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Cat. No.: HY-134980

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LK-980

LK-980 is a cholesterol biosynthesis inhibitor. LK-980 primarily inhibits human sterol Δ7-reductase (DHCR7), and more weakly inhibits sterol Δ14-reductase (DHCR14), sterol Δ24-reductase (DHCR24), and sterol C5-desaturase (SC5DL). LK-980 is slowly metabolized in human primary hepatocytes and does not induce CYP3A4 enzyme activity or mRNA expression. LK-980 can be used in research related to cholesterol metabolism disorders such as hyperlipidemia and atherosclerosis, as well as cardiovascular diseases.

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CAS No.: 943250-95-1
Formule: C₁₉H₂₅N₃O
Masse moléculaire:311.43

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Please store the product under the recommended conditions in the Certificate of Analysis.

LK-980 Chemical Structure

CAS No.: 943250-95-1

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- In Vitro
Chemical Information
Pureté et documentation
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Activité biologique

Description

In Vitro

LK-980 (100 µM; 50 min) did not inhibit HMGCR activity in HepG2 microsomes^[1].
LK-980 (1 µM) was slowly metabolized by human primary hepatocytes, with a half-life of 4.32 h in HH-114 and >6 h in HH-089 and HH-129^[1].
LK-980 (10 µM; 48 h) primarily inhibits DHCR7 in human primary hepatocytes, increasing 7-dehydrocholesterol by 34.16-fold, while slight increases in FF-MAS, desmosterol, and lathosterol indicate weak inhibition of DHCR14, DHCR24, and SC5DL^[1].
LK-980 (10 µM; 12-48 h) does not induce CYP3A4 activity or mRNA in human primary hepatocytes^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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Chemical Information

CAS No. 943250-95-1
Masse moléculaire 311.43
Formule C₁₉H₂₅N₃O
SMILES

OC(C=1C=NC=CC1)CN2CCN(CCC=3C=CC=CC3)CC2
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Acimovic J, et al. Inhibition of human sterol Δ7-reductase and other postlanosterol enzymes by LK-980, a novel inhibitor of cholesterol synthesis. Drug metabolism and disposition: the biological fate of chemicals. 2011 Jan;39(1):39-46.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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