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PZ038

Sigma-Aldrich

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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5 MG
$102.60
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$305.20

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5 MG
$102.60
25 MG
$305.20

About This Item

Empirical Formula (Hill Notation):
C20H20N4O4
CAS Number:
2570808-90-9
Molecular Weight:
380.40
MDL number:
MFCD32644796
UNSPSC Code:
12352200
NACRES:
NA.77

$102.60

List Price$108.00Save 5%
Web-Only Promotion

Available to ship onApril 15, 2025Details

Request a Bulk Order

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).[1][2]

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.

pictograms

Exclamation mark
GHS07

signalword

Warning

hcodes

H302

Hazard Classifications

Acute Tox. 4 Oral

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000231317
0000282308
0000282309

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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)
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)

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