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

Ivacaftor  (Synonyms: VX-770)

Cat. No.: HY-13017 Purity: 99.90%
COA 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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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO USD 101 In-stock
Solid
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10 mg USD 158 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Ivacaftor:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

392.49

Formula

C24H28N2O3

CAS No.
Appearance

Solid

Color

White to off-white

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 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

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

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

  • 3.

    Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (6.37 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.90%

References
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Ivacaftor Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

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Ivacaftor
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