N106

• CAT Number: I011223
• CAS Number: 862974-25-2
• Molecular Formula: C17H14N4O3S
• Molecular Weight: 354.38
• Purity: ≥95%
• Synonyms: N-(4-methoxy-1,3-benzothiazol-2-yl)-5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-amine
• InChI: InChI=1S/C17H14N4O3S/c1-22-11-8-6-10(7-9-11)15-20-21-16(24-15)19-17-18-14-12(23-2)4-3-5-13(14)25-17/h3-9H,1-2H3,(H,18,19,21)
• InChIKey: FBCSWQRNKAYAGY-UHFFFAOYSA-N
• SMILES: COC1=CC=C(C=C1)C2=NN=C(O2)NC3=NC4=C(C=CC=C4S3)OC

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].
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].

Reference

[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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