1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. Calcium Channel
  3. CDN1163

CDN1163 

Cat. No.: HY-101455 Purity: 99.12%
Handling Instructions

CDN1163 is an allosteric sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) activator that improves Ca2+ homeostasis. CDN1163 attenuates diabetes and metabolic disorders.

For research use only. We do not sell to patients.

CDN1163 Chemical Structure

CDN1163 Chemical Structure

CAS No. : 892711-75-0

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10 mM * 1 mL in DMSO USD 77 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

CDN1163 is an allosteric sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) activator that improves Ca2+ homeostasis. CDN1163 attenuates diabetes and metabolic disorders[1].

IC50 & Target[1]

Ca2+

 

In Vitro

CDN1163 (5.5-25 mM; 0-8 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[2].

Western Blot Analysis[2]

Cell Line: Rat cardiac myocyte cells (H9c2)
Concentration: 5.5 mM, 25 mM
Incubation Time: 0 hour, 4 hours, 8 hours
Result: High glucose-induced resistin and nuclear NFATc expression were significantly reduced. The phosphorylation of AMPKα is increased in a time-dependent manner.
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[1].

Animal Model: Male 8-10-week old ob/ob mice and lean ob/+ mice[1]
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.
Molecular Weight

320.39

Formula

C₂₀H₂₀N₂O₂

CAS No.

892711-75-0

SMILES

O=C(NC1=C2N=C(C)C=CC2=CC=C1)C3=CC=C(OC(C)C)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (156.06 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.80 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (7.80 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.80 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

CDN1163CDN 1163CDN-1163Calcium ChannelCa2+ channelsCa channelsInhibitorinhibitorinhibit

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CDN1163
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HY-101455
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