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M2537

Sigma-Aldrich

米法斯丁

≥98% (HPLC), powder or crystals

别名:

ML-236B, 康帕丁

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About This Item

经验公式（希尔记法）:
C23H34O5
CAS号:
73573-88-3
分子量:
390.51
Beilstein:
1269441
MDL號碼:
MFCD05662341
分類程式碼代碼:
12352200
PubChem物質ID:
24278540
NACRES:
NA.77

化驗

≥98% (HPLC)

形狀

powder or crystals

顏色

white to light yellow

mp

151 °C

溶解度

ethanol: 25-26 mg/mL, clear, colorless

抗生素活性譜

neoplastics

作用方式

enzyme | inhibits

起源

Daiichi-Sankyo

儲存溫度

2-8°C

SMILES 字串

[H][C@]12[C@H](CCC=C1C=C[C@H](C)[C@@H]2CC[C@@H]3C[C@@H](O)CC(=O)O3)OC(=O)[C@@H](C)CC

InChI

1S/C23H34O5/c1-4-14(2)23(26)28-20-7-5-6-16-9-8-15(3)19(22(16)20)11-10-18-12-17(24)13-21(25)27-18/h6,8-9,14-15,17-20,22,24H,4-5,7,10-13H2,1-3H3/t14-,15-,17+,18+,19-,20-,22-/m0/s1

InChI 密鑰

AJLFOPYRIVGYMJ-INTXDZFKSA-N

基因資訊

human ... HMGCL(3155) , HMGCR(3156)
rat ... Hmgcr(25675)

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相关类别

一般說明

化学结构：他汀
美伐他汀(Mevastatin)是一种聚酮，属于他汀类化合物。结构中含有一个羟基-六氢萘环。

應用

美伐他汀已用于：
  • 通过细胞毒性检测分析其对慢性淋巴细胞白血病(CLL)细胞的影响
  • 分析其作为异戊二烯化抑制剂，对K-Ras转染人胚胎肾细胞(HEK)的影响
  • 研究其作为他汀类药物，对人乳腺癌细胞和胶质母细胞瘤的体外抗癌作用

生化／生理作用

美伐他汀是一种参与胆固醇合成的主要酶——3-羟基3-甲戊二酰辅酶A还原酶（HMG-CoA还原酶）的选择性抑制剂，可用作降胆固醇药。美伐他汀来源于各种真菌。美伐他汀可作为抗骨吸收剂，对骨质疏松症有治疗作用。可通过诱发破骨细胞凋亡抑制骨吸收。美伐他汀也参与蛋白质（如Ras）异戊二烯化的抑制。可通过抑制转录因子Rho的四异戊二烯化，提高内皮一氧化氮合酶(eNOS)mRNA和蛋白质水平。

特點和優勢

该化合物由 第一三共制药开发。要浏览其他制药公司开发的化合物列表批准的药物/候选药物的列表， 点击这里 。

包裝

无底玻璃瓶。内含物装在插入的融合锥内。

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

個人防護裝備

Eyeshields, Gloves, type N95 (US)

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
049M4755V
048M4833V
126M4789V
086M4819V
056M4775V

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C M Shipman et al.
Cancer research, 58(23), 5294-5297 (1998-12-16)
It has recently been suggested that bisphosphonates may have direct antitumor effects in vivo, in addition to their therapeutic antiresorptive properties. Bisphosphonates can inhibit proliferation and cause apoptosis in human myeloma cells in vitro. In macrophages, bisphosphonate-induced apoptosis was recently
F P Coxon et al.
Molecular pharmacology, 54(4), 631-638 (1998-10-10)
The exact mechanisms of action of antiresorptive bisphosphonate drugs remain unclear, although they may inhibit bone resorption by mechanisms that can lead to osteoclast apoptosis. These drugs also cause apoptosis in J774 macrophages, probably as a consequence of inhibition of
J T Woo et al.
Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research, 15(4), 650-662 (2000-04-26)
Compactin (mevastatin), which inhibits 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, and thus biosynthesis of cholesterol and the prenylation of proteins, inhibits osteoclastic bone resorption. Although it has been suggested that compactin inhibits bone resorption by inducing apoptosis of osteoclasts, the pathway by
U Laufs et al.
The Journal of biological chemistry, 273(37), 24266-24271 (1998-09-03)
The mechanism by which 3-hydroxy-3-methylglutaryl (HMG)-CoA reductase inhibitors increase endothelial nitric oxide synthase (eNOS) expression is unknown. To determine whether changes in isoprenoid synthesis affects eNOS expression, human endothelial cells were treated with the HMG-CoA reductase inhibitor, mevastatin (1-10 microM)
S P Luckman et al.
Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research, 13(4), 581-589 (1998-04-29)
Bisphosphonates are currently the most important class of antiresorptive drugs used for the treatment of metabolic bone diseases. Although the molecular targets of bisphosphonates have not been identified, these compounds inhibit bone resorption by mechanisms that can lead to osteoclast
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