PZ038

PF-06928215

≥98% (HPLC)

• Synonym(e): 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
• Empirische Formel (Hill-System): C₂₀H₂₀N₄O₄
• CAS-Nummer: 2570808-90-9
• Molekulargewicht: 380.40
• MDL-Nummer: MFCD32644796
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥98% (HPLC)
• Form: powder
• Farbe: white to beige
• Löslichkeit: DMSO: 2 mg/mL, clear
• Lagertemp.: room temp

Beschreibung

Anwendung

PF-06928215 has been used to study its inhibitory effects on cyclic GMP-AMP synthase (cGAS).

Biochem./physiol. Wirkung

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.

Sicherheitshinweise

• Piktogramme: GHS07
• Signalwort: Warning
• H-Sätze: H302
• P-Sätze: P264 - P270 - P301 + P312 - P501
• Gefahreneinstufungen: Acute Tox. 4 Oral
• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable