MDL | - |
---|---|
Molecular Weight | 354.38 |
Molecular Formula | C17H14N4O3S |
SMILES | COC1=C2C(SC(NC3=NN=C(C4=CC=C(OC)C=C4)O3)=N2)=CC=C1 |
N106 is a first-in-class sarcoplasmic reticulum calcium ATPase (SERCA2a) SUMOylation activator. N106 directly activates the SUMO-activating enzyme, E1 ligase. N106 can be used for heart failure research [1] .
N106 treatment increases contractile properties of cultured rat cardiomyocytes. N106 increases cell contractility, calcium-transient SERCA2a's ATPase activity and SUMOylation within 10 min of exposure, and these effects are sustained at 24 h in cardiomyocytes [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In a murine model, the half-life of N106 is determined to be ∼65.4 min with a C
max
of ∼2.24 μM when the mice received 10 mg/kg of N106 by intravenous injection. The oral bioavailability (F%) is 56% and 50%, and terminal elimination half-life (t
1/2
) is 19 min
[1]
.
In vivo, N106 (10 mg/kg) increases cardiac SERCA2A SUMOylation, and significantly improves ventricular function in mice with heart failure
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Solid
Room temperature in continental US; may vary elsewhere.
Powder | -20°C | 3 years |
---|---|---|
In solvent | -80°C | 6 months |
-20°C | 1 month |
DMSO : 62.5 mg/mL ( 176.36 mM ; ultrasonic and warming and heat to 60°C)
Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 2.8218 mL | 14.1091 mL | 28.2183 mL |
5 mM | 0.5644 mL | 2.8218 mL | 5.6437 mL |
10 mM | 0.2822 mL | 1.4109 mL | 2.8218 mL |