2. Others Membrane Transporter/Ion Channel
  3. Drug Isomer CFTR
  4. (R)-Elexacaftor

(R)-Elexacaftor  (Synonyms: (R)-VX-445)

Cat. No.: HY-111772A Purity: 99.44%
COA
SDS
Handling Instructions Technical Support

(R)-Elexacaftor ((R)-VX-445) is the enantiomer of Elexacaftor (HY-111772). Elexacaftor is an orally active CFTR modulator that targets nucleotide-binding domain 1. Elexacaftor stabilizes misfolded F508del-CFTR protein, enhances its trafficking to the plasma membrane, and significantly improves metabolic stability, thermal stability and ion conductivity. Elexacaftor not only restores chloride transport function in nasal epithelial cells and rescues multiple CFTR mutation subtypes, but also exerts multiplicative synergistic effects with Ivacaftor (HY-13017), and is often used in a triple combination therapy with Tezacaftor (HY-15448). Elexacaftor is widely used in basic and clinical translational research on cystic fibrosis.

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

(R)-Elexacaftor

(R)-Elexacaftor Chemical Structure

CAS No. : 2229860-99-3

Size Price 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
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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

Other Forms of (R)-Elexacaftor:

(R)-Elexacaftor Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

(R)-Elexacaftor ((R)-VX-445) is the enantiomer of Elexacaftor (HY-111772). Elexacaftor is an orally active CFTR modulator that targets nucleotide-binding domain 1. Elexacaftor stabilizes misfolded F508del-CFTR protein, enhances its trafficking to the plasma membrane, and significantly improves metabolic stability, thermal stability and ion conductivity. Elexacaftor not only restores chloride transport function in nasal epithelial cells and rescues multiple CFTR mutation subtypes, but also exerts multiplicative synergistic effects with Ivacaftor (HY-13017), and is often used in a triple combination therapy with Tezacaftor (HY-15448). Elexacaftor is widely used in basic and clinical translational research on cystic fibrosis[1][2][3][4][5].

In Vitro

Combined treatment of CFBE41o-F508del-CFTR cells with Elexacaftor (3 μM; 24 h), Ivacaftor (HY-13017) and Tezacaftor (HY-15448) synergistically increases the proportion of mature F508del-CFTR, with maximum maturity observed after 24 h of treatment, although its level remains lower than that of wild-type CFTR[1].
When Elexacaftor (0.99 μM; 24 h) is used in combination with Ivacaftor (HY-13017) and Tezacaftor (HY-15448) to treat CFBE41o-F508del-CFTR cells, it maintains a maturation level of F508del-CFTR comparable to that achieved with the full dose of 3 μM, while lower concentrations reduce the maturation efficiency[1].

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

(R)-Elexacaftor Related Antibodies

Western Blot Analysis[4]

Cell Line: CFBE41o- cells expressing F508del-CFTR
Concentration: 3 μM (as part of ET or ETI); 0 μM (DMSO control)
Incubation Time: 2 h, 4 h, 6 h, 8 h, 24 h
Result: Reached C/(B+C) ratio of 0.32 (n = 5) after 2 h of ETI treatment, higher than 0.21 (n = 5) for ET treatment.
Reached C/(B+C) ratio of 0.60 (n = 5) for ETI and 0.73 (n = 5) for ET at 24 h.
Did not reach the WT-CFTR ratio of 0.96 (n = 5).

Western Blot Analysis[4]

Cell Line: CFBE41o- cells expressing F508del-CFTR
Concentration: 3 μM (100% ETI), 0.99 μM (33% ETI), 0.33 μM (11% ETI), 0.099 μM (3.3% ETI), 0.033 μM (1.1% ETI) (as part of ETI); 0 μM (DMSO control)
Incubation Time: 24 h
Result: Showed no significant difference in C/(B+C) ratio between 100% ETI (0.47) and 33% ETI (0.38, n = 4, p = 0.07).
Reduced the C/(B+C) ratio to ~50-60% of the 100% ETI level (0.24, n = 4, p = 0.003 vs. 100% ETI) at 11% ETI.
Resulted in very low C/(B+C) ratio indistinguishable from DMSO control at 3.3% and 1.1% ETI.
Molecular Weight

597.65

Formula

C26H34F3N7O4S
CAS No.
Appearance

Solid

Color

White to light yellow

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
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 : 100 mg/mL (167.32 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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.
Purity & Documentation
References

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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.

(R)-Elexacaftor 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:

(R)-Elexacaftor2229860-99-3(R)-VX-445Drug IsomerCFTRCystic fibrosis transmembrane conductance regulatorcystic fibrosis transmembrane conductance regulatorR117H-CFTRnucleotide binding domain 1non-CF human nasal epithelial cellsCFBE41o-F508del-CFTR cellsG551D-FRT cellsG551D-CFTRcystic fibrosisF508del-CFTRnasal epitheliumInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
(R)-Elexacaftor
Cat. No.:
HY-111772A
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (252 KB) Français - FR (252 KB) Deutsch - DE (252 KB) Norwegian - NO (252 KB) Español - ES (252 KB) Swedish - SV (252 KB) Italian - IT (252 KB) Korean - KR (252 KB) Portuguese - PT (252 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.