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GJG057

Chemical Structure : GJG057

CAS No.: 2761767-18-2

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GJG057 (GJG-057)

Catalog No.: PC-23998Not For Human Use, Lab Use Only.

GJG057 is a potent, selective and orally bioavailable inhibitor of leukotriene C4 synthase (LTC4S) with IC50 of 44 nM in whole blood LTC4 release assay and 14 nM in enzymatic assays.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

GJG057 is a potent, selective and orally bioavailable inhibitor of leukotriene C4 synthase (LTC4S) with IC50 of 44 nM in whole blood LTC4 release assay and 14 nM in enzymatic assays.
GJG057 is over 40 times more potent than AZD9898.
GJG057 shows promising selectivity against a broad panel of receptors, enzymes, transporters, and channels with all IC50 values >10 μM.
GJG057 shows efficacy in a murine asthma exacerbation model as well as in a mastoparan-induced skin challenge PK/PD model.

Physicochemical Properties

M.Wt 456.42
Formula C21H21F5N4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

1-(3,4-Difluorophenyl)-9-(6-(2,2,2-trifluoroethoxy)pyrimidin-4-yl)-1,9-diazaspiro[5.5]undecan-2-one

References

1. Thoma G, et al. J Med Chem. 2025 Feb 17. doi: 10.1021/acs.jmedchem.4c02897.

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