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PZ038 Sigma-Aldrich

PF-06928215

≥98% (HPLC)

Synonym: (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

  • Empirical Formula (Hill Notation) C20H20N4O4

  • Molecular Weight 380.40

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Properties

Related Categories Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, P-PH
assay   ≥98% (HPLC)
form   powder
color   white to beige
solubility   DMSO: 2 mg/mL, clear
storage temp.   room temp

Description

Legal Information

Sold for research purposes under agreement from Pfizer Inc.

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 μM; 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-β 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.

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport

Documents

Certificate of Analysis

Protocols & Articles
Peer-Reviewed Papers
15

References

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