CDN 1163 Chemical Properties

Melting point:

87 - 89°C

storage temp. 

2-8°C

solubility 

Soluble in DMSO (>25 mg/ml)

form 

powder

color 

white to beige

Stability:

Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

CDN 1163 Usage And Synthesis

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.

storage

Store at RT

References

[1] SOOJEONG KANG. Small Molecular Allosteric Activator of the Sarco/Endoplasmic Reticulum Ca2+-ATPase (SERCA) Attenuates Diabetes and Metabolic Disorders.[J]. The Journal of Biological Chemistry, 2016, 291 10: 5185-5198. DOI:10.1074/jbc.m115.705012
[2] DAHL R. A new target for Parkinson’s disease: Small molecule SERCA activator CDN1163 ameliorates dyskinesia in 6-OHDA-lesioned rats[J]. Bioorganic & Medicinal Chemistry, 2017, 25 1: Pages 53-57. DOI:10.1016/j.bmc.2016.10.008
[3] RIZWAN QAISAR. Restoration of Sarcoplasmic Reticulum Ca2+ ATPase (SERCA) Activity Prevents Age-Related Muscle Atrophy and Weakness in Mice.[J]. International Journal of Molecular Sciences, 2020, 22 1. DOI:10.3390/ijms22010037
[4] JIAOJIAO PENG. Sarco/Endoplasmic Reticulum Ca2+ Transporting ATPase (SERCA) Modulates Autophagic, Inflammatory, and Mitochondrial Responses during Influenza A Virus Infection in Human Lung Cells.[J]. Journal of Virology, 2021, 95 10. DOI:10.1128/jvi.00217-21

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