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Tezacaftor

Name: Tezacaftor
Brand: TargetMol
SKU: T2263
Price: 34 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: VX661) Copy Product Info

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Synonyms: VX661

Catalog No. T2263 Copy Product Info

Purity: 99.96%

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Tezacaftor (VX-661) is a cystic fibrosis transmembrane conductance regulator (CFTR) corrector. Tezacaftor increases the number of functional CFTR proteins by promoting the proper folding and transport of mutant CFTR proteins to the cell surface, thereby restoring chloride channel function. Tezacaftor is commonly used in cystic fibrosis research.

Cas No. 1152311-62-0

Pack Size	Price	USA Stock	Global Stock
1 mg	$34	In Stock	In Stock
2 mg	$48	In Stock	In Stock
5 mg	$75	In Stock	In Stock
10 mg	$125	In Stock	In Stock
25 mg	$223	In Stock	In Stock
50 mg	$360	In Stock	In Stock
100 mg	$531	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$90	In Stock	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.96%

Color:White

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COA HNMR HPLC

Product Introduction

Bioactivity

Description	Tezacaftor (VX-661) is a cystic fibrosis transmembrane conductance regulator (CFTR) corrector. Tezacaftor increases the number of functional CFTR proteins by promoting the proper folding and transport of mutant CFTR proteins to the cell surface, thereby restoring chloride channel function. Tezacaftor is commonly used in cystic fibrosis research.
Targets & IC50	DEGS:3 µM
In vitro	Methods: Peripheral blood was collected from cystic fibrosis patients before treatment with Elexacaftor/Tezacaftor/Ivacaftor, 1 month after treatment initiation, and 6 months after treatment initiation. Peripheral blood mononuclear cells were isolated and co-incubated with GFP-expressing Pseudomonas aeruginosa PAO1 strain for 30 minutes, followed by assessment of intracellular viable bacteria count. Results: Pre-treatment CF patients exhibited significantly lower intracellular viable bacteria counts in monocytes compared to healthy controls, indicating phagocytic dysfunction. At 1 month and 6 months post-treatment, intracellular viable bacteria counts increased significantly (by 2-fold and 2.5-fold, respectively), demonstrating marked improvement in phagocytic function. [1] Methods: Differentiated CF human bronchial epithelial cells (HBEC) with the F508del-CFTR homozygous genotype were treated with the ETI combination (Elexacaftor (3 μM) + Tezacaftor (3 μM) + Ivacaftor (1 μM)), dissolved in DMSO, added to the basolateral medium. The control consisted of an equal volume of DMSO. Treatment lasted 72 hours. with drug solution replaced every 24 hours. μOCT measurements assessed mucus clearance time (MCT), airway surface liquid depth (ASL), and perichylial liquid depth (PCL). Results: ETI treatment efficacy: After 72 hours of ETI treatment, CF HBECs exhibited significant recovery in ASL, PCL, and MCT, approaching non-CF levels. [2]
In vivo	The F508del mutation channel can avoid degradation and be transported to the cell membrane under the action of VX-661.
Synonyms	VX661

Chemical Properties

Molecular Weight	520.5
Formula	C₂₆H₂₇F₃N₂O₆
Cas No.	1152311-62-0
Smiles	CC(C)(CO)c1cc2cc(NC(=O)C3(CC3)c3ccc4OC(F)(F)Oc4c3)c(F)cc2n1C[C@@H](O)CO
Relative Density.	1.49 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 245 mg/mL (470.7 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (9.61 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9212 mL	9.6061 mL	19.2123 mL	96.0615 mL
5 mM	0.3842 mL	1.9212 mL	3.8425 mL	19.2123 mL
10 mM	0.1921 mL	0.9606 mL	1.9212 mL	9.6061 mL
20 mM	0.0961 mL	0.4803 mL	0.9606 mL	4.8031 mL
50 mM	0.0384 mL	0.1921 mL	0.3842 mL	1.9212 mL
100 mM	0.0192 mL	0.0961 mL	0.1921 mL	0.9606 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc