Home Transmembrane Transporters CFTR activator GLPG1837 For research use only.

GLPG1837

Synonyms: ABBV-974

GLPG1837 (ABBV-974) is a novel CFTR potentiator with an EC50 value of 3 nM for F508del, showing enhanced efficacy on CFTR mutants harboring class III mutations compared to Ivacaftor.

GLPG1837 Chemical Structure

GLPG1837 Chemical Structure

CAS No. 1654725-02-6

Purity & Quality Control

Batch: S869801 DMSO]69 mg/mL]false]Ethanol]5 mg/mL]false]Water]Insoluble]false Purity: 99.55%
99.55

GLPG1837 Related Products

Signaling Pathway

CFTR Signaling Pathways

CFTR Signaling Pathway

Biological Activity

Description GLPG1837 (ABBV-974) is a novel CFTR potentiator with an EC50 value of 3 nM for F508del, showing enhanced efficacy on CFTR mutants harboring class III mutations compared to Ivacaftor.
Targets
CFTR(F508del) [1] CFTR(G551D) [1]
3 nM(EC50) 339 nM(EC50)
In vitro
In vitro GLPG1837 has an attractive in vitro ADME profile, showing low Clint,unb in both microsomal and hepatocytes stability assays, good permeability, and no off-target inhibition of CYPs and the hERG channel[1].
In Vivo
In vivo The pharmacokinetic profile of GLPG1837 is attractive, showing a low Cl,unb and good F% in both rat and dog. The CL (L/h/kg) of GLPG1837 after intravenous injection of 1 mg/kg dose are 1.92 and 0.32 in rats and dogs, respectively. T1/2 is 1.84 h in rats while 3 h in dogs. After 5 mg/kg p.o, the oral availability of GLPG1837 in rat is 67%. In dogs, F%>100[1].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02690519 Completed
Cystic Fibrosis
Galapagos NV
 January 2016 Phase 2
NCT02562950 Completed
Healthy
Galapagos NV
 September 2015 Phase 1

Chemical Information & Solubility

Molecular Weight 348.42 Formula

C16H20N4O3S
CAS No. 1654725-02-6 SDF --
Smiles CC1(CC2=C(C(O1)(C)C)SC(=C2C(=O)N)NC(=O)C3=CC=NN3)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 69 mg/mL ( (198.03 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble


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In vivo
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In vivo Formulation Calculator

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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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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