Lumacaftor (VX-809; VRT 826809)
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 500mg | $245 | Check With Us |
| 1g | $445 | Check With Us |
| 5g | $1200 | Check With Us |
: Cat #: V1690 CAS #: 936727-05-8 Purity ≥ 98%
Description: Lumacaftor (formerly VX809; VRT-826809; VRT826809; VX-809; Orkambi) is a potent and orally bioavailable CFTR (cystic fibrosis transmembrane conductance regulator) corrector with antifibrotic effects.
Top Publications Citing Invivochem Products
Publications Citing InvivoChem Products
Product Promise
- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 452.41 |
|---|---|
| Molecular Formula | C24H18F2N2O5 |
| CAS No. | 936727-05-8 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 90 mg/mL (198.9 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: 6 mg/mL (13.3 mM) | |
| Solubility In Vivo | 30% PEG400+0.5% Tween80+5% Propylene glycol: 30 mg/mL |
| Synonyms | VRT-826809; VX-809; VRT 826809; VX809; VRT826809; VX 809; Lumacaftor; Orkambi |
| Protocol | In Vitro | In fischer rat thyroid (FRT) cells, Lumacaftor improves F508del-CFTR maturation by 7.1±0.3 fold (n=3) compared with vehicle-treated cells (EC50, 0.1±0.1 μM; n=3) and enhances F508del-CFTR-mediated chloride transport by approximately fivefold (EC50, 0.5±0.1 μM; n=3). At Lumacaftor concentrations greater than 10 μM, the response is reduced, resulting in a bell-shaped dose-response relationship with an IC50 of approximately 100 μM. Lumacaftor is orally bioavailable in rats and achieved in vivo plasma levels significantly above concentrations required for in vitro efficacy |
|---|---|---|
| In Vivo | Oral dosing of 1 mg/kg Lumacaftor in male Sprague-Dawley rats results in a Cmax of 2.4±1.3 μM with a t1/2 of 7.7±0.4 h (mean±SD; n=3), indicating that that Lumacaftor is orally bioavailable and able to reach plasma levels that significantly exceeded EC50s for F508del-CFTR correction |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.2104 mL | 11.0519 mL | 22.1038 mL | 44.2077 mL |
| 5mM | 0.4421 mL | 2.2104 mL | 4.4208 mL | 8.8415 mL |
| 10mM | 0.2210 mL | 1.1052 mL | 2.2104 mL | 4.4208 mL |
| 20mM | 0.1105 mL | 0.5526 mL | 1.1052 mL | 2.2104 mL |
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start)
×
Volume(start)
=
Concentration(final)
×
Volume(final)
This equation is commonly abbreviated as: C1 V1 = C2 V2
Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg
Average weight of animals g
Dosing volume per animal µL
Number of animals
Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
DMSO(Master liquid 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 master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (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.