[CAS NO. 738606-46-7] ETC-1002

Name: ETC-1002
Brand: Arctom Scientific
SKU: SLK-S7953

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PRODUCTS SPECIFICATIONS [738606-46-7]

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Catalog

SLK-S7953

Brand

Selleck

CAS

738606-46-7

DESCRIPTION [738606-46-7]

Overview

MDL	-
Molecular Weight	344.49
Molecular Formula	C19H36O5
SMILES	C(C(C(O)=O)(C)C)CCCCC(CCCCCC(C(O)=O)(C)C)O

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	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
50 mM	0.0581 mL	0.2903 mL	0.5806 mL

Description

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 . It has potent inhibitory activity against hepatic (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. 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

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.

References

[1] Nikolic D, et al. Atherosclerosis. 2014, 237(2):705-710.
[2] Filippov S, et al. J Lipid Res. 2013, 54(8):2095-2108.
[3] Pinkosky SL, et al. J Lipid Res. 2013, 54(1):134-151.

Synonyms

Pentadecanedioic acid, 8-hydroxy-2,2,14,14-tetramethyl-

8-Hydroxy-2,2,14,14-tetramethylpentadecanedioic acid

ESP 55016

ETC 1002

Bempedoic acid

Nilemdo

Nexletol