| Description |
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].
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| Related Catalog |
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| In Vitro |
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].
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| In Vivo |
In a murine model, the half-life of N106 is determined to be ∼65.4 min with a Cmax 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 (t1/2) 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].
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| References |
[1]. Changwon Kho, et al. Small-molecule activation of SERCA2a SUMOylation for the treatment of heart failure. Nat Commun. 2015 Jun 12;6:7229.
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