Lovastatin

別名: Mevinolin, MK-803 中文名稱：洛伐他汀

目錄號(hào)：S2061 Purity: 99.99%

Lovastatin是一種HMG-CoA還原酶抑制劑，無(wú)細(xì)胞試驗(yàn)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

CAS: 75330-75-5

規(guī)格	價(jià)格	庫(kù)存
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
更大包裝有超大折扣
400-668-6834 [email protected]

產(chǎn)品質(zhì)控

批次：純度： 99.99%

99.99

Lovastatin相關(guān)產(chǎn)品

相關(guān)產(chǎn)品	Mevastatin Clinofibrate SR-12813	點(diǎn)擊展開(kāi)
相關(guān)化合物庫(kù)	代謝化合物庫(kù) 抗癌代謝化合物庫(kù) 谷氨酰胺代謝化合物庫(kù) 糖代謝化合物庫(kù) 脂代謝化合物庫(kù)	點(diǎn)擊展開(kāi)

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	給藥濃度	孵育時(shí)間	活性描述	文獻(xiàn)信息(PMID)
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
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

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

靶點(diǎn)

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(guò)95％的DNA合成的抑制，這通過(guò)[³H]胸苷與DNA的結(jié)合測(cè)定。Lovastatin使細(xì)胞同步在G1，而不是在細(xì)胞周期的G0期。Lovastatin對(duì)RAS的依賴性以及RAS無(wú)關(guān)的細(xì)胞系有相似的生長(zhǎng)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(guò)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是羥甲基戊二酰基（HMG)-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(zhǎng)-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(shí)驗(yàn)圖片	檢測(cè)方法	檢測(cè)指標(biāo)	實(shí)驗(yàn)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
臨床試驗(yàn)信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

參考文獻(xiàn)
https://pubmed.ncbi.nlm.nih.gov/9389730/ https://pubmed.ncbi.nlm.nih.gov/1711413/ https://pubmed.ncbi.nlm.nih.gov/12815379/ https://pubmed.ncbi.nlm.nih.gov/10393901/ https://pubmed.ncbi.nlm.nih.gov/1673788/ https://pubmed.ncbi.nlm.nih.gov/31037159/ + 展開(kāi)

參考文獻(xiàn)

https://pubmed.ncbi.nlm.nih.gov/9389730/
https://pubmed.ncbi.nlm.nih.gov/1711413/
https://pubmed.ncbi.nlm.nih.gov/12815379/

https://pubmed.ncbi.nlm.nih.gov/10393901/
https://pubmed.ncbi.nlm.nih.gov/1673788/
https://pubmed.ncbi.nlm.nih.gov/31037159/

+ 展開(kāi)

化學(xué)信息&溶解度

分子量	404.54	分子式	C₂₄H₃₆O₅
CAS號(hào)	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(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 80 mg/mL ( (197.75 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Ethanol : 35 mg/mL (86.51 mM)

Water : Insoluble

DMSO : 80 mg/mL ( (197.75 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Ethanol : 30 mg/mL (74.15 mM)

Water : Insoluble

DMSO : 81 mg/mL ( (200.22 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Ethanol : 29 mg/mL (71.68 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解配方批次：現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑				動(dòng)物體內(nèi)配方計(jì)算器
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 該配方已經(jīng)過(guò)Selleck實(shí)驗(yàn)室實(shí)測(cè)。如果上述溶解方案不能滿足您的需求，可聯(lián)系Selleck銷售提供定制化測(cè)試。	2.500mg/ml (6.18mM)	以 1 mL 工作液為例，取50μL50mg/ml的澄清DMSO儲(chǔ)備液加到400μL PEG300中，混合均勻使其澄清；向上述體系中加入50μLTween80，混合均勻使其澄清；然后繼續(xù)加入500μL ddH2O定容至 1 mL。工作液請(qǐng)現(xiàn)配現(xiàn)用！
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請(qǐng)輸入動(dòng)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(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)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(guò)該批次藥物DMSO溶解度，請(qǐng)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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* 必填項(xiàng)

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Lovastatin

產(chǎn)品質(zhì)控

Lovastatin相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

生物活性

化學(xué)信息&溶解度

實(shí)驗(yàn)計(jì)算

技術(shù)支持