Ivacaftor [873054-44-5]
Référence HY-13017-5mg
Conditionnement : 5mg
Marque : MedChemExpress
Ivacaftor (VX-770) is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively.
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Ivacaftor Chemical Structure
CAS No. : 873054-44-5
This product is a controlled substance and not for sale in your territory.
Based on 5 publication(s) in Google Scholar
Other Forms of Ivacaftor:
- Ivacaftor-d9 In-stock
- Ivacaftor-d4 In-stock
- Ivacaftor benzenesulfonate Obtenir un devis
- Ivacaftor hydrate Obtenir un devis
- Ivacaftor-d19 Obtenir un devis
- Ivacaftor-d18 Obtenir un devis
Description |
Ivacaftor (VX-770) is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively. |
IC50 & Target |
EC50: 100 nM (G551D-CFTR), 25 nM (F508del-CFTR)[1] |
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In Vitro |
Ivacaftor (10 µM) increases the PC secretion activity by 3-fold for ABCB4-G535D, 13.7-fold for ABCB4-G536R, 6.7-fold for ABCB4-S1076C, 9.4-fold for ABCB4-S1176L, and 5.7-fold for ABCB4-G1178S. Ivacaftor corrects the functional defect of ABCB4 mutants[1]. Ivacaftor (10 μM) significantly increases CFTR activity in W1282X-expressing cells compared to R1162X CFTR cells[2]. Ivacaftor shows no significant activity against 160 targets tested including the GABAA benzodiazepine receptor. Ivacaftor increases the chloride secretion with an EC50 of 0.236 ± 0.200 μM, a 10-fold shift in potency compared to the F508del HBEs[3]. In recombinant cells, VX-770 increases CFTR channel open probability (Po) in both the F508del processing mutation and the G551D gating mutation. VX-770 increases forskolin-stimulated IT in temperature-corrected F508del-FRT cells by appr 6-fold with an EC50 of 25 nM[4]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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In Vivo |
Ivacaftor (1-200 mg/kg, p.o.) exhibits good oral bioavailability in rat[3]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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Essai clinique |
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Masse moléculaire |
392.49 |
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Formule |
C24H28N2O3 |
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CAS No. |
873054-44-5 |
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Appearance |
Solid |
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Color |
White to off-white |
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SMILES |
CC(C)(C1=C(C=C(C(C(C)(C)C)=C1)O)NC(C2=CNC3=C(C2=O)C=CC=C3)=O)C |
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Livraison | Room temperature in continental US; may vary elsewhere. |
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Stockage |
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Solvant et solubilité |
In Vitro:
DMSO : 50 mg/mL (127.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) Preparing
Stock Solutions
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.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 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:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume 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
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.
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Pureté et documentation |
Purity: 99.90% |
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Références |
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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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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DMSO | 1 mM | 2.5478 mL | 12.7392 mL | 25.4784 mL | 63.6959 mL |
5 mM | 0.5096 mL | 2.5478 mL | 5.0957 mL | 12.7392 mL | |
10 mM | 0.2548 mL | 1.2739 mL | 2.5478 mL | 6.3696 mL | |
15 mM | 0.1699 mL | 0.8493 mL | 1.6986 mL | 4.2464 mL | |
20 mM | 0.1274 mL | 0.6370 mL | 1.2739 mL | 3.1848 mL | |
25 mM | 0.1019 mL | 0.5096 mL | 1.0191 mL | 2.5478 mL | |
30 mM | 0.0849 mL | 0.4246 mL | 0.8493 mL | 2.1232 mL | |
40 mM | 0.0637 mL | 0.3185 mL | 0.6370 mL | 1.5924 mL | |
50 mM | 0.0510 mL | 0.2548 mL | 0.5096 mL | 1.2739 mL | |
60 mM | 0.0425 mL | 0.2123 mL | 0.4246 mL | 1.0616 mL | |
80 mM | 0.0318 mL | 0.1592 mL | 0.3185 mL | 0.7962 mL | |
100 mM | 0.0255 mL | 0.1274 mL | 0.2548 mL | 0.6370 mL |