GLPG1837

Catalog No.S8698 Synonyms: ABBV-974

For research use only.

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

CAS No. 1654725-02-6

Selleck's GLPG1837 has been cited by 2 Publications

Purity & Quality Control

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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

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 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].

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 348.42
Formula

C16H20N4O3S

CAS No. 1654725-02-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1(CC2=C(C(O1)(C)C)SC(=C2C(=O)N)NC(=O)C3=CC=NN3)C

In vivo Formulation Calculator (Clear solution)

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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02690519 Completed Drug: GLPG1837 dose 1|Drug: GLPG1837 dose 2 Cystic Fibrosis Galapagos NV January 2016 Phase 2
NCT02562950 Completed Drug: GLPG1837 500 mg|Drug: Midazolam|Drug: GLPG1837 1000 mg Healthy Galapagos NV September 2015 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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