Description
CDN1163 (892711-75-0) is an allosteric activator of the sarco/endoplasmic reticulum Ca2+-ATPase (SERCA).1,2? It lowered fasting glucose levels, improved glucose tolerance, and ameliorated hepatitis steatosis in ob/ob mice.1?? CDN1163 also rescued neurons from ER-stress-induced cell death in vitro and displayed significant efficacy in a rat 6-hydroxydopamine (6-OHDA) model of Parkinson’s disease.2 It reduced age-related muscle atrophy and weakness in a C57BL/6J mice.3? CDN1163 decreased inflammatory cytokines and chemokines and attenuated mitochondrial dysfunction in Influenza A infected H1395 cells.4
Uses
4-(1-Methylethoxy)-N-(2-methyl-8-quinolinyl)benzamide is an allosteric activator that increases Ca2+-ATPase activity and Ca2+ uptake by ER microsomes. 4-(1-Methylethoxy)-N-(2-methyl-8-quinolinyl)benzamide may have therapeutic potential for treating type-2 diabetes and metabolic dysfunction.
Definition
ChEBI: CDN1163 is a secondary carboxamide resulting from the formal condensation of the carboxy group of 4-isopropoxybenzoic acid with the primary amino group of 2-methylquinolin-8-amine. An allosteric activator of sarco/endoplasmic reticulum Ca(2+)-ATPase (SERCA). It has a role as a SERCA activator. It is a member of quinolines, a secondary carboxamide and an aromatic ether.
Biochem/physiol Actions
CDN1163 is an allosteric activator of sarco/ endoplasmic reticulum Ca2+-ATPase (SERCA) that potently lowered fasting blood glucose, improved glucose tolerance and ameliorated hepatosteatosis in ob/ob mice. Additionally CDN1163 induces significant reduction in adipose tissue weight with no change in lean mass in ob/ob mice. CDN1163 has no effect on glucose levels or body weight in lean control mice.
References
Kang et al. (2016), Small Molecular Allosteric Activator of the Sarco/Endoplasmic Reticulum Ca2+-ATPase (SERCA) Attenuates Diabetes and Metabolic Disorders; J. Biol. 291 5185
Dahl (2017), A new target for Parkinson’s disease: Small molecule SERCA activator CDN1163 ameliorates dyskinesia in 6-OHDA-lesioned rats; Bioorg. Med. Chem. 25 53
Qaisar et al. (2020), Restoration of Sarcoplasmic Reticulum Ca2+ ATPase (SERCA) Activity Prevents Age-Related Muscle Atrophy and Weakness in Mice; Int. J. Mol. Sci. 22 37
Peng et al. (2021), Sarco/Endoplasmic Reticulum Ca2+ Transporting ATPase (SERCA) Modulates Autophagic, Inflammatory, and Mitochondrial Responses during Influenza A Virus Infection in Human Lung Cells; J. Virol. 1128/JVI00217-21
