PZ038
PF-06928215
≥98% (HPLC)
Synonym(s):
rel-(1R,2S)2(7-Oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3 carboxamido) cyclohexane-1-carboxylic acid, rel-(1R,2S)2(7-Oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carboxamido)cyclohexanecarboxylic acid
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About This Item
Empirical Formula (Hill Notation):
C20H20N4O4
CAS Number:
Molecular Weight:
380.40
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Product Name
PF-06928215, ≥98% (HPLC)
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
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 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.
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Subhadip Choudhuri et al.
PLoS pathogens, 16(4), e1008474-e1008474 (2020-04-22)
Trypanosoma cruzi (T. cruzi) is the etiological agent of Chagas cardiomyopathy. In the present study, we investigated the role of extracellular vesicles (Ev) in shaping the macrophage (Mφ) response in progressive Chagas disease (CD). We purified T. cruzi Ev (TcEv)
Structure of the human cGAS-DNA complex reveals enhanced control of immune surveillance
Zhou W, et al.
Cell, 174(2), 300-311 (2018)
Discovery of PF-06928215 as a high affinity inhibitor of cGAS enabled by a novel fluorescence polarization assay
Hall J, et al.
PLoS ONE, 12(9), e0184843-e0184843 (2017)
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