Size | Price | Stock | Qty |
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1mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
Bempedoic acid (formerly ESP-55016; ETC-1002; ESP55016; ETC1002; Nexletol; Bempedoate) is an ATP-citrate lyase (ACL) inhibitor and hepatic AMP-activated protein kinase (AMPK) activator. It is a once-daily, orally bioavailable LDL-C lowering medication that has been approved for the treatment of hypercholesterolemia. It was created to lower high LDL-C levels and prevent the negative effects of other LDL-C lowering treatments. Bempedoic acid enters the liver through cell surface receptors that are distinct from the transporters that take up statins specifically after being quickly absorbed in the small intestine. The metabolism of lipids and carbohydrates is regulated by bempedoic acid.
Targets |
AMPK
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ln Vitro |
Bempedoic acid (ETC-1002) activates AMP-activated protein kinase in a Ca2+/calmodulin-dependent kinase β-independent and liver kinase β 1-dependent manner, without detectable changes in adenylate energy charge.It has been demonstrated that bempedoic acid quickly converts to a CoA thioester in the liver, which directly inhibits ATP-citrate lyase[1]. Increased AMP-activated protein kinase (AMPK) phosphorylation is associated with decreased MAP kinase activity and decreased production of proinflammatory cytokines and chemokines in cells treated with bempedoic acid (ETC-1002)[2].
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ln Vivo |
Bempedoic acid (ETC-1002) treatment for two weeks causes a noticeable and long-lasting increase in AMPK and ACC phosphorylation in the livers of rats. In rat liver, Bempedoic acid is more prevalent >100-fold than CoA thioester and is connected to AMPK activation[1]. Leukocytes' ability to home into the mouse peritoneal cavity is suppressed by bempedoic acid (ETC-1002). In a mouse model of diet-induced obesity, Bempedoic acid improves adipose AMPK activity, lowers JNK phosphorylation, and decreases expression of the macrophage-specific marker 4F/80[2].
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Enzyme Assay |
7.5× compounds are added to a 96-well PolyPlate containing 60 μL of Buffer per well with substrates CoA (200 μM), ATP (400 μM), and [14C]citrate. Reaction is started with 4 μL (300 ng/well) ACL, and the plate is incubated at 37°C for 3 h.
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Cell Assay |
Glucose production is measured in primary rat hepatocyte cultures. It contains nonessential amino acids, 10 mM lactate, 1 mM pyruvate, and is free of glucose and phenol red. Cells are cultured in this mixture. Bempedoic acid (0.1 to 100 μM) is incubated with the cells in a variety of concentrations[1].
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Animal Protocol |
Rats: Male Wistar Han rats are fasted for 48 hours and then given a single dose of bempedoic acid before receiving a second 48-hour feeding of a high-carbohydrate diet. Rats are kept on a standard chow diet and given oral gavage doses of bempedoic acid for a two-week assessment. The dose is 30 mg/kg/day given in the morning. Food is discontinued two hours before the final oral dose of engine control or bempedoic acid after nutritional staging and/or dosing[1].
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References |
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Molecular Formula |
C19H36O5
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Molecular Weight |
344.4861
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Exact Mass |
344.2563
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Elemental Analysis |
C, 66.25; H, 10.53; O, 23.22
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CAS # |
738606-46-7
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Related CAS # |
Bempedoic acid-d4;2408131-70-2;Bempedoic acid-d5;2408131-71-3
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Appearance |
White to light yellow solid powder
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LogP |
4.47
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tPSA |
94.83
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SMILES |
CC(C)(CCCCCC(CCCCCC(C)(C)C(=O)O)O)C(=O)O
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InChi Key |
HYHMLYSLQUKXKP-UHFFFAOYSA-N
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InChi Code |
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)
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Chemical Name |
8-hydroxy-2,2,14,14-tetramethylpentadecanedioic acid
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Synonyms |
ETC-1002; ETC 1002; ETC1002; ESP-55016; Bempedoate; Bempedoic acid; ETC-1002ESP55016; ETC1002ESP
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~100 mg/mL (~290.3 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.87 mg/mL (8.33 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.87 mg/mL (8.33 mM) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.26 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (7.26 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 5: ≥ 2.5 mg/mL (7.26 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 6: 0.57 mg/mL (1.65 mM) in 1% DMSO + 99% Saline (add these co-solvents sequentially from left to right, and one by one),suspension solution;clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.9028 mL | 14.5142 mL | 29.0284 mL | |
5 mM | 0.5806 mL | 2.9028 mL | 5.8057 mL | |
10 mM | 0.2903 mL | 1.4514 mL | 2.9028 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Status | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT04929249 | Active Recruiting |
Drug: Inclisiran | Atherosclerotic Cardiovascular Disease |
Novartis Pharmaceuticals | June 25, 2021 | Phase 3 |
NCT05694260 | Recruiting | Drug: Bempedoic acid | Hypercholesterolemia | Esperion Therapeutics, Inc. | January 12, 2023 | Phase 2 |
NCT05488431 | Recruiting | Drug: Bempedoic acid Other: Placebo |
Dyslipidemias HIV Infections |
Priscilla Hsue, MD | March 1, 2023 | Phase 2 |
NCT05103254 | Recruiting | Drug: Bempedoic Acid Drug: Bempedoic Acid / Ezetimibe |
Pregnancy Hyperlipidemias |
Esperion Therapeutics, Inc. | September 1, 2021 | |
NCT06035874 | Not yet recruiting | Drug: Bempedoic acid | Type 2 Diabetes | Medanta, The Medicity, India | October 15, 2023 |