Bempedoic acid (ETC-1002)

Catalog No.S7953 Batch:S795301

Technical Data

Formula

C₁₉H₃₆O₅

Molecular Weight

344.49

CAS No.

738606-46-7

Solubility (25°C)*

In vitro

DMSO

68 mg/mL (197.39 mM)

Water

Insoluble

Ethanol

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	5%DMSO 1 Corn oil	5.0mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Bempedoic acid (ETC-1002),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 ^[1]

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^[1]. 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^[2].

In vivo

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^[2]. ETC-1002 is an inactive prodrug and converted to an active ACL inhibitor(ECT-1002-CoA) by endogenous liver ACS activity in vivo^[3].

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines Primary rat hepatocytes and differentiated human monocyte-derived macrophages Concentrations 30 μM or 100 μM Incubation Time 12 h Method Primary rat hepatocytes and differentiated human MDMs are treated with indicated concentrations of ETC-1002 for 12 h. Working solutions of ETC-1002 are prepared in serum-free RPMI 1640 containing 12 mM HEPES, 10,000 U/ml penicillin, and 100 μg/ml streptomycin.
Animal Study:^{^[2]}	Animal Models C57BL/6 male mice Dosages 10 ml/kg Administration i.p.

Cell Assay:^{^[2]}

Cell lines
Primary rat hepatocytes and differentiated human monocyte-derived macrophages
Concentrations
30 μM or 100 μM
Incubation Time
12 h
Method
Primary rat hepatocytes and differentiated human MDMs are treated with indicated concentrations of ETC-1002 for 12 h. Working solutions of ETC-1002 are prepared in serum-free RPMI 1640 containing 12 mM HEPES, 10,000 U/ml penicillin, and 100 μg/ml streptomycin.

Animal Study:^{^[2]}

Animal Models
C57BL/6 male mice
Dosages
10 ml/kg
Administration
i.p.

References

Selleck's Bempedoic acid (ETC-1002) has been cited by 4 publications

Chemically induced revitalization of damaged hepatocytes for regenerative liver repair [ iScience, 2023, 26(12):108532]	PubMed: 38144457
Combined inhibition of ACLY and CDK4/6 reduces cancer cell growth and invasion [ Oncol Rep, 2023, 49(2)32]	PubMed: 36562384
MK8722, an AMPK activator, inhibiting carcinoma proliferation, invasion and migration in human pancreatic cancer cells [ Biomed Pharmacother, 2021, 144:112325]	PubMed: 34656065
Classic and Targeted Anti-Leukaemic Agents Interfere With the Cholesterol Biogenesis Metagene in Acute Myeloid Leukaemia: Therapeutic Implications [ J Cell Mol Med, 2020, 25]	PubMed: 32450611

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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