Name | ETC-1002 |
Synonyms | CS-1544 ETC-1002 ESP 55016 Bempedoate Bempedoic Acid ETC-1002 (ESP 55016) Bempedoic Acid(ETC-1002 ETC-1002(BEMPEDOIC ACID) |
CAS | 738606-46-7 |
Molecular Formula | C19H36O5 |
Molar Mass | 344.49 |
Density | 1.045±0.06 g/cm3(Predicted) |
Melting Point | 87 - 92°C |
Boling Point | 506.5±35.0 °C(Predicted) |
Solubility | 10 mM in DMSO |
Appearance | Solid |
Color | White to Off-White |
pKa | 4.55±0.45(Predicted) |
Storage Condition | Refrigerator |
In vitro study | ETC-1002 is a novel and under investigation LDL-C-lowering small molecule. It is a dicarboxylic acid faction. Its mechanism of action is mainly to target two liver enzymes: adenosine triphosphate-citrate lyase (ACL) and adenosine monophosphate-activated protein kinase (AMPK) inhibit sterol and fatty acid synthesis and promote mitochondrial long-chain fatty acid oxidation. ETC-1002 increases AMPK phosphorylation levels, decreases MAPKs activity, and decreases pro-inflammatory cytokine and chemokine production. These ETC-1002 effects of regulating soluble inflammatory factors can be significantly inhibited by LKB1 siRNAs, suggesting that ETC-1002 may activate AMPK and exert its anti-inflammatory effect through lkb1-dependent mechanisms. |
In vivo study | In vivo experiments, ETC-1002 inhibited the migration of sulfur glia-induced leukocytes to the peritoneal cavity of mice. Similarly, in a mouse model of diet-induced obesity, ETC-1002 restored adipose AMPK activity, decreased JNK phosphorylation, and reduced macrophage-specific marker 4F/80 expression. ETC-1002 is a pro-drug in an inactive state that is converted in vivo by endogenous liver ACS activity into an ACL inhibitor (active state, ECT-1002-CoA). |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.903 ml | 14.514 ml | 29.029 ml |
5 mM | 0.581 ml | 2.903 ml | 5.806 ml |
10 mM | 0.29 ml | 1.451 ml | 2.903 ml |
5 mM | 0.058 ml | 0.29 ml | 0.581 ml |