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GLPG1837

Catalog No. T7083 CAS 1654725-02-6

Synonyms: ABBV-974

GLPG1837 is an effective <a href="/target/CFTR" style="display: inline; color: #c13a36">CFTR</a> potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D <a href="/target/CFTR" style="display: inline; color: #c13a36">CFTR</a>, respectively.

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GLPG1837, CAS 1654725-02-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 54.00
2 mg	In stock	$ 64.00
5 mg	In stock	$ 117.00
10 mg	In stock	$ 158.00
1 mL * 10 mM (in DMSO)	In stock	$ 90.00

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Purity: 99.73%

Purity: 98%

Biological Description

Chemical Properties

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Description	GLPG1837 is an effective CFTR potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively.
Targets&IC50	G551D CFTR:339 nM (EC50), F508del CFTR:3 nM (EC50)
In vitro	GLPG1837 increases the conductivity of the G551D CFTR channel with the obtained potency of 181 nM[1]. GLPG1837 is reversible CFTR potentiator, with the apparent affinity within a range of 0.2～2 μM[2].
Cell Research	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.

Synonyms	ABBV-974
Molecular Weight	348.42
Formula	C16H20N4O3S
CAS No.	1654725-02-6

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 60 mg/mL

H2O: Insoluble

Ethanol: 5 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Van der Plas SE, et al. Discovery of N-(3-Carbamoyl-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-2-yl)-lH-pyrazole-5-carboxamide (GLPG1837), a Novel Potentiator Which Can Open Class III Mutant Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Channels to a High Extent. J Med Chem. 2018 Feb 22;61(4):1425-1435. 2. Yeh HI, et al. A common mechanism for CFTR potentiators. J Gen Physiol. 2017 Dec 4;149(12):1105-1118.

Related compound libraries

This product is contained In the following compound libraries：

Clinical Compound Library Ion Channel Inhibitor Library Orally Active Compound Library Bioactive Compound Library Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Bioactive Compounds Library Max Autophagy Compound Library Anti-Cancer Compound Library

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Keywords

GLPG1837 1654725-02-6 Autophagy Membrane transporter/Ion channel CFTR GLPG-1837 ABBV 974 Cystic fibrosis transmembrane conductance regulator Inhibitor inhibit GLPG 1837 ABBV-974 ABBV974 inhibitor

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