Information ETC-1002 ETC-1002 (Bempedoic acid, ESP-55016),also known as Bempedoic acid, is an orally available, once-daily LDL-C lowering small molecule designed to lower elevated levels of LDL-C and to avoid side effects associated with existing LDL-C lowering therapies.ETC-1002 is an activator of hepatic AMP-activated protein kinase (AMPK) . It has potent inhibitory activity against hepatic ATP-citrate lyase (IC50=29 uM). Targets AMPK In vitro ETC-1002 is a new investigational low density lipoprotein cholesterol (LDL-C)-lowering agent which is a dicarboxylic acid derivative with a novel mechanism of action targeting two hepatic enzymes--adenosine triphosphate-citrate lyase (ACL) and adenosine monophosphate-activated protein kinase (AMPK), inhibiting sterol and fatty acid synthesis and promoting mitochondrial long-chain fatty acid oxidation. It increases levels of AMP-activated protein kinase (AMPK) phosphorylation, reduces activity of MAP kinases and decreases production of proinflammatory cytokines and chemokines. These effects on soluble mediators of inflammation can be significantly abrogated by LKB1 siRNAs, indicating that ETC-1002 activates AMPK and exerts its anti-inflammatory effects via an LKB1-dependent mechanism. In vivo ETC-1002 suppresses thioglycollate-induced homing of leukocytes into mouse peritoneal cavity. Similarly, in a mouse model of diet-induced obesity, ETC-1002 restores adipose AMPK activity, reduces JNK phosphorylation, and diminishes expression of macrophage-specific marker 4F/80. ETC-1002 is an inactive prodrug and converted to an active ACL inhibitor(ECT-1002-CoA) by endogenous liver ACS activity in vivo. Cell Research(from reference) Cell lines：Primary rat hepatocytes and differentiated human monocyte-derived macrophages Concentrations：30 μM or 100 μM Incubation Time：12 h
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ETC-1002
Dangerous GoodsCAS number：738606-46-7 molecular formula：C19H36O5
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | acido bempedoico | CHEBI:44212 | DB11936 | (2R,3R)-rel-2,3-Dihydroxysuccinic acid | A905695 | AS-49804 | EINECS 207-354-7 | Epitope ID:115015 | s7953 | acidum bempedoicum | AMY31933 | BEMPEDOIC ACID [USAN] | CCG-267969 | bempedoic-acid | Q27075007 | BEMPE | ||
| CAS number | 738606-46-7 | molecular formula | C19H36O5 |
| molecular weight | 344.49 g/mol | Exact mass | - |
| PSA | 94.800 Ų | logp | 4.800 |
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physicochemical properties
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Safety information
pictogram：
GHS08 , GHS07
Signal word：
Danger
Hazard Statement：
H373: 通过长时间或反复暴露对器官造成损害 H302: 吞食有害 H372: 通过长时间或反复暴露对器官造成损害
Statement of Preventive Measures：
P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P330: 漱口 P301+P317: 如果被吞咽：请寻求医疗帮助。 P319: 如果你感到不适，请寻求医疗帮助。
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MSDS
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