Structure of CDN1163
CAS No.: 892711-75-0
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
CDN1163 is an allosteric sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) activator that improves Ca2+ homeostasis. CDN1163 attenuates diabetes and metabolic disorders.
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Batch number can be found on the product's label following the word 'Batch'.
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Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
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CAS No. : | 892711-75-0 |
Formula : | C20H20N2O2 |
M.W : | 320.39 |
SMILES Code : | O=C(NC1=C2N=C(C)C=CC2=CC=C1)C3=CC=C(OC(C)C)C=C3 |
MDL No. : | MFCD07177494 |
InChI Key : | GVGVYDCVFBGALZ-UHFFFAOYSA-N |
Pubchem ID : | 16016585 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
H1395 cells | 10 μM | 24 hours | CDN1163 attenuated mitochondrial dysfunction in IAV-infected H1395 cells. | PMC8139658 |
Mouse renal tubular epithelial cells (mRTECs) | 10 μM | 1 h pretreatment followed by 24 h treatment | CDN1163 restored Cd2+-induced reduction in ER Ca2+ content and decreased the expression of ER stress markers BiP, PDI, and apoptosis marker cleaved caspase-3 | PMC10053525 |
HT22 cells | 10 μM | 10 min | CDN1163 enhanced cytoplasmic Ca2+ clearance of SERCA2 mutants and attenuated hypo-glutamate-induced excitotoxicity | PMC9065279 |
Reconstituted proteoliposomes (containing SERCA1a isoform) | 10μM | 15 minutes | Confirmed direct interaction with SERCA protein showing ~26% increase in charge displacement | PMC8571031 |
Rabbit skeletal muscle SR vesicles | 10μM | 15 minutes | CDN1163 significantly enhanced ATP-dependent Ca2+ translocation by SERCA with ~30% increase in charge displacement | PMC8571031 |
Jurkat T lymphocytes | 10 µM | 20 min | Short-term exposure to CDN1163 significantly increased Ca2+ release responses induced by low-dose tBHQ, indicating enhanced Ca2+ release from the SERCA 3-regulated Ca2+ pool. | PMC11593871 |
HT22 mouse hippocampal neurons | 1 µM | 24 hours | CDN1163 significantly alleviated heat stress-induced calcium imbalance, reduced cytoplasmic Ca2+ levels and elevated ER Ca2+ levels, inhibited p-PERK and p-eIF2α protein expression, effectively attenuating endoplasmic reticulum stress and apoptosis. | PMC11167007 |
H9c2 cells | 10 μM | 24 hours | CDN1163 markedly abolished glucose-stimulated NFATc nuclear translocation, reduced resistin and nuclear NFATc expression, and increased AMPKα phosphorylation. | PMC6199245 |
HEK cells | 10 μM | 2-hour pretreatment followed by 16-hour exposure to H2O2 | To evaluate the rescue effect of CDN1163 on ER stress-induced cell death; CDN1163 significantly attenuated H2O2-stimulated cell death | PMC4777852 |
Jurkat T lymphocytes | 25 µM | 30 min | Short-term exposure to CDN1163 significantly inhibited Ca2+ uptake, suggesting SERCA function was suppressed. | PMC11593871 |
H2K-mdx myotubes | 100 μM | 30 minutes | CDN1163 significantly reduced cytosolic Ca2+ levels in H2K-mdx myotubes | PMC8170845 |
Lymphatic muscle cells (LMCs) | 5 μM | 48 hours | To evaluate the effect of CDN1163 on SERCA activity in insulin-resistant LMCs. Results showed that CDN1163 partially restored the contractile frequency of lymphatic vessels. | PMC7378550 |
Jurkat T lymphocytes | 10 µM | 72 h | Long-term exposure to CDN1163 increased Ca2+ store levels in the SERCA 2b pool but decreased store levels in the SERCA 3-regulated pool. | PMC11593871 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
C57BL/6 mice | Heat stress-induced cognitive impairment model | Intraperitoneal injection | 20 mg/kg | Once daily for 7 days | CDN1163 upregulated SERCA expression, restored Ca2+ homeostasis, improved learning and memory abilities, and alleviated hippocampal neuronal damage and endoplasmic reticulum stress-mediated apoptosis. | PMC11167007 |
Mice | CuZnSOD deficient Mice model | Intraperitoneal injection | 50 mg/kg | Three times per week for 7 weeks | CDN1163 completely restored SERCA activity and reversed the 23% reduction in gastrocnemius mass and 22% reduction in specific force in untreated Sod1-/- versus wild type mice. These changes were accompanied by restoration of autophagy protein markers to the levels found in wild-type mice. CDN1163 also reversed the increase in mitochondrial ROS generation and oxidative damage in muscle tissue from Sod1-/- mice. | PMC6174848 |
Mice | Wild-type (WT) and melanocortin-4 receptor knockout (Mc4r−/−) mice | Injections | 50 mg/kg | Once every 2 weeks for 8 weeks (four total doses); or three times per week for 8 weeks (24 total doses) | Studied the effects of CDN1163 on diet-induced steatohepatitis, showing that CDN1163 improved liver fibrosis and inflammation, restored glucose tolerance and insulin sensitivity, increased antioxidant enzyme expression, and decreased oxidative stress and ER stress gene expression. | PMC11179628 |
Mice | Diabetic Mice model (db/db mice) | Intraperitoneal injection | 100 mg/kg | 5 consecutive days | CDN1163 improved glucose tolerance, hepatosteatosis, skeletal muscle function, and insulin resistance in db/db mice. | PMC9099866 |
Wistar rats | Hindlimb unloading/suspension model | Intraperitoneal injection | 50 mg/kg | Once daily for 7 days | Treatment with SERCA activator CDN1163 during 7 days of unloading prevented an increase in soleus fatigue, the decrease of slow-type myosin, mitochondrial markers, and markers of calcium homeostasis but had no effect on muscle atrophy. | PMC10526198 |
C57BL/6J mice | Aged mice | Intra-peritoneal injection | 50 mg/kg | Three times per week for 10 months | CDN1163 treatment via diet and injection prevented age-related muscle atrophy and weakness, restored SERCA ATPase activity, and improved mitochondrial function. | PMC7792969 |
Ob/ob mice (obese/diabetic model) | Insulin resistance and type 2 diabetes model | Intraperitoneal injection | 50 mg/kg | Once daily for 5 consecutive days | To evaluate the effects of CDN1163 on blood glucose and metabolic parameters; CDN1163 significantly reduced fasting blood glucose, improved glucose tolerance, ameliorated hepatic steatosis, increased energy expenditure, and upregulated UCP1 and UCP3 expression in brown adipose tissue. Effects persisted for >6 weeks post-treatment. | PMC4777852 |
Mdx mice | Duchenne muscular dystrophy model | Intraperitoneal injection | 40 mg/kg | Three times per week for 7 weeks | CDN1163 ameliorated dystrophic phenotypes in mdx mice, including reduced muscle degeneration and fibrosis, enhanced muscle strength, and restored mitochondrial function | PMC8170845 |
Ob/ob mice | Diabetic mice model | Intraperitoneal injection | 50 mg/kg | 3× /week for 30 days | CDN1163 treatment significantly decreased resistin and nuclear NFATc protein expression and increased AMPKα activity/phosphorylation. | PMC6199245 |
Tags: CDN1163 | CDN 1163 | CDN-1163 | Calcium Channel | Ca2+ channels | Ca channels | 892711-75-0
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