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Synonyms | ML-236B,Compactin | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C23H34O5 |
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分子量 | 390.51 | CAS No. | 73573-88-3 | |
Solubility (25°C)* | 体外 | DMSO | 78 mg/mL (199.73 mM) | |
Ethanol | 7 mg/mL (17.92 mM) | |||
Water | Insoluble | |||
* <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. |
製品説明 | Mevastatin (ML-236B,Compactin) is a competitive inhibitor of HMG-Coenzyme A (HMG-CoA) reductase with a binding affinity 10,000 times greater than the HMG-CoA substrate itself. |
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in vitro | Mevastatin is a cholesterol-lowering agent isolated from Penicillium citinium. It reduces cholesterol synthesis to 50% of control at 0.01 pg/mL (26 nM). [1] It is structurally similar to the HMG, a substituent of the endogenous substrate of HMG-CoA reductase. Mevastatin is a prodrug that is activated in vivo via hydrolysis of the lactone ring. The hydrolyzed lactone ring mimics the tetrahedral intermediate produced by the reductase allowing the agent to bind with 10,000 times greater affinity than its natural substrate. The bicyclic portion of mevastatin binds to the coenzyme A portion of the active site. Mevastatin increases levels of eNOS mRNA and protein, reduces infarct size, and improves neurological deficits in a dose- and time-dependent manner.[2] |
in vivo | At doses of 5 and 20 mg/kg, mevastatin produces reduction of serum cholesterol levels at 3 hours after oral administration. It lowers the levels of serum cholesterol by approximately 30 % at a dose of 20 mg/kg. [1] Mevastatin lowers hepatic production of cholesterol by competitively inhibiting HMG-CoA reductase. Cholesterol levels are reduced only after 28 days of treatment and does not correlate with infarct reduction. Baseline absolute cerebral blood flow is 30% higher after 14-day high-dose treatment. [2] |
動物実験 | 動物モデル | Wistar-Imamichi male rats |
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投薬量 | 5 mg/kg, 20 mg/kg | |
投与方法 | orally |
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Data from [Data independently produced by , , Atherosclerosis, 2018, 276:28-38]
Data from [Data independently produced by , , Eur J Pharmacol, 2017, 813:161-171]
The cholesterol metabolite 25-hydroxycholesterol restrains the transcriptional regulator SREBP2 and limits intestinal IgA plasma cell differentiation [ Immunity, 2021, 54(10):2273-2287.e6] | PubMed: 34644558 |
Simvastatin Suppresses Human Breast Cancer Cell Invasion by Decreasing the Expression of Pituitary Tumor-Transforming Gene 1 [ Front Pharmacol, 2020, 11:574068] | PubMed: 33250768 |
Accumulation of 8,9-unsaturated sterols drives oligodendrocyte formation and remyelination [Hubler Z, et al. Nature, 2018, 560(7718):372-376] | PubMed: 30046109 |
Simvastatin functions as a heat shock protein 90 inhibitor against triple-negative breast cancer [Kou X, et al. Cancer Sci, 2018, 109(10):3272-3284] | PubMed: 30039622 |
MK-2206, an allosteric inhibitor of AKT, stimulates LDLR expression and LDL uptake: A potential hypocholesterolemic agent [Bjune K, et al. Atherosclerosis, 2018, 276:28-38] | PubMed: 30025252 |
Triciribine increases LDLR expression and LDL uptake through stabilization of LDLR mRNA. [ Sci Rep, 2018, 8(1):16174] | PubMed: 30385871 |
Vorinostat and Simvastatin have synergistic effects on triple-negative breast cancer cells via abrogating Rab7 prenylation. [Kou X, et al. Eur J Pharmacol, 2017, 813:161-171] | PubMed: 28826913 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。