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  2. Isotope-Labeled Compounds
  3. Lumacaftor-d4

Lumacaftor-d4  (Synonyms: VX-809-d4; VRT 826809-d4)

Cat. No.: HY-13262S Purity: 99.95%
COA Handling Instructions

Lumacaftor-d4 is the deuterium labeled Lumacaftor (HY-13262)[1].

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

Lumacaftor-d<sub>4</sub> Chemical Structure

Lumacaftor-d4 Chemical Structure

CAS No. : 2733561-44-7

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1 mg USD 1020 In-stock
5 mg USD 2980 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Lumacaftor-d4:

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Description

Lumacaftor-d4 is the deuterium labeled Lumacaftor (HY-13262)[1].

In Vitro

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
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[2]. Lumacaftor produces a concentration-dependent increase in the HRP luminescence signal after incubation with cells at 37°C or 27°C in both cell lines, with a similar EC50 value of approximately 0.3 μM. In F508-HRP CFBE41o- cells at 37°C, Lumacaftor increases the signal maximally to approximately 250 luminescence arbitrary units (a.u.) over the DMSO control baseline of approximately 60 a.u., representing an approximately 4-fold signal increase. Similarly, with the R1070W-HRP CFBE41o- cells, Lumacaftor increases the signal maximally to approximately 220 a.u. over the DMSO control baseline of approximately 85 a.u., representing an approximately 2.5-fold signal increase. Therefore, both cell lines produced robust signals with a good dynamic range for high-throughput screening[3].

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

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[2].

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

Molecular Weight

456.43

Formula

C24H14D4F2N2O5

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC1(F)OC(C=C(C=C2)C3(C([2H])([2H])C3([2H])[2H])C(NC4=NC(C5=CC=CC(C(O)=O)=C5)=C(C=C4)C)=O)=C2O1

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 (219.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

DMSO : 25 mg/mL (54.77 mM; ultrasonic and warming and heat to 60°C; 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 2.1909 mL 10.9546 mL 21.9092 mL
5 mM 0.4382 mL 2.1909 mL 4.3818 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.

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

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
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 / DMSO 1 mM 2.1909 mL 10.9546 mL 21.9092 mL 54.7729 mL
5 mM 0.4382 mL 2.1909 mL 4.3818 mL 10.9546 mL
10 mM 0.2191 mL 1.0955 mL 2.1909 mL 5.4773 mL
15 mM 0.1461 mL 0.7303 mL 1.4606 mL 3.6515 mL
20 mM 0.1095 mL 0.5477 mL 1.0955 mL 2.7386 mL
25 mM 0.0876 mL 0.4382 mL 0.8764 mL 2.1909 mL
30 mM 0.0730 mL 0.3652 mL 0.7303 mL 1.8258 mL
40 mM 0.0548 mL 0.2739 mL 0.5477 mL 1.3693 mL
50 mM 0.0438 mL 0.2191 mL 0.4382 mL 1.0955 mL
DMSO 60 mM 0.0365 mL 0.1826 mL 0.3652 mL 0.9129 mL
80 mM 0.0274 mL 0.1369 mL 0.2739 mL 0.6847 mL
100 mM 0.0219 mL 0.1095 mL 0.2191 mL 0.5477 mL
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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.

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Product Name:
Lumacaftor-d4
Cat. No.:
HY-13262S
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