Tezacaftor (Synonyms: VX-661)

Name: Tezacaftor
Brand: MedChemExpress
SKU: HY-15448
Rating: 5.0 (25 reviews)

Cat. No.: HY-15448 Purity: 99.85%: Data Sheet
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Tezacaftor (VX-661) is a F508del CFTR corrector. It helps CFTR protein reach the cell surface. However, Ivacaftor (VX-770, HY-13017), a CFTR potentiator, helps to prolong the opening time of cell surface CFTR protein channels. Tezacaftor combining with Ivacaftor, shows potent efficacy against cystic fibrosis and diseases with homozygous for the CFTR Phe508del mutation. Moreover, Elexacaftor (VX-445, HY-111772) is also a CFTR corrector. Elexacaftor-Tezacaftor-Ivacaftor aims at with cystic fibrosis (CF) with at least one Phe508del mutation, often avoids the indication for lung transplantation.

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

CAS No. : 1152311-62-0

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	Get quote
1 g	Get quote

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Customer Review

Based on 25 publication(s) in Google Scholar

Other Forms of Tezacaftor:

25 Publications Citing Use of MCE Tezacaftor

2D/3D Cell Culture and Differentiation

Bio/Physico-chemical Assay

: Tezacaftor purchased from MedChemExpress. Usage Cited in: J Med Chem. 2025 Feb 27;68(4):4596-4618. [Abstract]; ARN23765 stabilizes NBD1-ICL4 and NBD1-ICL1 interactions. HEK293 cells were transfected with the constructs coding for F508del-CFTR, F508del/R1070W-CFTR, and R170G-CFTR and incubated for 24 h with ARN23765 (10 nM) or Tezacaftor (VX-661, 3 μM). DMSO (0.2%) was used as negative control. Left: representative WBs with detection of CFTR B- and C-bands. Right: quantification (mean ± SD, 3–4 independent experiments) of CFTR band-C abundance, calculated using the conventional equation [band-C/band C+B].

: Tezacaftor purchased from MedChemExpress. Usage Cited in: J Med Chem. 2025 Feb 27;68(4):4596-4618. [Abstract]; ARN23765 stabilizes NBD1-ICL4 and NBD1-ICL1 interactions. HEK293 cells were transfected with the constructs coding for F508del-CFTR, F508del/R1070W-CFTR, and R170G-CFTR and incubated for 24 h with ARN23765 (10 nM) or Tezacaftor (VX-661, 3 μM). DMSO (0.2%) was used as negative control. CFTR channel activity was evaluated with fluorometric imaging plate reader functional assay (FLIPR).40 Plasma membrane depolarization was detected as an increase in fluorescence (ΔF), after which CFTR was inhibited by the addition of inhibitor-172, (10 μM). Left: representative fluorescence traces. Right: peak change in fluorescence (mean ± SD, 8 replicates), expressed relative to baseline fluorescence (ΔF/F0). FSK: forskolin; CFTR Inh: inhibitor-172.

: Tezacaftor purchased from MedChemExpress. Usage Cited in: iScience. 2024 Aug 9;27(9):110703. [Abstract]; Representative traces of whole-cell currents of HEK-293 cells cotransfected with PIEZO1 and CFTR mutant F508del, pre-treated with combination of CFTR correctors VX445/VX661 (Tezacafto) (2 μM each) for 24 h.107 Bath solution contained 10 μM Yoda1, 20 μM Forskolin, and 20 μM CFTRinh-172.

: Tezacaftor purchased from MedChemExpress. Usage Cited in: iScience. 2024 Aug 9;27(9):110703. [Abstract]; Summary of Yoda1-induced current in HEK-293 cells transfected with PIEZO1 only or cotransfected with PIEZO1 and CFTR mutant F508del. Cells were pre-treated with or without combination of CFTR correctors VX445/VX661 (Tezacafto) (2 μM each) for 24 h.

: Tezacaftor purchased from MedChemExpress. Usage Cited in: Cell. 2022 Jan 6;185(1):158-168.e11. [Abstract]; Competition binding assay. The binding of [H³]lumacaftor (10 nM) was plotted as a function of the competitor’s concentration. Data were fit to a single-site competitive binding model. The K_i values for lumacaftor and Tezacaftor are 7.7 ± 2.0 nM and 0.12 ± 0.04 mM, respectively. No competition was observed for elexacaftor and Corr-4a.

: Tezacaftor purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2020 Dec 31;22(1):344.; Representative brightfield images of G542X intestinal organoids treated with 100 µM G418, 2.5 mM gentamicin, or 2.5 mM paromomycin and indicated combinations of 1 µM SMG1i and/or 3.3 µM Tezacaftor (VX-661) at 0 min and 180 min following treatment with 10 µM forskolin. Scale bar is 100 µm.

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Description

In Vitro

Tezacaftor (2 μM, 24 h) increases the expression level of N1303K-CFTR in HEK293 and CFBE cells^[4].

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

Western Blot Analysis^[4]

Cell Line:	HEK293, CFBE
Concentration:	2 μM
Incubation Time:	24 h
Result:	Increased N1303K-CFTR expression levels.

Clinical Trial

Molecular Weight

520.50

Formula

C₂₆H₂₇F₃N₂O₆

CAS No.

1152311-62-0

Appearance

Solid

Color

White to yellow

SMILES

O=C(C1(C2=CC=C(OC(F)(F)O3)C3=C2)CC1)NC4=CC5=C(N(C[C@@H](O)CO)C(C(C)(C)CO)=C5)C=C4F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (96.06 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9212 mL	9.6061 mL	19.2123 mL
5 mM	0.3842 mL	1.9212 mL	3.8425 mL
10 mM	0.1921 mL	0.9606 mL	1.9212 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.94%

Select Batch:

Data Sheet (282 KB) SDS (396 KB)

COA (260 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[1]. Treatment with VX-661 and Ivacaftor in a Phase 2 Study Resulted in Statistically Significant Improvements in Lung Function in People with Cystic Fibrosis Who Have Two Copies of the F508del Mutation. April 18, 2013

[2]. Taylor-Cousar JL, et al. Tezacaftor-Ivacaftor in Patients with Cystic Fibrosis Homozygous for Phe508del. N Engl J Med. 2017 Nov 23;377(21):2013-2023. [Content Brief]

[3]. Burgel PR, et al. Rapid Improvement after Starting Elexacaftor-Tezacaftor-Ivacaftor in Patients with Cystic Fibrosis and Advanced Pulmonary Disease. Am J Respir Crit Care Med. 2021 Jul 1;204(1):64-73. [Content Brief]

[4]. Huang Y, et al. Elexacaftor/Tezacaftor/Ivacaftor Improved Clinical Outcomes in a Patient with N1303K-CFTR Based on In Vitro Experimental Evidence. Am J Respir Crit Care Med. 2021 Nov 15;204(10):1231-1235. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9212 mL	9.6061 mL	19.2123 mL	48.0307 mL
	5 mM	0.3842 mL	1.9212 mL	3.8425 mL	9.6061 mL
	10 mM	0.1921 mL	0.9606 mL	1.9212 mL	4.8031 mL
	15 mM	0.1281 mL	0.6404 mL	1.2808 mL	3.2020 mL
	20 mM	0.0961 mL	0.4803 mL	0.9606 mL	2.4015 mL
	25 mM	0.0768 mL	0.3842 mL	0.7685 mL	1.9212 mL
	30 mM	0.0640 mL	0.3202 mL	0.6404 mL	1.6010 mL
	40 mM	0.0480 mL	0.2402 mL	0.4803 mL	1.2008 mL
	50 mM	0.0384 mL	0.1921 mL	0.3842 mL	0.9606 mL
	60 mM	0.0320 mL	0.1601 mL	0.3202 mL	0.8005 mL
	80 mM	0.0240 mL	0.1201 mL	0.2402 mL	0.6004 mL

Tezacaftor 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.

Keywords:

Tezacaftor1152311-62-0VX-661VX661VX 661CFTRCystic fibrosis transmembrane conductance regulatorModulatorHEK293CFBELung transplantationInhibitorinhibitorinhibit

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Tezacaftor (Synonyms: VX-661)

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Other Forms of Tezacaftor:

Tezacaftor Related Antibodies

25 Publications Citing Use of MCE Tezacaftor

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•Related Screening Libraries:

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Purity & Documentation

References

Customer Review

Tezacaftor Related Antibodies

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Complete Stock Solution Preparation Table

Tezacaftor Related Classifications

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