GLPG1837

For research use only.

Catalog No.S8698 Synonyms: ABBV-974

1 publication

GLPG1837 Chemical Structure

CAS No. 1654725-02-6

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.

Selleck's GLPG1837 has been cited by 1 publication

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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

Solubility (25°C)

In vitro DMSO 69 mg/mL (198.03 mM)
Water Insoluble
Ethanol '5 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 348.42
Formula

C16H20N4O3S

CAS No. 1654725-02-6
Storage powder
in solvent
Synonyms ABBV-974
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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Molarity Calculator

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

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Molecular Weight Calculator

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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

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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CFTR Signaling Pathway Map

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