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| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| E425759-1ml |
1ml |
现货  |
|
| 英文别名 | bempedoic acid|ETC-1002|738606-46-7|8-Hydroxy-2,2,14,14-tetramethylpentadecanedioic acid|Nexletol|Nilemdo|ESP-55016|ETC1002|Bempedoate|UNII-1EJ6Z6Q368|acido bempedoico|acide bempedoique|acidum bempedoicum|ETC 1002|ESP 55016|Bempedoic acid [USAN:INN]|1EJ6Z |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | ETC-1002 |
| 生化机理 | 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). |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
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 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 |
| IUPAC Name | 8-hydroxy-2,2,14,14-tetramethylpentadecanedioic acid |
|---|---|
| INCHI | InChI=1S/C19H36O5/c1-18(2,16(21)22)13-9-5-7-11-15(20)12-8-6-10-14-19(3,4)17(23)24/h15,20H,5-14H2,1-4H3,(H,21,22)(H,23,24) |
| InChi Key | HYHMLYSLQUKXKP-UHFFFAOYSA-N |
| Canonical SMILES | CC(C)(CCCCCC(CCCCCC(C)(C)C(=O)O)O)C(=O)O |
| Isomeric SMILES | CC(C)(CCCCCC(CCCCCC(C)(C)C(=O)O)O)C(=O)O |
| PubChem CID | 10472693 |
| 分子量 | 344.49 |
| 熔点 | 87 - 92°C |
|---|
| 象形图 |
Health Hazard 
Harmful |
|---|---|
| 信号词 | Danger |
| 危险声明 |
H373: Causes damage to organs through prolonged or repeated exposure H302: Harmful if swallowed H372: Causes damage to organs through prolonged or repeated exposure |
| 预防措施声明 | P501,P264,P260,P270,P330,P301+P317,P319 |
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