1. Membrane Transporter/Ion Channel
  2. CFTR
  3. Icenticaftor

Icenticaftor (Synonyms: QBW251)

Cat. No.: HY-109177 Purity: 99.87%
Handling Instructions

Icenticaftor (QBW251) is an orally active CFTR channel potentiator, with EC50s of 79 nM and 497 nM for F508del and G551D CFTR, respectively. Icenticaftor can be used for chronic obstructive pulmonary disease (COPD) and cystic fibrosis research.

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

Icenticaftor Chemical Structure

Icenticaftor Chemical Structure

CAS No. : 1334546-77-8

Size Price Stock Quantity
5 mg USD 950 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
50 mg USD 3500 In-stock
Estimated Time of Arrival: December 31
100 mg USD 5500 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Icenticaftor (QBW251) is an orally active CFTR channel potentiator, with EC50s of 79 nM and 497 nM for F508del and G551D CFTR, respectively. Icenticaftor can be used for chronic obstructive pulmonary disease (COPD) and cystic fibrosis research[1].

IC50 & Target

EC50: 79 nM (F508del CFTR) and 497 nM (G551D CFTR)[1]

In Vitro

Icenticaftor (QBW251), an orally bioavailable small molecule CFTR potentiator, can restore CFTR function in specific CFTR genotypes as well as wild-type CFTR[2].

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

In Vivo

In Sprague-Dawley rats, the pharmacokinetic profile of Icenticaftor is established. After oral administration at a dose of 3 mg/kg, the oral bioavailability is 90%, and AUClast is 20 635 nmol/L•h[1].

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

Clinical Trial
Molecular Weight

361.24

Formula

C12H13F6N3O3

CAS No.
SMILES

O=C(C1=NC(OC)=C(C(F)(F)F)C=C1N)NC[[email protected]](C)(O)C(F)(F)F

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 : 150 mg/mL (415.24 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7682 mL 13.8412 mL 27.6824 mL
5 mM 0.5536 mL 2.7682 mL 5.5365 mL
10 mM 0.2768 mL 1.3841 mL 2.7682 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: 4.25 mg/mL (11.77 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 4.25 mg/mL (11.77 mM); Clear solution

  • 3.

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

    Solubility: ≥ 4.25 mg/mL (11.77 mM); Clear solution

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

Purity: 99.87%

References
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Icenticaftor
Cat. No.:
HY-109177
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