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| | ETC-1002 Basic information |
| Product Name: | ETC-1002 | | Synonyms: | ETC-1002;Bempedoic Acid;ETC-1002 (ESP 55016);ESP 55016;ETC-1002(BEMPEDOIC ACID);CS-1544;Bempedoic Acid(ETC-1002;Bempedoate | | CAS: | 738606-46-7 | | MF: | C19H36O5 | | MW: | 344.49 | | EINECS: | | | Product Categories: | API | | Mol File: | 738606-46-7.mol |  |
| | ETC-1002 Chemical Properties |
| 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) | | pka | 4.55±0.45(Predicted) | | form | Solid | | color | White to Off-White |
| | ETC-1002 Usage And Synthesis |
| 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. | | Description | ETC-1002 is a prodrug form of ETC-1002-CoA. 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. | | 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. |
| | ETC-1002 Preparation Products And Raw materials |
| Raw materials | methyl 3-bromo-2,2-dimethylpropanoate-->Hexanoic acid, 6-bromo-2,2-dimethyl-, methyl ester-->Pentadecanedioic acid, 8-hydroxy-2,2,14,14-tetramethyl-, 1,15-diethyl ester-->2,2,14,14-tetramethyl-8-oxopentadecanedioic acid-->2,2,14,14-Tetramethyl-8-oxopentadecanedioic acid diethyl ester-->ethyl 6-bromo-2,2-dimethylhexanoate-->1,5-Dibromopentane |
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