SML3474

PF-06928215, cis-racemate

≥98% (HPLC)

• Sinonimo/i: Cis-2-(7-Oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3 carboxamido) cyclohexane-1-carboxylic acid, Cis-2-(7-Oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carboxamido)cyclohexanecarboxylic acid, PF-06928215 cis-enantiomers (1R,2S) and (1S,2R)
• Formula empirica (notazione di Hill): C₂₀H₂₀N₄O₄
• Numero CAS: 2570808-90-9
• Peso molecolare: 380.40
• Numero MDL: MFCD32644796
• Codice UNSPSC: 51111800
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥98% (HPLC)
• Stato: powder
• Colore: white to beige
• Solubilità: DMSO: 2 mg/mL, clear (Warmed)
• Temperatura di conservazione: 2-8°C
• Stringa SMILE: OC([C@H](CCCC1)[C@H]1NC(C2=C3N(N=C2)C(C=C(C4=CC=CC=C4)N3)=O)=O)=O

Descrizione

Azioni biochim/fisiol

PF-06928215 is a high affinity (KD of the (1R,2S) enantiomer = 200 nM) active site-targeting, substrate-competitive cyclic GMP-AMP synthase (cGAS) inhibitor (IC50 = 4.9 μM using the (1R,2S) enantiomer; 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. Note: this product contains the two cis-enantiomers (1R,2S) and (1S,2R).

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable