862974-25-2

862974-25-2 structure

Name: N106
Chemical Name: 4-Methoxy-N-[5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl]-1,3-benzothiazol-2-amine
CAS Number: 862974-25-2
Molecular Formula: C₁₇H₁₄N₄O₃S
Molecular Weight: 354.383
Create Date: 2018-07-16 08:17:12
Modify Date: 2024-01-04 00:48:42
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].

Name	4-Methoxy-N-[5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl]-1,3-benzothiazol-2-amine
Synonyms	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

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.