BAY41-4109 is a heteroaryldihydropyrimidine (HAP)-based capsid assembly modulator (CAM) that destabilizes hepatitis B virus (HBV) capsid assembly. BAY41-4109 inhibits HBV replication in HepG2.2.15 cultures with little host cytotoxicity (IC50 = 53 nM vs. CC50 = 7 μM in 8 days). Despite its relatively short half-life in vivo (plasma t1/2 = 5 h/dog, 2 h/rat, ≤1 h/mouse), BAY41-4109 shows greater antiviral efficacy than 3TC in Tg [HBV1.3 fsX-3′5′] mice (HBV DNA reduction = 52%/BAY vs. 36%/3TC in liver via 30 mg/kg b.i.d. p.o.; 70% vs. 30% in plasma with 15 mg BAY/kg or 30 mg/kg 3TC b.i.d. p.o., respectively) with good oral availability (F/tmax =31%/mouse, 58%/rat & dog).
Heteroaryldihydropyrimidine (HAP) capsid assembly modulator (CAM) that destabilizes hepatitis B virus (HBV) capsid assembly and replication in vitro & in vivo.
A cell-permeable pyrazolopyridinylpyrimidine compound that acts as a selective and potent stimulator of soluble guanylate cyclase (effective dose ~ 0.1 nM to 100 µM using recombinant soluble guanylate cyclase).
form
powder
form
powder
form
powder
form
solid
assay
≥98% (HPLC)
assay
≥97% (HPLC)
assay
≥98% (HPLC)
assay
≥98% (HPLC)
storage temp.
−20°C
storage temp.
2-8°C
storage temp.
2-8°C
storage temp.
2-8°C
solubility
DMSO: 2 mg/mL, clear
solubility
DMSO: 5 mg/mL, clear (warmed)
solubility
DMSO: 2 mg/mL, clear (warmed)
solubility
DMSO: 10 mg/mL
color
white to beige
color
white to light brown
color
white to very dark brown
color
white
Clase de almacenamiento
11 - Combustible Solids
¿Qué está pasando?
WGK 3
Punto de inflamación (°F)
Not applicable
Punto de inflamación (°C)
Not applicable
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