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Ivacaftor-d4

目录号 : GC70634

Ivacaftor-d4(VX-770-d4)是氘标记的Ivacaftor。

Ivacaftor-d4 Chemical Structure

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1 mg
¥3,060.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

Ivacaftor-d4 (VX-770-d4) is the deuterium labeled-Ivacaftor . Ivacaftor is a potent and orally active CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively.

Ivacaftor (10 μM) increases 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. Ivacaftor corrects the functional defect of ABCB4 mutants[1].
Ivacaftor (10 μM) significantly increases CFTR activity in W1282X-expressing cells compared to R1162X CFTR cells[2].
Ivacaftor shows no significant activity against 160 targets tested including the GABAA benzodiazepine receptor. Ivacaftor increases the chloride secretion with an EC50 value of 0.236 ± 0.200 μM, a 10-fold shift in potency compared to the F508del HBEs[3].
In recombinant cells, Ivacaftor increases CFTR channel open probability (Po) in both the F508del processing mutation and the G551D gating mutation. Ivacaftor increases forskolin-stimulated IT in temperature-corrected F508del-FRT cells by appr 6-fold with an EC50 of 25 nM[4].

Ivacaftor (1-200 mg/kg, p.o.) exhibits good oral bioavailability in rat[3].

Chemical Properties

Cas No. SDF
分子式 C24H24D4N2O3 分子量 396.52
溶解度 DMSO : 50 mg/mL (126.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) 储存条件 4°C, sealed storage, away from moisture
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.5219 mL 12.6097 mL 25.2194 mL
5 mM 0.5044 mL 2.5219 mL 5.0439 mL
10 mM 0.2522 mL 1.261 mL 2.5219 mL
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