Home Transmembrane Transporters CFTR activator GLPG1837

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GLPG1837 CFTR activator

Cat.No.S8698

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 CFTR activator Chemical Structure

Chemical Structure

Molecular Weight: 348.42

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 69 mg/mL (198.03 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble

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Mass Concentration Volume Molecular Weight
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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 348.42 Formula

C16H20N4O3S

 Storage (From the date of receipt)
CAS No. 1654725-02-6 -- Storage of Stock Solutions

Synonyms ABBV-974 Smiles CC1(CC2=C(C(O1)(C)C)SC(=C2C(=O)N)NC(=O)C3=CC=NN3)C

Mechanism of Action

Targets/IC50/Ki
CFTR(F508del)
3 nM(EC50)
CFTR(G551D)
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.
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 this compound 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 this chemical in rat is 67%. In dogs, F%>100.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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