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Elexacaftor

Name: Elexacaftor
Brand: TargetMol
SKU: T14935
Price: 89 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T14935Cas No. 2216712-66-0

Alias VX-445

Elexacaftor (VX-445) is a cystic fibrosis transmembrane conductance regulator (CFTR) corrector. It promotes the processing and trafficking of CFTR, increases the amount of CFTR on the cell surface, and improves the processing and trafficking of Phe508del CFTR protein.

Elexacaftor

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Purity: 99.87%

Catalog No. T14935Alias VX-445Cas No. 2216712-66-0

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$89	In Stock	In Stock
2 mg	$139	In Stock	In Stock
5 mg	$255	In Stock	In Stock
10 mg	$413	In Stock	In Stock
25 mg	$812	In Stock	In Stock
50 mg	$1,130	In Stock	In Stock
100 mg	$1,520	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$337	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.87%

Appearance:Solid

Color:White

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COA HNMR HPLC

Product Introduction

Bioactivity

Description	Elexacaftor (VX-445) is a cystic fibrosis transmembrane conductance regulator (CFTR) corrector. It promotes the processing and trafficking of CFTR, increases the amount of CFTR on the cell surface, and improves the processing and trafficking of Phe508del CFTR protein.
Targets&IC50	CFTR:1.01 μM
In vitro	Elexacaftor (VX-445) has the potential to treat cystic fibrosis and it also is a next-generation cystic fibrosis transmembrane conductance regulator (CFTR) corrector designed to restore Phe508del CFTR protein function. VX-445-Tezacaftor-VX-770 significantly improves Phe508del CFTR protein processing, trafficking, chloride transport. To a greater extent than any two of these agents in dual combination[2].
In vivo	METHODS: Patients with the Phe508del–Phe508del genotype underwent a 4-week run-in of tezacaftor and ivacaftor and were randomized to receive either elexacaftor (VX-445) (200 mg orally daily) plus tezacaftor (100 mg daily) and ivacaftor (150 mg daily) or matching placebo plus tezacaftor and ivacaftor for 4 weeks. RESULTS Treatment with elexacaftor (VX-445)-tezacaftor-ivacaftor significantly increased the percentage predicted FEV1 by up to 13.8 percentage points in patients with the Phe508del-MF genotype and up to 11.0 percentage points in patients with the Phe508del-Phe508del genotype who were already receiving tezacaftor-ivacaftor.[2]
Synonyms	VX-445

Chemical Properties

Molecular Weight	597.65
Formula	C₂₆H₃₄F₃N₇O₄S
Cas No.	2216712-66-0
Smiles	C(NS(=O)(=O)C1=CN(C)N=C1C)(=O)C2=C(N=C(C=C2)N3N=C(OCC(C(F)(F)F)(C)C)C=C3)N4C[C@@H](C)CC4(C)C
Relative Density.	1.38 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 125 mg/mL (209.15 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (6.69 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	1.6732 mL	8.3661 mL	16.7322 mL	83.6610 mL
5 mM	0.3346 mL	1.6732 mL	3.3464 mL	16.7322 mL
10 mM	0.1673 mL	0.8366 mL	1.6732 mL	8.3661 mL
20 mM	0.0837 mL	0.4183 mL	0.8366 mL	4.1831 mL
50 mM	0.0335 mL	0.1673 mL	0.3346 mL	1.6732 mL
100 mM	0.0167 mL	0.0837 mL	0.1673 mL	0.8366 mL

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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