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25mg |
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Purity: ≥98%
CDN-1163 is a small molecule activator of sarco/endoplasmic reticulum Ca2+-ATPase (SERCA). CDN-1163 increases ER calcium content, rescues neurons from ER stress-induced cell death in vitro, and shows significant efficacy in the rat 6-hydroxydopamine (6-OHDA) model of Parkinson's disease.
ln Vitro |
Treatment with CDN1163 (10 μM; 24 hours; rat cardiomyocytes) decreases nuclear NFATc and resistin expression produced by high hyperglycemia and, in a time-dependent way, enhances AMPKα phosphorylation [2].
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ln Vivo |
Male ob/ob and lean ob/+ mice were given 50 mg/kg of CDN1163 intraperitoneally (i.p.) for five days. This treatment improved hepatic Ca2+ transport activity, decreased endoplasmic reticulum (ER) stress-induced cell death in vitro, and increased SERCA2 Ca2+-ATPase activity. In ob/ob mice, CDN1163 lowers blood glucose levels, enhances metabolic parameters and gluconeogenesis gene expression, reverses hepatic steatosis, prevents ER stress and ER stress-induced apoptosis, and boosts mitochondrial efficiency [1].
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Cell Assay |
Western Blot analysis [2]
Cell Types: rat cardiomyocytes (H9c2) Tested Concentrations: 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: High glucose-induced resistin and nuclear NFATc expression were Dramatically diminished. Phosphorylation of AMPKα increases in a time-dependent manner. |
Animal Protocol |
Animal/Disease Models: Male 8-10 week old ob/ob mice and lean ob/+ mice [1]
Doses: 50 mg/kg Route of Administration: intraperitoneal (ip) injection; continued for 5 days Experimental Results: Dramatically diminished fasting blood glucose and improved Glucose tolerance, improves hepatic steatosis but does not change blood glucose levels or body weight. The expression of uncoupling protein 1 (UCP1) and UCP3 in brown adipose tissue increases, and the hepatic expression of genes involved in gluconeogenesis and lipogenesis is diminished, attenuating the ER stress response and ER stress-induced apoptosis, and may Improved mitochondrial biogenesis through SERCA2-mediated activation of the AMP-activated protein kinase pathway. |
References |
[1]. Kang S, et al. Small Molecular Allosteric Activator of the Sarco/Endoplasmic Reticulum Ca2+-ATPase (SERCA) Attenuates Diabetes and Metabolic Disorders. J Biol Chem. 2016 Mar 4;291(10):5185-98.
[2]. Singh R, et al. A role for calcium in resistin transcriptional activation in diabetic hearts. Sci Rep. 2018 Oct 23;8(1):15633. |
Molecular Formula |
C20H20N2O2
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Molecular Weight |
320.39
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Exact Mass |
320.1525
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CAS # |
892711-75-0
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Related CAS # |
892711-75-0
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C(NC1=C2N=C(C)C=CC2=CC=C1)C3=CC=C(OC(C)C)C=C3
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Chemical Name |
4-(1-Methylethoxy)-N-(2-methyl-8-quinolinyl)benzamide
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Synonyms |
CDN 1163 CDN1163CDN-1163
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~100 mg/mL (~312.12 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.80 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (7.80 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.80 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.1212 mL | 15.6060 mL | 31.2120 mL | |
5 mM | 0.6242 mL | 3.1212 mL | 6.2424 mL | |
10 mM | 0.3121 mL | 1.5606 mL | 3.1212 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.