1. Membrane Transporter/Ion Channel
    Autophagy
  2. CFTR
    Autophagy
  3. Ivacaftor

Ivacaftor (Synonyms: VX-770)

Cat. No.: HY-13017 Purity: 99.96%
Handling Instructions

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

For research use only. We do not sell to patients.

Ivacaftor Chemical Structure

Ivacaftor Chemical Structure

CAS No. : 873054-44-5

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10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
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10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
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100 mg USD 780 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

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

IC50 & Target

EC50: 100 nM (G551D-CFTR), 25 nM (F508del-CFTR)[1]

In Vitro

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 of 0.236 ± 0.200 μM, a 10-fold shift in potency compared to the F508del HBEs[3]. In recombinant cells, VX-770 increases CFTR channel open probability (Po) in both the F508del processing mutation and the G551D gating mutation. VX-770 increases forskolin-stimulated IT in temperature-corrected F508del-FRT cells by appr 6-fold with an EC50 of 25 nM[4].

In Vivo

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

Clinical Trial
Molecular Weight

392.49

Formula

C₂₄H₂₈N₂O₃

CAS No.

873054-44-5

SMILES

CC(C)(C1=C(C=C(C(C(C)(C)C)=C1)O)NC(C2=CNC3=C(C2=O)C=CC=C3)=O)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (127.39 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.96%

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Keywords:

IvacaftorVX-770VX770VX 770CFTRAutophagyCystic fibrosis transmembrane conductance regulatorInhibitorinhibitorinhibit

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Ivacaftor
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