Reagentes e instrumentos para imunologia, biologia celular e biologia molecular.
 
> Elexacaftor [2216712-66-0]

Elexacaftor [2216712-66-0]

Imprimir Imprimir
Please log in

Referência HY-111772-10mg

Tamanho : 10mg

Marca : MedChemExpress

Contactar o distribuidor local :


Telefone : +1 850 650 7790

Elexacaftor (VX-445, Compound 1) is a modulator of cystic fibrosis transmembrane conductance regulator (CFTR). Elexacaftor (VX-445, Compound 1) facilitates the processing and trafficking of CFTR to increase the amount of CFTR at the cell surface.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

Elexacaftor Chemical Structure

Elexacaftor Chemical Structure

CAS No. : 2216712-66-0

This product is a controlled substance and not for sale in your territory.

Based on 22 publication(s) in Google Scholar

Other Forms of Elexacaftor:

  • (R)-Elexacaftor In-stock
  • Elexacaftor-d3 In-stock
  • Elexacaftor-13C,d3 Obtenir un devis

    Elexacaftor purchased from MedChemExpress. Usage Cited in: J Cyst Fibros. 2022.

    Elexacaftor/Tezacaftor (elexa/teza; 3 μM/10 μM; 24 h) combination causes a significant increase in the expression of the mature protein, with no changes in the expression of the immature, core-glycosylated form (B band) in Epithelia.
    Description

    Elexacaftor (VX-445, Compound 1) is a modulator of cystic fibrosis transmembrane conductance regulator (CFTR). Elexacaftor (VX-445, Compound 1) facilitates the processing and trafficking of CFTR to increase the amount of CFTR at the cell surface[1].

    IC50 & Target

    CFTR[1].
    In Vitro

    Elexacaftor (VX-445) is a next-generation cystic fibrosis transmembrane conductance regulator (CFTR) corrector designed to restore Phe508del CFTR protein function. Elexacaftor (VX-445) has the potential to treat cystic fibrosis. VX-445-Tezacaftor-VX-770 significantly improves Phe508del CFTR protein processing, trafficking, and chloride transport to a greater extent than any two of these agents in dual combination[2].

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

    Elexacaftor Related Antibodies
    Essai clinique
    Masse moléculaire

    597.65

    Formule

    C26H34F3N7O4S
    CAS No.

    2216712-66-0
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC1(C)C[C@H](C)CN1C2=C(C(NS(C3=CN(C)N=C3C)(=O)=O)=O)C=CC(N4C=CC(OCC(C)(C(F)(F)F)C)=N4)=N2
    Livraison

    Room temperature in continental US; may vary elsewhere.
    Stockage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvant et solubilité
    In Vitro: 

    DMSO : 125 mg/mL (209.15 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 1.6732 mL 8.3661 mL 16.7322 mL
    5 mM 0.3346 mL 1.6732 mL 3.3464 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Calculateur de molarité

    • Calculateur de dilution

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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: ≥ 2.08 mg/mL (3.48 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% Corn Oil

      Solubility: ≥ 2.08 mg/mL (3.48 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 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 (20.8 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)

    g

    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).
    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.
    Pureté et documentation
    Références

    • [1]. Alexander Russell Abela, et al. MODULATOR OF THE CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR , PHARMACEUTICAL COMPOSITIONS , METHODS OF TREATMENT , AND PROCESS FOR MAKING THE MODULATOR. US 20180162839 A1.

      [2]. Keating D, et al. VX-445-Tezacaftor-VX-770 in Patients with Cystic Fibrosis and One or Two Phe508del Alleles. N Engl J Med. 2018 Oct 25;379(17):1612-1620.  [Content Brief]

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.6732 mL 8.3661 mL 16.7322 mL 41.8305 mL
    5 mM 0.3346 mL 1.6732 mL 3.3464 mL 8.3661 mL
    10 mM 0.1673 mL 0.8366 mL 1.6732 mL 4.1831 mL
    15 mM 0.1115 mL 0.5577 mL 1.1155 mL 2.7887 mL
    20 mM 0.0837 mL 0.4183 mL 0.8366 mL 2.0915 mL
    25 mM 0.0669 mL 0.3346 mL 0.6693 mL 1.6732 mL
    30 mM 0.0558 mL 0.2789 mL 0.5577 mL 1.3944 mL
    40 mM 0.0418 mL 0.2092 mL 0.4183 mL 1.0458 mL
    50 mM 0.0335 mL 0.1673 mL 0.3346 mL 0.8366 mL
    60 mM 0.0279 mL 0.1394 mL 0.2789 mL 0.6972 mL
    80 mM 0.0209 mL 0.1046 mL 0.2092 mL 0.5229 mL
    100 mM 0.0167 mL 0.0837 mL 0.1673 mL 0.4183 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    Elexacaftor Related Classifications

    Help & FAQs

    Keywords:

    Elexacaftor2216712-66-0VX-445VX445VX 445CFTRAutophagyCystic fibrosis transmembrane conductance regulatorCysticFibrosisInhibitorinhibitorinhibit

    Você também pode estar interessado nos seguintes produtos:



    Referência
    Descrição
    Cond.
    Price Bef. VAT
    A2664-5mg
    VX-661 [1152311-62-0]
     5mg