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Lovastatin

別名: Mevinolin, MK-803 中文名稱：洛伐他汀

Lovastatin是一種HMG-CoA還原酶抑制劑，無細(xì)胞試驗中IC50為3.4 nM，用于降膽固醇（降脂藥）。Lovastatin 可觸發(fā)自噬。

Lovastatin Chemical Structure

Lovastatin Chemical Structure

CAS: 75330-75-5

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 742.83 現(xiàn)貨
50mg 578.06 現(xiàn)貨
200mg 1387.21 現(xiàn)貨
1g 4832.1 現(xiàn)貨
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Lovastatin相關(guān)產(chǎn)品

相關(guān)信號通路圖

HMG-CoA Reductase Signaling Pathways

HMG-CoA Reductase信號通路圖

細(xì)胞實驗數(shù)據(jù)示例

細(xì)胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻(xiàn)信息
SW480 Growth inhibition assay 20 uM 48 hrs Reversal of growth inhibition of human SW480 cells at 20 uM after 48 hrs by MTS assay in presence of >50 uM mevalonate 17472962
SW480 Function assay 20 uM 48 hrs Decrease in survivin expression in human SW480 cells at 20 uM after 48 hrs by immunoblot analysis 17472962
SW480 Function assay 20 uM 48 hrs Reversal of reduction in survivin expression in human SW480 cells at 20 uM after 48 hrs by immunoblot analysis in presence of 100 uM mevalonate 17472962
SW480 Function assay 20 uM 48 hrs Reversal of reduction in survivin mRNA expression in human SW480 cells at 20 uM after 48 hrs by RT-PCR technique in presence of 100 uM mevalonate 17472962
SW480 Growth inhibition assay 20 uM 48 hrs Reversal of growth inhibition of human SW480 cells at 20 uM after 48 hrs by immunoblot analysis in presence of farnesyl pyrophosphate 17472962
SW480 Growth inhibition assay 20 uM 48 hrs Reversal of growth inhibition of human SW480 cells at 20 uM after 48 hrs by immunoblot analysis in presence of geranylgeranyl pyrophosphate 17472962
SW480 Function assay 20 uM 48 hrs Decrease in isoprenylated Ras level in human SW480 cells at 20 uM after 48 hrs by immunoblot analysis 17472962
SW480 Function assay 20 uM 48 hrs Reversal of decrease in isoprenylated Ras level in human SW480 cells at 20 uM after 48 hrs by immunoblot analysis in presence of mevalonate 17472962
SW480 Function assay 20 uM 48 hrs Reversal of decrease in isoprenylated Ras level in human SW480 cells at 20 uM after 48 hrs by immunoblot analysis in presence of farnesyl pyrophosphate 17472962
SW480 Function assay 20 uM 48 hrs Reversal of decrease in isoprenylated Ras level in human SW480 cells at 20 uM after 48 hrs by immunoblot analysis in presence of geranylgeranyl pyrophosphate 17472962
MDA-MB-231 Function assay 1 to 10 uM 24 hrs Induction of p21 expression in human PR, ER, HER2-negative human MDA-MB-231 cells at 1 to 10 uM after 24 hrs by western blot analysis 24556504
MDA-MB-231 Growth inhibition assay >10 uM 48 hrs Total growth inhibition of PR, ER, HER2-negative human MDA-MB-231 cells at >10 uM after 48 hrs by WST-1 assay 24556504
RPMI-8226 Function assay 10 uM 48 hrs Inhibition of HMG-coA reductase in human RPMI-8226 cells assessed as disruption of Rap1a geranylgeranylation at 10 uM after 48 hrs by western blot analysis 24726306
HepG2 Function assay 1 uM 6 hrs Lipid-lowering effect in human HepG2 cells assessed as reduction in oleic acid-induced lipid accumulation at 1 uM after 6 hrs by oil-red O staining based spectrophotometry 25304895
HepG2 Function assay 10 uM 24 hrs Lipid-lowering effect in human HepG2 cells assessed as reduction in oleic acid-induced total cholesterol accumulation at 10 uM after 24 hrs by oil-red O staining based spectrophotometry 25304895
HepG2 Function assay 10 uM 24 hrs Lipid-lowering effect in human HepG2 cells assessed as reduction in oleic acid-induced triglyceride accumulation at 10 uM after 24 hrs by oil-red O staining based spectrophotometry 25304895
RPMI8226 Apoptosis assay 20 uM 48 hrs Induction of apoptosis in human RPMI8226 cells assessed as increase in PARP cleavage at 20 uM incubated for 48 hrs by immunoblot method 25935643
RPMI8226 Apoptosis assay 20 uM 48 hrs Induction of apoptosis in human RPMI8226 cells assessed as increase in caspase-3 cleavage at 20 uM incubated for 48 hrs by immunoblot method 25935643
MDA-MB-231 Function assay 30 uM 24 hrs Induction of reactive oxygen species in human MDA-MB-231 cells at 30 uM after 24 hrs by DCFH-DA probe-based flow cytometric method 27756564
MDA-MB-231 Function assay 10 uM 6 to 24 hrs Induction of CHK1/2 phosphorylation in human MDA-MB-231 cells assessed as increase in p53 phosphorylation at 10 uM after 6 to 24 hrs by Western blot method 27756564
MDA-MB-231 Function assay 10 uM 6 to 24 hrs Induction of ATM phosphorylation in human MDA-MB-231 cells at 10 uM after 6 to 24 hrs by Western blot method 27756564
RPMI8226 Function assay 0.5 uM 48 hrs Inhibition of FTase in human RPMI8226 cells assessed as disruption of H-ras farnesylation at 0.5 uM after 48 hrs by immunoblot analysis 31699606
RPMI8226 Function assay 0.5 uM 48 hrs Inhibition of GGtase-1 in human RPMI8226 cells assessed as disruption of Rap1a geranylgeranylation at 0.5 uM after 48 hrs by immunoblot analysis 31699606
LS180 Function assay 20 uM Inhibition of survivin expression in parent human LS180 cells at 20 uM by immunoblot analysis 17472962
LS180 Function assay 20 uM Inhibition of survivin expression in survivin gene transfected human LS180 cells at 20 uM immunoblot analysis 17472962
SW480 Function assay 20 uM Inhibition of FBS-stimulated increase in Ras protein expression in human SW480 cells assessed as GTP-bound protein at 20 uM by immunoblot analysis 17472962
SW480 Function assay 20 uM Reversal of inhibition of FBS-stimulated increase in Ras protein expression in human SW480 cells assessed as GTP-bound protein at 20 uM by immunoblot analysis 17472962
SW480 Function assay 20 uM Inhibition of FBS-stimulated increase in Akt phosphorylation in human SW480 cells at 20 uM by immunoblot analysis 17472962
Neuro2a Function assay 1 uM Inhibition of HMGCoA reductase in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis 26789657
SW480 Growth inhibition assay 96 hrs Growth inhibition of human SW480 cells after 96 hrs by MTS assay, IC50=7.1μM. 17472962
Huh-7/3-1 Antiviral assay 72 hrs Antiviral activity against Hepatitis C virus (isolate Con1) genotype 1b in human Huh-7/3-1 cells assessed as inhibition of HCV replication after 72 hrs by luciferase assay 16408072
LS180 Growth inhibition assay 96 hrs Growth inhibition of human LS180 cells after 96 hrs by MTS assay, IC50=25.3μM. 17472962
HT29 Growth inhibition assay 96 hrs Growth inhibition of human HT29 cells after 96 hrs by MTS assay, IC50=46.8μM. 17472962
LS180 Growth inhibition assay 72 hrs Blockade of growth inhibition of human LS180 cells after 72 hrs by MTS method 17472962
K562 Function assay 48 hrs Inhibition of GGTase1 in human K562 cells assessed as reduction of Rap1a protein geranylgeranylation after 48 hrs by Western blotting 20832326
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50=11.4μM. 23570542
A549 Function assay 5 mins Inhibition of HMG-CoA reductase in human A549 cells after 5 mins by spectrophotometric analysis, IC50=19.8μM. 23570542
HS68 Cytotoxicity assay 72 hrs Cytotoxicity against human HS68 cells after 72 hrs by MTT assay, IC50=23.2μM. 23570542
MEF Cytotoxicity assay 72 hrs Cytotoxicity against mouse MEF cells after 72 hrs by MTT assay, IC50=35μM. 23570542
MDA-MB-361 Growth inhibition assay 48 hrs Growth inhibition of ER-positive, HER2-positive human MDA-MB-361 cells after 48 hrs by WST-1 assay 24556504
MDA-MB-468 Growth inhibition assay 48 hrs Total growth inhibition of PR, ER, HER2-negative human MDA-MB-468 cells after 48 hrs by WST-1 assay 24556504
AU565 Growth inhibition assay 48 hrs Growth inhibition of ER-negative, HER2-positive human AU565 cells after 48 hrs by WST-1 assay 24556504
MCF7 Growth inhibition assay 48 hrs Total growth inhibition of ER-positive, HER2-negative human MCF7 cells after 48 hrs by WST-1 assay 24556504
HepG2 Function assay 6 hrs Lipid lowering activity in human HepG2 cells assessed as decrease in oleic acid elicited lipid accumulation after 6 hrs by oil-red O staining method, IC50=8.3μM. 26169125
A549 Antiviral assay 48 hrs Antiviral activity against Dengue virus 2 NGC infected in human A549 cells assessed as reduction in virus replication after 48 hrs by renilla luciferase reporter gene assay, EC50=1.82μM. 26771861
PC3 Cytotoxicity assay 48 hrs Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by SRB assay, IC50=5.4μM. 27756564
HEK293 Function assay TP_TRANSPORTER: inhibition of estradiol-17beta-glucuronide uptake(estradiol-17beta-glucuronide:0.02uM) in OATP1B1-expressing HEK293 cells, IC50=28μM. 15616150
MDCK Function assay TP_TRANSPORTER: inhibition of calcein-AM efflux in MDR1-expressing MDCK cells, IC50=10μM. 15616150
NIH-3T3-G185 Function assay TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells, IC50=32.7μM. 11716514
3T3-G185 Function assay TP_TRANSPORTER: inhibition of Daunorubicin transport in 3T3-G185 cells, IC50=26μM. 11474784
HEP-G2 Function assay Tested for ability to inhibit incorporation of [14C]acetate into cholesterol in cultured human hepatoma (HEP-G2) cells; 0.061-0.10, IC50=0.079μM. 8246237
HEP G2 Function assay Tested for inhibition of cholesterol biosynthesis in HEP G2 cells, IC50=0.029μM. 7932551
HEP G2 Function assay Inhibition of cellular HMG-CoA reductase in cultures of human HEP G2 cells, determined by decreased incorporation of sodium [14C]acetate into cholesterol., IC50=0.05μM. 2296036
HEP G2 Function assay Inhibition of cellular HMG-CoA reductase in cultures of hepatic cells (HEP G2, a human hepatoma cell line), IC50=0.00005μM. 2153213
HEP G2 Function assay Inhibition of the incorporation of sodium [14C]acetate into cholesterol in HEP G2 cells., IC50=0.05μM. 1656041
HES 9 cell line Function assay Concentration required to inhibit HMG-CoA reductase by 50% was determined in HES 9 cell line, IC50=0.013 μM 1527791
Vero Cytotoxicity assay Cytotoxicity against African green monkey Vero cells, IC50=2.2μM. 27228159
KB Cytotoxicity assay Cytotoxicity against human KB cells by resazurin microplate assay, IC50=15.6μM. 27228159
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
A549 Function assay Reductase Activity Assay: The HMGR activity was performed using HMG-CoA reductase assay kit from Sigma-Aldrich with the human recombinant protein or 100 μg total cell lysates from A549 cells. Lovastatin was used as a positive control, IC50=0.0295μM. ChEMBL
HepG2 Function assay Compound was evaluated for inhibitory activity against HMG-CoA reductase in HepG2 cells, IC50=0.039μM. ChEMBL
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生物活性

產(chǎn)品描述 Lovastatin是一種HMG-CoA還原酶抑制劑，無細(xì)胞試驗中IC50為3.4 nM，用于降膽固醇（降脂藥）。Lovastatin 可觸發(fā)自噬。
靶點
HMG-CoA reductase [1]
(Cell-free assay)
3.4 nM
體外研究(In Vitro)
體外研究活性

在大鼠原代星形膠質(zhì)細(xì)胞中，Lovastatin抑制了LPS-和細(xì)胞因子介導(dǎo)的NO產(chǎn)生以及iNOS的表達(dá)。在大鼠原代星形膠質(zhì)細(xì)胞，小膠質(zhì)細(xì)胞和巨噬細(xì)胞中，Lovastatin抑制了LPS-誘導(dǎo)的TNF-α，IL-1β和IL-6的表達(dá)。[1]

Lovastatin導(dǎo)致超過95％的DNA合成的抑制，這通過[3H]胸苷與DNA的結(jié)合測定。Lovastatin使細(xì)胞同步在G1，而不是在細(xì)胞周期的G0期。Lovastatin對RAS的依賴性以及RAS無關(guān)的細(xì)胞系有相似的生長抑制活性。[2]

Lovastatin使載脂蛋白-B的含脂蛋白顯著減少，特別是低密度脂蛋白膽固醇，以及血漿甘油三酯erides，以及高密度脂蛋白膽固醇的少量增加。[3]

Lovastatin通過抑制蛋白酶體使細(xì)胞停滯，這導(dǎo)致p21和p27蛋白的積累，使細(xì)胞阻滯在G1期。Lovastatin是羥甲基戊二?；℉MG)-CoA還原酶，是膽固醇合成的限速酶。Lovastatin可用于阻止培養(yǎng)細(xì)胞在細(xì)胞周期的G1期，導(dǎo)致細(xì)胞周期蛋白依賴性激酶抑制劑（CKIs）p21和p27蛋白的穩(wěn)定化。[4]

在表達(dá)激活p21ras的人膀胱癌T24細(xì)胞中，Lovastatin（2-10 mM）使細(xì)胞停留在G1期和并延長-或使一小部分細(xì)胞停滯-在細(xì)胞周期中的G2期。的G2期。在人膀胱癌T24細(xì)胞中，Lovastatin（50 mM）表現(xiàn)細(xì)胞毒性。[5]
實驗圖片 檢測方法 檢測指標(biāo) 實驗圖片 PMID
Western blot p-AKT / AKT / p-GSK3β / GSK3β / p-β-catenin / β-catenin / TAZ HMGR 30975976
Immunofluorescence β-catenin 30975976
Growth inhibition assay Cell viability 20205716
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01478828 Terminated
Prostate Cancer
Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Patrick C Walsh Prostate Cancer Research Fund
 July 13 2012 Not Applicable
NCT01527669 Completed
Healthy Subjects
National Taiwan University Hospital|National Science Council Taiwan
 February 2012 Phase 4
NCT01385020 Completed
Healthy Subjects
National Taiwan University Hospital|National Science Council Taiwan
 July 2011 Phase 4
NCT00700921 Completed
Chronic Obstructive Pulmonary Disease (COPD)
National Jewish Health|National Heart Lung and Blood Institute (NHLBI)
 April 2008 Phase 2

化學(xué)信息&溶解度

分子量 404.54 分子式

C24H36O5
CAS號 75330-75-5 SDF Download Lovastatin SDF
Smiles CCC(C)C(=O)OC1CC(C=C2C1C(C(C=C2)C)CCC3CC(CC(=O)O3)O)C
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 80 mg/mL ( (197.75 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 35 mg/mL (86.51 mM)

Water : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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