| Identification | Back Directory | [Name]
ETC-1002 | [CAS]
738606-46-7 | [Synonyms]
CS-1544
ETC-1002
ESP 55016
Bempedoate
Bempedoic Acid
ETC-1002 (ESP 55016)
Bempedoic Acid(ETC-1002
ETC-1002(BEMPEDOIC ACID)
BEMPEDOIC ACID;ESP-55016;SGI-7079
Pentadecanedioic acid, 8-hydroxy-2,2,14,14-tetramethyl-
ESP-55016; ESP55016; ESP 55016; ETC-1002; ETC 1002; ETC1002; BEMPEDOATE; BEMPEDOIC ACID | [Molecular Formula]
C19H36O5 | [MDL Number]
MFCD18800820 | [MOL File]
738606-46-7.mol | [Molecular Weight]
344.49 |
| Chemical Properties | Back Directory | [Melting point ]
87 - 92°C | [Boiling point ]
506.5±35.0 °C(Predicted) | [density ]
1.045±0.06 g/cm3(Predicted) | [storage temp. ]
Refrigerator | [solubility ]
Chloroform (Slightly), Methanol (Slightly) | [form ]
Solid | [pka]
4.55±0.45(Predicted) | [color ]
White to Off-White | [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) | [InChIKey]
HYHMLYSLQUKXKP-UHFFFAOYSA-N | [SMILES]
C(O)(=O)C(C)(C)CCCCCC(O)CCCCCC(C)(C)C(O)=O |
| Hazard Information | Back Directory | [Description]
ETC-1002 is a prodrug form of ETC-1002-CoA.1 ETC-1002 is conjugated to coenzyme A (CoA) by very long-chain acyl-CoA synthetase-1 (ACSVL1) to form ETC-1002-CoA, which inhibits ATP citrate lyase (Ki = 2 μM) and activates AMP-activated protein kinase (AMPK). ETC-1002 suppresses total lipid synthesis in wild-type and AMPKβ1 knockout primary murine hepatocytes. In vivo, ETC-1002 (30 mg/kg) prevents increases in hepatic cholesterol and reduces the size of aortic atherosclerotic lesions induced by a high-fat high-cholesterol diet in Apoe-/-/Ampkβ1-/- (DKO) mice. | [Description]
Etc-1002 is a small molecule that can be used orally to lower LDL-C and is an activator of LIVER AMPK. ETC-1002 has an effective inhibitory effect on liver ATP-Citrate lyase. | [Uses]
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). | [Definition]
ChEBI: Bempedoic acid is an alpha,omega-dicarboxylic acid that is pentadecanedioic acid which is substituted by methyl groups groups at positions 2 and 14, and by a hydroxy group at position 8. It is a drug used for the treatment of high LDL cholesterol, which is sometimes referred to as 'bad cholesterol'. It has a role as an antilipemic drug, an EC 2.3.3.8 (ATP citrate synthase) inhibitor and a prodrug. |
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