Mevastatin

製品コードS4223 バッチS422302

印刷

化学情報

Chemical Structure Synonyms ML-236B,Compactin Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C23H34O5
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.

溶剤液（一定の濃度）を調合する

生物活性

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.
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]

プロトコル(参考用のみ)

動物実験 動物モデル Wistar-Imamichi male rats
投薬量 5 mg/kg, 20 mg/kg
投与方法 orally

カスタマーフィードバック

Data from [Data independently produced by , , Atherosclerosis, 2018, 276:28-38]

Data from [Data independently produced by , , Eur J Pharmacol, 2017, 813:161-171]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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。

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