Synonyms: (1R,2S)-2-(7-Oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3 carboxamido) cyclohexane-1-carboxylic acid; (1R,2S)-2-(7-Oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carboxamido)cyclohexanecarboxylic acid
Molecular Formula: C20H20N4O4
Molecular Weight: 380.4
Linear Structural Formula: C20H20N4O4
Purity: >=98% (HPLC)
Storage: room temp
Application: PF-06928215 has been used to study its inhibitory effects on cyclic GMP-AMP synthase (cGAS).
Biochem Physiol Actions: PF-06928215 is a high affinity (KD = 200 nM) active site-targeting, substrate-competitive cyclic GMP-AMP synthase (cGAS) inhibitor (IC50 = 4.9 muM; in the presence of 1 mM ATP, 0.3 mM GTP, 100 nM 45-bp interferon-stimulatory dsDNA (ISD)). PF-06928215 displays no inhibitory potency against dsDNA-induced IFN-beta expression in cellular cGAS assays, most likely due to limited cell-permeability and/or high levels of cellular ATP and GTP in the reporter cells employed.
Legal Information: Sold for research purposes under agreement from Pfizer Inc.