CDN1163

SKU: orb1223730

Description

CDN1163 (CDN-1163) is a small molecule, allosteric activator of SERCA2, dose-dependently increases the Vmax of SERCA2 Ca2+-ATPase activity in ER microsomes; increases Ca2+-ATPase activity and significantly enhances Ca2+ uptake into the ER, attenuates H2O2-stimulated cell death in HEK cells; improves glucose homeostasis and metabolic parameters, increases glucose tolerance in ob/ob mice; CDN1163 reduces lipid accumulation and decreases lipogenesis in obese mice livers.

Key Properties

• CAS Number: 892711-75-0
• MW: 320.392
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₀N₂O₂
• SMILES: O=C(NC1=C2N=C(C)C=CC2=CC=C1)C3=CC=C(OC(C)C)C=C3
• Target: Calcium Channel
• Solubility: DMSO : 50 mg/mL 156.06 mM; H2O : < 0.1 mg/mL

Bioactivity

• In Vivo:
  CDN1163 (50 mg/kg; intraperitoneal injection; for 5 days; male ob/ob mice and lean ob/+ mice) increases SERCA2 Ca2+-ATPase activity, decreases endoplasmic reticulum (ER) stress-induced cell death in vitro and improves liver Ca2+ transport activity. CDN1163 reduces blood glucose levels and improves metabolic parameters and gluconeogenic gene expression, reverses hepatic steatosis, inhibits ER stress and ER stress-induced apoptosis, and improves mitochondrial efficiency in ob/ob mice In vivo. Animal model: Male 8-10-week old ob/ob mice and lean ob/+ mice. Dosage: 50 mg/kg. Administration: Intraperitoneal injection; for 5 days. Result: Markedly lowered fasting blood glucose, improved glucose tolerance, and ameliorated hepatosteatosis but did not alter glucose levels or body weight. Increased expression of uncoupling protein 1 (UCP1) and UCP3 in brown adipose tissue and reduced the hepatic expression of genes involved in gluconeogenesis and lipogenesis, attenuated ER stress response and ER stress-induced apoptosis, and improved mitochondrial biogenesis, possibly through SERCA2-mediated activation of AMP-activated protein kinase pathway.
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• In Vitro:
  CDN1163 (10 μM; 24 hours; rat cardiac myocyte cells) treatment reduces high glucose-induced resistin and nuclear NFATc expression and increases the phosphorylation of AMPKα in a time-dependent manner. Western blot analysis. Cell line: Rat cardiac myocyte cells (H9c2). Concentration: 10 μM. Incubation time: 24 hours. Result: High glucose-induced resistin and nuclear NFATc expression are significantly reduced. The phosphorylation of AMPKα is increased in a time-dependent manner.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CDN 1163 | CDN-1163

Quick Database Links

Gene Symbol

Calcium Channel