CFTR are 100 nM and 25 nM, respectively [1].

VX-770 has been reported to reduce ENaC-mediated Na+ absorption and increase the amount of fluid on the apical surface in human CF bronchial epithelia (HBE) carrying G551D/F508del [1]. VX-770 combined with OAG has been shown to increase G551D-CFTR activity and OAG-dependent Ca2+ influx and in Chinese hamster ovary (CHO) cells [2].

References:
1. Van Goor F1, Hadida S, Grootenhuis PD, Burton B, Cao D, Neuberger T, Turnbull A, Singh A, Joubran J, Hazlewood A, Zhou J, McCartney J,Arumugam V, Decker C, Yang J, Young C, Olson ER, Wine JJ, Frizzell RA, Ashlock M, Negulescu P. Rescue of CF airway epithelial cell function in vitro by a CFTR potentiator, VX-770. Proc Natl Acad Sci U S A. 2009 Nov 3;106(44):18825-30.
2. Vachel L1, Norez C, Becq F, Vandebrouck C. Effect of VX-770 (ivacaftor) and OAG on Ca2+ influx and CFTR activity in G551D and F508del-CFTR expressing cells. J Cyst Fibros. 2013 Dec;12(6):584-91

Chemical Properties

Cas No. 873054-44-5 SDF
别名 依伐卡托; VX-770
化学名 N-(2,4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide hydrate
Canonical SMILES CC(C1=CC(C(C)(C)C)=C(C=C1NC(C2=CNC3=CC=CC=C3C2=O)=O)O)(C)C.O
分子式 C24H28N2O3 分子量 392.49
溶解度 ≥ 19.6mg/mL in DMSO, ≥ 2.95 mg/mL in EtOH with ultrasonic 储存条件 Store at -20°C
General tips 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。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.5478 mL 12.7392 mL 25.4784 mL
5 mM 0.5096 mL 2.5478 mL 5.0957 mL
10 mM 0.2548 mL 1.2739 mL 2.5478 mL
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