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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 943250-95-1
- 分子式: C19H25N3O
- 分子量:311.43
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
体外実験
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. Further protocols information, click here.
化学情報
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CAS 番号 943250-95-1
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分子量 311.43
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分子式 C19H25N3O
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SMILES
OC(C=1C=NC=CC1)CN2CCN(CCC=3C=CC=CC3)CC2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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RT-PCR
Reverse transcription technology uses RNA as a template to synthesize DNA. RT-PCR is simple, specific and sensitive, and can be used to detect gene expression levels and expression differences in cells; detect RNA virus content; clone cDNA sequences of specific genes.
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
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Real Time qPCR (Q-PCR)
Real-time quantitative PCR (qPCR) quantifies an amplifiable nucleic-acid target by monitoring fluorescence during PCR cycling rather than measuring product only after amplification. The increase in fluorescence tracks accumulation of PCR product, and the quantification cycle (Cq; historically also Ct/CP) is related to the initial amount of target: samples containing more starting target generally reach the defined fluorescence threshold in fewer cycles.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)