2. Membrane Transporter/Ion Channel Autophagy
  3. CFTR Autophagy
  4. GLPG1837

GLPG1837 is a potent and reversible CFTR potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively.

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

GLPG1837 Chemical Structure

GLPG1837 Chemical Structure

CAS No. : 1654725-02-6

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Based on 1 publication(s) in Google Scholar

GLPG1837 Related Antibodies

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Description

GLPG1837 is a potent and reversible CFTR potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively.

IC50 & Target

EC50: 3 nM (F508del CFTR), 339 nM (G551D CFTR)[1]
In Vitro

GLPG1837 is a potent CFTR potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively. GLPG1837 increases the conductivity of the G551D CFTR channel with obtained potency of 181 nM[1]. GLPG1837 is reversible CFTR potentiator, with a the apparent affinity within a range of 0.2∼2 µM[2].

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

GLPG1837 Related Antibodies
Clinical Trial
Molecular Weight

348.42

Formula

C16H20N4O3S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=NNC=C1)NC(S2)=C(C(N)=O)C3=C2C(C)(C)OC(C)(C)C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 250 mg/mL (717.52 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8701 mL 14.3505 mL 28.7010 mL
5 mM 0.5740 mL 2.8701 mL 5.7402 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Working solution concentration: mg/mL
Purity & Documentation
References
Cell Assay
[1]

CFBe41o- cells are cultured in Eagle’s Minimal Essential Medium (MEM) supplemented with 10% fetal bovine serum (FBS), 1% penicillin/streptomycin, 1% l-glutamine, and 500 μg/mL hygromycin B. The cells are grown on culture flasks coated with 0.01% bovine serum albumin (BSA), 30 μg/mL Purecol, and 0.001% human fibronectin. CFBe41o- cells are transduced with adenoviruses containing F508del CFTR and YFP (H148Q/I152L/F47L). HEK293 cells are cultured in Dulbecco’s Modified Eagle Medium (DMEM) supplemented with 10% FBS and 1% penicillin/streptomycin. HEK293 cells are transfected with plasmids containing G551D, G178R, S549N, R117H, CFTR, and YFP (H148Q/I152L/F47L). Directly after transfection, the HEK293 cells are seeded in black 96-well plates coated with poly-d-lysine at a density of 70000 cells per well. The next day, cells are incubated for 24 h at 27°C (CFBE41o−) or 37°C (HEK293). Then cells are treated for 10 min with 10 μM forskolin and the desired concentration of potentiator at room temperature.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8701 mL 14.3505 mL 28.7010 mL 71.7525 mL
5 mM 0.5740 mL 2.8701 mL 5.7402 mL 14.3505 mL
10 mM 0.2870 mL 1.4350 mL 2.8701 mL 7.1752 mL
15 mM 0.1913 mL 0.9567 mL 1.9134 mL 4.7835 mL
20 mM 0.1435 mL 0.7175 mL 1.4350 mL 3.5876 mL
25 mM 0.1148 mL 0.5740 mL 1.1480 mL 2.8701 mL
30 mM 0.0957 mL 0.4783 mL 0.9567 mL 2.3917 mL
40 mM 0.0718 mL 0.3588 mL 0.7175 mL 1.7938 mL
50 mM 0.0574 mL 0.2870 mL 0.5740 mL 1.4350 mL
60 mM 0.0478 mL 0.2392 mL 0.4783 mL 1.1959 mL
80 mM 0.0359 mL 0.1794 mL 0.3588 mL 0.8969 mL
100 mM 0.0287 mL 0.1435 mL 0.2870 mL 0.7175 mL
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GLPG1837 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:

GLPG18371654725-02-6ABBV-974GLPG 1837GLPG-1837ABBV974ABBV 974CFTRAutophagyCystic fibrosis transmembrane conductance regulatorInhibitorinhibitorinhibit

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