N106

Names

[ Name ]:
N106

[Synonym ]:
2-Benzothiazolamine, 4-methoxy-N-[5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl]-
MFCD05892638
4-Methoxy-N-[5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl]-1,3-benzothiazol-2-amine

Biological Activity

[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].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Metabolic Enzyme/Protease >> E1/E2/E3 Enzyme

[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].

[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].

[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.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
545.4±56.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₇H₁₄N₄O₃S

[ Molecular Weight ]:
354.383

[ Flash Point ]:
283.6±31.8 °C

[ Exact Mass ]:
354.078674

[ LogP ]:
4.43

[ Vapour Pressure ]:
0.0±1.5 mmHg at 25°C

[ Index of Refraction ]:
1.681

[ Storage condition ]:
-20°C