Mevastatin

製品コードS4223 バッチS422304

印刷

化学情報

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

20 mg/mL (51.21 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.33mg/ml (3.41mM)	Taking the 1 mL working solution as an example, add 50 μL of 26.6 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.156mg/ml (0.40mM)	Taking the 1 mL working solution as an example, add 50 μL of 3.12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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) は、HMG-Coenzyme A (HMG-CoA) 還元酵素の競合的阻害剤であり、HMG-CoA 基質そのものよりも 10,000 倍高い結合親和性を持っています。
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). This compound is structurally similar to the HMG, a substituent of the endogenous substrate of HMG-CoA reductase. It 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 this chemical binds to the coenzyme A portion of the active site. It increases levels of eNOS mRNA and protein, reduces infarct size, and improves neurological deficits in a dose- and time-dependent manner.
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. This compound 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.

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

参考

https://pubmed.ncbi.nlm.nih.gov/1010803/
https://pubmed.ncbi.nlm.nih.gov/11283400/

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：

Propafenone facilitates mitochondrial-associated ferroptosis and synergizes with immunotherapy in melanoma [ J Immunother Cancer, 2024, 12(11)e009805]	PubMed: 39581704
Systems immunology-based drug repurposing framework to target inflammation in atherosclerosis [ Nat Cardiovasc Res, 2023, 2(6):550-571]	PubMed: 37771373
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。