CDN-1163 | CAS#892711-75-0 | SERCA activator

MedKoo Cat#: 561360 | Name: CDN-1163

Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

CDN-1163

CAS#892711-75-0

Theoretical Analysis

MedKoo Cat#: 561360

Name: CDN-1163

CAS#: 892711-75-0

Chemical Formula: C20H20N2O2

Exact Mass: 320.1525

Molecular Weight: 320.39

Elemental Analysis: C, 74.98; H, 6.29; N, 8.74; O, 9.99

Price and Availability

Size	Price	Availability
50mg	USD 450.00	2 Weeks
100mg	USD 850.00	2 Weeks
200mg	USD 1,350.00	2 Weeks
500mg	USD 2,450.00	2 Weeks

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Related CAS #

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Synonym

CDN-1163; CDN 1163; CDN1163;

IUPAC/Chemical Name

4-(1-Methylethoxy)-N-(2-methyl-8-quinolinyl)benzamide

InChi Key

GVGVYDCVFBGALZ-UHFFFAOYSA-N

InChi Code

InChI=1S/C20H20N2O2/c1-13(2)24-17-11-9-16(10-12-17)20(23)22-18-6-4-5-15-8-7-14(3)21-19(15)18/h4-13H,1-3H3,(H,22,23)

SMILES Code

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

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

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Biological target:

CDN1163 is a small molecular allosteric activator of the sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) that improves Ca2+ homeostasis.

In vitro activity:

Herein, we found that SERCA activity was suppressed in influenza A virus infected human lung cells (H1395) and that CDN1163, an activator of SERCA, restored autophagic flux and thus reduced autophagosome accumulation caused by the influenza A virus. Activating SERCA activity with CDN1163 also decreased expression of inflammatory cytokines and chemokines and attenuated mitochondrial dysfunction in IAV-infected H1395 cells. Reference: J Virol. 2021 Mar 10;95(10):e00217-21. https://journals.asm.org/doi/10.1128/JVI.00217-21?url_ver=Z39.88-2003&rfr_id=ori:rid:crossref.org&rfr_dat=cr_pub%20%200pubmed

In vivo activity:

16-month male C57BL/6J mice were treated with vehicle or CDN1163, an allosteric SERCA activator, for 10 months. At 26 months, maximal SERCA activity was reduced 41% in gastrocnemius muscle in vehicle-treated mice but maintained in old CDN1163 treated mice. Reductions in gastrocnemius mass (9%) and in vitro specific force generation in extensor digitorum longus muscle (11%) in 26 versus 16-month-old wild-type mice were also reversed by CDN1163. CDN1163 administered by intra-peritoneal injection also prevented the increase in mitochondrial ROS production in gastrocnemius muscles of aged mice. Transcriptomic analysis revealed that these effects are at least in part mediated by enhanced cellular energetics by activation of PGC1-α, UCP1, HSF1, and APMK and increased regenerative capacity by suppression of MEF2C and p38 MAPK signaling. Reference: Int J Mol Sci. 2020 Dec 22;22(1):37. https://www.ncbi.nlm.nih.gov/pmc/articles/pmid/33375170/

	Solvent	mg/mL	mM
Solubility
	DMSO	64.0	199.76

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 320.39 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

In vitro protocol:

1. Peng J, Ran Y, Xie H, Deng L, Li C, Ling C. Sarco/Endoplasmic Reticulum Ca2+ Transporting ATPase (SERCA) Modulates Autophagic, Inflammatory, and Mitochondrial Responses during Influenza A Virus Infection in Human Lung Cells. J Virol. 2021 Mar 10;95(10):e00217-21. doi: 10.1128/JVI.00217-21. Epub ahead of print. PMID: 33692207; PMCID: PMC8139658. 2. Singh R, Moreno P, Hajjar RJ, Lebeche D. A role for calcium in resistin transcriptional activation in diabetic hearts. Sci Rep. 2018 Oct 23;8(1):15633. doi: 10.1038/s41598-018-34112-4. PMID: 30353146; PMCID: PMC6199245.

In vivo protocol:

1. Qaisar R, Pharaoh G, Bhaskaran S, Xu H, Ranjit R, Bian J, Ahn B, Georgescu C, Wren JD, Van Remmen H. Restoration of Sarcoplasmic Reticulum Ca2+ ATPase (SERCA) Activity Prevents Age-Related Muscle Atrophy and Weakness in Mice. Int J Mol Sci. 2020 Dec 22;22(1):37. doi: 10.3390/ijms22010037. PMID: 33375170; PMCID: PMC7792969. 2. Britzolaki A, Cronin CC, Flaherty PR, Rufo RL, Pitychoutis PM. Chronic but not acute pharmacological activation of SERCA induces behavioral and neurochemical effects in male and female mice. Behav Brain Res. 2021 Feb 5;399:112984. doi: 10.1016/j.bbr.2020.112984. Epub 2020 Nov 1. PMID: 33137400; PMCID: PMC7855138.

1: Dahl R. A new target for Parkinson's disease: Small molecule SERCA activator CDN1163 ameliorates dyskinesia in 6-OHDA-lesioned rats. Bioorg Med Chem. 2017 Jan 1;25(1):53-57. doi: 10.1016/j.bmc.2016.10.008. Epub 2016 Oct 12. PubMed PMID: 27776889. 2: Kang S, Dahl R, Hsieh W, Shin A, Zsebo KM, Buettner C, Hajjar RJ, Lebeche D. 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. doi: 10.1074/jbc.M115.705012. Epub 2015 Dec 23. PubMed PMID: 26702054; PubMed Central PMCID: PMC4777852.

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