| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
|
Purity: ≥98%
Elexacaftor (VX-445, WHO-11180; WHO11180; VX445; Kaftrio; Trikafta) is one of three components in the fixed-dose combination medication (Elexacaftor/tezacaftor/ivacaftor, trade name: Trikafta and Kaftrio) used in patients who have cystic fibrosis with a F508del mutation. Elexacaftor is a potent and next-generation modulator of cystic fibrosis transmembrane conductance regulator (CFTR) that was designed to restore the function of Phe508del CFTR protein in patients who are diagnnosed with cystic fibrosis. Elexacaftor is administered with tezacaftor and ivacaftor as a three-drug cocktail (Elexacaftor–tezacaftor–ivacaftor).
| ln Vitro |
In order to restore Phe508del CFTR protein function, elexacaftor (VX-445) is a next-generation cystic fibrosis transmembrane regulator (CFTR) corrector. It may be possible to treat cystic fibrosis with elexacaftor (VX-445). When employed in tandem, VX-445-Tezacaftor-VX-770 greatly enhanced the Phe508del CFTR protein's processing, transport, and chloride ion transport while also increasing the quantity of each chemical to the degree that it was combined [2].
|
|---|---|
| References |
[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. |
| Molecular Formula |
C26H34F3N7O4S
|
|---|---|
| Molecular Weight |
597.6529
|
| Elemental Analysis |
C, 52.25 H, 5.73 F, 9.54 N, 16.41 O, 10.71 S, 5.36
|
| CAS # |
2216712-66-0
|
| Related CAS # |
(R)-Elexacaftor;2229860-99-3;Elexacaftor-d3;Elexacaftor-13C,d3
|
| SMILES |
O=C(C1=CC=C(N2N=C(OCC(C)(C)C(F)(F)F)C=C2)N=C1N3C(C)(C)C[C@H](C)C3)NS(=O)(C4=CN(C)N=C4C)=O
|
| InChi Key |
MVRHVFSOIWFBTE-INIZCTEOSA-N
|
| InChi Code |
InChI=1S/C26H34F3N7O4S/c1-16-12-25(5,6)35(13-16)22-18(23(37)33-41(38,39)19-14-34(7)31-17(19)2)8-9-20(30-22)36-11-10-21(32-36)40-15-24(3,4)26(27,28)29/h8-11,14,16H,12-13,15H2,1-7H3,(H,33,37)/t16-/m0/s1
|
| Chemical Name |
(S)-N-((1,3-dimethyl-1H-pyrazol-4-yl)sulfonyl)-6-(3-(3,3,3-trifluoro-2,2-dimethylpropoxy)-1H-pyrazol-1-yl)-2-(2,2,4-trimethylpyrrolidin-1-yl)nicotinamide
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~209.15 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.48 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.48 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.1673 mL | 0.8366 mL | 1.6732 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06331000 | Not yet recruiting | Drug: elexacaftor-tezacaftor-ivacaftor treatment |
Cystic Fibrosis | University Hospital, Strasbourg, France | March 2024 | |
| NCT05576324 | Recruiting | Drug: Elexacaftor / Ivacaftor / Tezacaftor | Cystic Fibrosis | University of Erlangen-Nürnberg Medical School |
December 30, 2020 | |
| NCT06184763 | Active, not recruiting | Other: 6-minute walk test | Cystic Fibrosis | Hospices Civils de Lyon | August 1, 2023 | |
| NCT06072365 | Completed | Other: nutritional intake questionnaire |
Cystic Fibrosis | University Hospital, Toulouse | October 21, 2021 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA