CDN1163

An allosteric activator of SERCA2

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库存: 现货

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5mg

￥825.00

660.00

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10mg

￥1337.00

1070.00

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50mg

￥4587.00

3670.00

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100mg

￥8237.00

6590.00

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货号: ajce46906
CAS: 892711-75-0
别名: 4-异丙氧基-N-(2-甲基喹啉-8-基)苯甲酰胺
分子式: C20H20N2O2
分子量: 320.39
纯度: >98%
溶解度: DMSO : 50 mg/mL (156.06 mM);Water : < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

CDN1163 is an allosteric activator of sarcoplasmic/endoplasmic reticulum Ca²⁺-ATPase 2 (SERCA2) that enhances calcium uptake in endoplasmic reticulum (ER) vesicles when used at concentrations ranging from 1 to 10 ?M.¹ It decreases peroxide-induced cell death in HEK293 cells. CDN1163 (50 mg/kg) increases calcium uptake in ER microsomes isolated from obese mouse liver. It decreases blood glucose levels, plasma and hepatic triglyceride levels, and plasma cholesterol and malondialdehyde (MDA) levels in obese mice. CDN1163 (50 mg/kg) restores SERCA activity, prevents gastrocnemius muscle loss and contractile dysfunction, and reduces mitochondrial production of reactive oxygen species (ROS) in the CuZnSOD-deficient (Sod^-/-) mouse model of oxidative stress-related muscle atrophy and weakness.² It also improves motor deficits in the initiation time (IT), stepping, and cylinder tests for akinesia in a rat model of Parkinson’s disease induced by 6-OHDA .³

1.Kang, S., Dahl, R., Hsieh, W., et al.Small molecular allosteric activator of the sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) attenuates diabetes and metabolic disordersJ. Biol. Chem.291(10)5185-5198(2016) 2.Qaisar, R., Bhaskaran, S., Ranjit, R., et al.Restoration of SERCA ATPase prevents oxidative stress-related muscle atrophy and weaknessRedox Biol.2068-74(2019) 3.Dahl, R.A new target for Parkinson's disease: Small molecule SERCA activator CDN1163 ameliorates dyskinesia in 6-OHDA-lesioned ratsBioorg. Med. Chem.25(1)53-57(2017)