HMG-CoA Reductase

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抑制剂选择性比较

HMG-CoA Reductase产品

所有产品 HMG-CoA Reductase抑制剂(13) 新HMG-CoA Reductase产品

产品目录	产品描述	文献引用	实验数据
S1792	Simvastatin Simvastatin 是一种HMG-CoA reductase竞争性抑制剂，无细胞试验中K_i为0.1-0.2 nM。	Cancer Cell, 2019, 36(2):179-193 Acta Biomater, 2019, 90:324-336 Int J Oncol, 2019, 54(6):2054-2068	Statin-Related Inhibition of Dehydroepiandrosterone Sulfate (DHEAS) Uptake by SLCO2B1 in Prostate Cancer (PC) Cells. B, Uptake of DHEAS in PC cells with 2.5 µM DHEAS and different concentrations of statins when incubated for 60 minutes. Statistical analysis was performed by comparing each condition with the DHEAS 2.5 µM and no statin state except when indicated. C, Uptake of DHEAS in PC cells before (scrambled short hairpin RNA) and after (short hairpin RNA 2B1) SLCO2B1 is knocked down when incubated with 2.5 μM DHEAS and 100 μM atorvastatin for 10 and 60 minutes. Statistical analysis was performed by comparing each condition with scrambled short hairpin RNA after 10 minutes with DHEAS except when indicated. P = .02 for the comparison between scrambled short hairpin RNA with 10 vs 60 minutes of DHEAS incubation for LNCaP and .01 for 22RV1. Other P values are indicated in the figure. Bars indicate means and error bars indicate standard deviation.
S2169	Rosuvastatin Calcium Rosuvastatin Calcium是一种竞争性HMG-CoA reductase抑制剂，无细胞试验中IC50为11 nM。	Cancer Lett, 2016, 10.1016/j.canlet.2016.03.004. Biochim Biophys Acta, 2015, 10.1016/j.bbagen.2015.03.011 Toxicol In Vitro, 2015, 29(3):621-30	MDA-MB-231 cells were treated with simvastatin (SIM) or rosuvastatin (ROSU) in combination with ZOL for 48 h. Vitality and apoptosis were measured by using the cell titer blue and the caspase 3/7 Glo assay. Data are shown as mean ± SD of at least three individual experiments (p ≤ 0.05; p ≤ 0.01; **p ≤ 0.001).
S1759	Pitavastatin Calcium Pitavastatin Calcium，一种新型的Statins类药物，是pitavastatin的钙盐形式。Pitavastatin是高效的HMG-CoA reductase抑制剂。	Drug Metab Dispos, 2017, 45(6):612-623 PLoS One, 2017, 12(5):e0178278 Sci Rep, 2015, 5:16407	Western blotting showed that in U87 cells treated with pitavastatin, the LC3-II isoform dramatically increased after statin treatment and showed at day 2, 3 and 4.
S2061	Lovastatin Lovastatin是一种HMG-CoA还原酶抑制剂，无细胞试验中IC50为3.4 nM，用于降胆固醇（降脂药）。	Theranostics, 2019, 9(7):2100-2114 Nat Commun, 2018, 9(1):1524 Mol Cancer Ther, 2018, 17(8):1781-1792	To evaluate the role of cell cycle progression in androgen induced DSB formation, LAPC4 cells were either treated with solvent control or 50 μM lovastatin for 36 h prior to stimulation with 100 nM DHT for 6 h. Note that androgen induced γH2A.X foci formation was not different between control and lovastatin pre-treated cells.
S1909	Fluvastatin Sodium Fluvastatin Sodium抑制HMG-CoA reductase活性，无细胞试验中IC50为8 nM。	Nat Commun, 2018, 9(1):1524 Anticancer Res, 2018, 38(6):3471-3476 Mol Cancer Ther, 2018, 17(8):1781-1792	The concentration of lanosterol slightly increases (f) and that of desmosterol significantly increases (g) in the brains of fluvastatin-treated 129.Mecp2tm1.1Bird/Y mice at P70 (n = 4 mice per group; P = 0.042). *P ≤ 0.05 determined using Dunnett’s post-hoc test to compare statin- with vehicle-treated groups. All error bars represent the s.e.m.
S5715^New	atorvastatin Atorvastatin is a lipid lowering agent. It is a competitive inhibitor of hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase, the rate-determining enzyme in cholesterol biosynthesis via the mevalonate pathway.
S5713^New	Pravastatin Pravastatin is a lipoprotein-lowering drug via reversibly inhibiting hydroxymethylglutaryl-CoA (HMG-CoA) reductase and the synthesis of very-low-density lipoproteins.	J Cell Physiol, 2019, 234(3):2058-2066
S2077	Atorvastatin Calcium Atorvastatin Calcium 是一种HMG-CoA reductase抑制剂，用作降胆固醇药物，并阻断胆固醇的产生。	BMC Pharmacol Toxicol, 2013, 14:15	Micrographs of hematoxylin and eosin-stained liver sections from untreated and atorvastatin-treated TO mouse. Results of representative experiment of liver specimens incubated in vitro at 37癈 with and without 1.0 礛 atorvastatin for 6 hr is shown. A liver specimen at 0 hr is also shown. Liver structure and cytology are preserved in treated and untreated specimens. Inflammation and cholestasis are absent. (Hematoxylin and eosin, 10?and 40?.
S3036	Pravastatin sodium Pravastatin sodium是一种HMG-CoA还原酶抑制剂，能抑制甾醇合成，其IC50为5.6 μM。	Cancer Sci, 2018, 109(10):3272-3284 Prostate, 2017, 77(13):1303-1311 Eur J Pharmacol, 2017, 813:161-171	B, Uptake of DHEAS in PC cells with 2.5 µM DHEAS and different concentrations of statins when incubated for 60 minutes. Statistical analysis was performed by comparing each condition with the DHEAS 2.5 µM and no statin state except when indicated.
S2664	Clinofibrate Clinofibrate抑制hydroxymethylglutaryl coenzyme A reductase (HMGCR)（羟甲基戊二酰辅酶A还原酶），IC50为0.47 mM，是一种降脂剂，用于控制血液中的高胆固醇和甘油三酯水平。
S4223	Mevastatin Mevastatin 是竞争性HMG辅酶A（HMG-COA）还原酶抑制剂，比HMG-CoA底物本身结合亲合力高10,000倍。	Nature, 2018, 560(7718):372-376 Cancer Sci, 2018, 109(10):3272-3284 Atherosclerosis, 2018, 276:28-38	Sterol-starved HepG2 cells were treated with vehicle or mevastatin for 24 h before exposure to the indicated concentrations of MK-2206 for a further 14 h. Cells were then harvested and subjected to Western blot analysis. Upper panel shows one representative blot from six experiments. Lower panel: the immunoblots data were plotted relative to vehicle-treated cells. Error bars represent SD. One, two and three asterisks indicate p < 0.05, p < 0.01 and p < 0.001, respectively, compared with matched vehicle-treated cells.
S8302	SR-12813 SR-12813是孕烷X受体（PXR）的激动剂。
S5072	Rosuvastatin Rosuvastatin is an inhibitor of HMG-CoA reductase, an enzyme that catalyzes the rate-limiting step in cholesterol biosynthesis, with Ki value (inhibition constant) of approximately 0.1 nM.	Biochim Biophys Acta, 2015, 1850(7):1415-25 Breast Cancer Res Treat, 2015, 154(3):623-31

产品目录	产品描述	文献引用	实验数据
S1792	Simvastatin Simvastatin 是一种HMG-CoA reductase竞争性抑制剂，无细胞试验中K_i为0.1-0.2 nM。	Cancer Cell,2019, 36(2):179-193 Acta Biomater,2019, 90:324-336 Int J Oncol,2019, 54(6):2054-2068	Statin-Related Inhibition of Dehydroepiandrosterone Sulfate (DHEAS) Uptake by SLCO2B1 in Prostate Cancer (PC) Cells. B, Uptake of DHEAS in PC cells with 2.5 µM DHEAS and different concentrations of statins when incubated for 60 minutes. Statistical analysis was performed by comparing each condition with the DHEAS 2.5 µM and no statin state except when indicated. C, Uptake of DHEAS in PC cells before (scrambled short hairpin RNA) and after (short hairpin RNA 2B1) SLCO2B1 is knocked down when incubated with 2.5 μM DHEAS and 100 μM atorvastatin for 10 and 60 minutes. Statistical analysis was performed by comparing each condition with scrambled short hairpin RNA after 10 minutes with DHEAS except when indicated. P = .02 for the comparison between scrambled short hairpin RNA with 10 vs 60 minutes of DHEAS incubation for LNCaP and .01 for 22RV1. Other P values are indicated in the figure. Bars indicate means and error bars indicate standard deviation.
S2169	Rosuvastatin Calcium Rosuvastatin Calcium是一种竞争性HMG-CoA reductase抑制剂，无细胞试验中IC50为11 nM。	Cancer Lett,2016, 10.1016/j.canlet.2016.03.004. Biochim Biophys Acta,2015, 10.1016/j.bbagen.2015.03.011 Toxicol In Vitro,2015, 29(3):621-30	MDA-MB-231 cells were treated with simvastatin (SIM) or rosuvastatin (ROSU) in combination with ZOL for 48 h. Vitality and apoptosis were measured by using the cell titer blue and the caspase 3/7 Glo assay. Data are shown as mean ± SD of at least three individual experiments (p ≤ 0.05; p ≤ 0.01; **p ≤ 0.001).
S1759	Pitavastatin Calcium Pitavastatin Calcium，一种新型的Statins类药物，是pitavastatin的钙盐形式。Pitavastatin是高效的HMG-CoA reductase抑制剂。	Drug Metab Dispos,2017, 45(6):612-623 PLoS One,2017, 12(5):e0178278 Sci Rep,2015, 5:16407	Western blotting showed that in U87 cells treated with pitavastatin, the LC3-II isoform dramatically increased after statin treatment and showed at day 2, 3 and 4.
S2061	Lovastatin Lovastatin是一种HMG-CoA还原酶抑制剂，无细胞试验中IC50为3.4 nM，用于降胆固醇（降脂药）。	Theranostics,2019, 9(7):2100-2114 Nat Commun,2018, 9(1):1524 Mol Cancer Ther,2018, 17(8):1781-1792	To evaluate the role of cell cycle progression in androgen induced DSB formation, LAPC4 cells were either treated with solvent control or 50 μM lovastatin for 36 h prior to stimulation with 100 nM DHT for 6 h. Note that androgen induced γH2A.X foci formation was not different between control and lovastatin pre-treated cells.
S1909	Fluvastatin Sodium Fluvastatin Sodium抑制HMG-CoA reductase活性，无细胞试验中IC50为8 nM。	Nat Commun,2018, 9(1):1524 Anticancer Res,2018, 38(6):3471-3476 Mol Cancer Ther,2018, 17(8):1781-1792	The concentration of lanosterol slightly increases (f) and that of desmosterol significantly increases (g) in the brains of fluvastatin-treated 129.Mecp2tm1.1Bird/Y mice at P70 (n = 4 mice per group; P = 0.042). *P ≤ 0.05 determined using Dunnett’s post-hoc test to compare statin- with vehicle-treated groups. All error bars represent the s.e.m.
S5715^New	atorvastatin Atorvastatin is a lipid lowering agent. It is a competitive inhibitor of hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase, the rate-determining enzyme in cholesterol biosynthesis via the mevalonate pathway.
S5713^New	Pravastatin Pravastatin is a lipoprotein-lowering drug via reversibly inhibiting hydroxymethylglutaryl-CoA (HMG-CoA) reductase and the synthesis of very-low-density lipoproteins.	J Cell Physiol,2019, 234(3):2058-2066
S2077	Atorvastatin Calcium Atorvastatin Calcium 是一种HMG-CoA reductase抑制剂，用作降胆固醇药物，并阻断胆固醇的产生。	BMC Pharmacol Toxicol,2013, 14:15	Micrographs of hematoxylin and eosin-stained liver sections from untreated and atorvastatin-treated TO mouse. Results of representative experiment of liver specimens incubated in vitro at 37癈 with and without 1.0 礛 atorvastatin for 6 hr is shown. A liver specimen at 0 hr is also shown. Liver structure and cytology are preserved in treated and untreated specimens. Inflammation and cholestasis are absent. (Hematoxylin and eosin, 10?and 40?.
S3036	Pravastatin sodium Pravastatin sodium是一种HMG-CoA还原酶抑制剂，能抑制甾醇合成，其IC50为5.6 μM。	Cancer Sci,2018, 109(10):3272-3284 Prostate,2017, 77(13):1303-1311 Eur J Pharmacol,2017, 813:161-171	B, Uptake of DHEAS in PC cells with 2.5 µM DHEAS and different concentrations of statins when incubated for 60 minutes. Statistical analysis was performed by comparing each condition with the DHEAS 2.5 µM and no statin state except when indicated.
S2664	Clinofibrate Clinofibrate抑制hydroxymethylglutaryl coenzyme A reductase (HMGCR)（羟甲基戊二酰辅酶A还原酶），IC50为0.47 mM，是一种降脂剂，用于控制血液中的高胆固醇和甘油三酯水平。
S4223	Mevastatin Mevastatin 是竞争性HMG辅酶A（HMG-COA）还原酶抑制剂，比HMG-CoA底物本身结合亲合力高10,000倍。	Nature,2018, 560(7718):372-376 Cancer Sci,2018, 109(10):3272-3284 Atherosclerosis,2018, 276:28-38	Sterol-starved HepG2 cells were treated with vehicle or mevastatin for 24 h before exposure to the indicated concentrations of MK-2206 for a further 14 h. Cells were then harvested and subjected to Western blot analysis. Upper panel shows one representative blot from six experiments. Lower panel: the immunoblots data were plotted relative to vehicle-treated cells. Error bars represent SD. One, two and three asterisks indicate p < 0.05, p < 0.01 and p < 0.001, respectively, compared with matched vehicle-treated cells.
S8302	SR-12813 SR-12813是孕烷X受体（PXR）的激动剂。
S5072	Rosuvastatin Rosuvastatin is an inhibitor of HMG-CoA reductase, an enzyme that catalyzes the rate-limiting step in cholesterol biosynthesis, with Ki value (inhibition constant) of approximately 0.1 nM.	Biochim Biophys Acta,2015, 1850(7):1415-25 Breast Cancer Res Treat,2015, 154(3):623-31