HMG-CoA Reductase (HMGCR)
HMG-CoA Reductase (HMGCR) is the rate-limiting enzyme for cholesterol synthesis in the conversion of HMG-CoA to mevalonate. HMGCR is found in eukaryotes and prokaryotes. The phylogenetic analysis has revealed two classes of HMG-CoA reductase, the Class I enzymes of eukaryotes and some archaea and the Class II enzymes of eubacteria and certain other archaea.
Both in eukaryotes and in archaebacteria the enzyme HMGCR is known to catalyze an early reaction unique to isoprenoid biosynthesis. In humans, the HMG-CoA reductase reaction is rate-limiting for the biosynthesis of cholesterol and therefore constitutes a prime target of drugs that reduce serum cholesterol levels.
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HMG-CoA Reductase (HMGCR) Related Products (168)
Related Products (168)
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Antibodies (13)
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Rebaudioside A
0 ImagesRebaudioside A is an orally effective steviol glycoside with high sweetness. Rebaudioside A acts as an inhibitor of α-glucosidase with an IC50 value of 35.01 μg/mL. Rebaudioside A increases the ATP/ADP ratio in β cells in a glucose-dependent manner, thereby inhibiting KATP channels, leading to membrane depolarization, calcium influx, and ultimately stimulating insulin secretion. Rebaudioside A activates the SREBP signaling pathway by inhibiting HMGCR, the rate-limiting enzyme in cholesterol synthesis, resulting in increased expression of LDLR on the cell surface, thus promoting the uptake of LDL-C in the blood. Rebaudioside A can be used for studies on blood glucose and lipid regulation as well as anti-obesity.
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Simvastatin acid ammonium
0 ImagesSynonyms: Tenivastatin ammoniumSimvastatin acid (Tenivastatin) ammonium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid ammonium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid ammonium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene.
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Meglutol
0 ImagesSynonyms: Dicrotalic acid; 3-Hydroxy-3-methylglutaric acidMeglutol is a lipid-lowering agent. Meglutol can reduces cholesterol, triglycerides, serum β-lipoprotein, and phospholipids, and inhibits the activity of HMG-CoA reductase (a rate-limiting enzyme in cholesterol biosynthesis). Meglutol can induce significant lipid oxidative damage in brain tissue. It is promising for research in the field of cardiovascular diseases and metabolic diseases.
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Thiolutin
0 ImagesThiolutin (Acetopyrrothin) is a sulfur-containing antibiotic, which is a potent inhibitor of bacterial and yeast RNA polymerases. Thiolutin can be produced by Streptomyces. Thiolutin inhibits AMSH (IC50 = 4 μM) and Rpn11 (IC50 = 0.53 μM). Thiolutin is a dual inhibitor of BRCC36 and the NLRP3 inflammasome, exhibiting anti-inflammatory effects. Thiolutin effectively suppresses the interaction between BRCC36 and HMGCR, leading to the inhibition of HCC growth. Thiolutin attenuates pyroptosis and NLRP3 inflammasome activation. Thiolutin markedly alleviates renal injury and inflammatory process in IgAN. Thiolutin is an anti-angiogenic compound which can ease Doxorubicin-induced cardiotoxicity (DOXIC)[1][2][3][4][5].
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Simvastatin hydroxy acid sodium
0 ImagesSynonyms: Tenivastatin sodium; Simvastatin Impurity A sodiumSimvastatin hydroxy acid (Tenivastatin) sodium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin hydroxy acid sodium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin hydroxy acid sodium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene.
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Lovastatin hydroxy acid sodium
0 ImagesSynonyms: Mevinolinic acid sodiumLovastatin hydroxy acid sodium (Mevinolinic acid sodium) is a highly potent inhibitor of HMG-CoA reductase with a Ki of 0.6 nM.
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Clitorin
0 ImagesClitorin is an orally active flavonoid compound that can be isolated from Carica papaya. Clitorin is an inhibitor of EGFR (IC50: 89.58 nM) and aromatase (IC50: 77.41 nM). Clitorin has antioxidant and anti-tumor activities. In the DPPH and ABTS radical scavenging assays, Clitorin has IC50 values of 91.96 ppm and 250.45 ppm, respectively. In addition, Clitorin can regulate lipogenesis and fatty acid oxidation and can be used in the research of non-alcoholic fatty liver disease.
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Hesperetin 7-O-glucoside
0 ImagesSynonyms: Hes-7-GHesperetin 7-O-glucoside is a typical flavonoid monoglucoside, which is an anti-inflammatory agent and an antihypertensive with orally active. Hesperetin 7-O-glucoside is a commonly used food adjuvant. Hesperetin 7-O-glucoside inhibits human intestinal maltase and human HMG-CoA reductase with Ki of 1.8 mM and 9.8 μM, respectively. Hesperetin 7-O-glucoside has antibacterial activity and can regulate intestinal flora and metabolic homeostasis in mice.
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β-Amyrin acetate
0 Imagesβ-Amyrin acetate is a triterpenoid with potent anti-inflammatory, antifungal, anti-diabetic, anti-hyperlipidemic activities. β-Amyrin acetate can inhibit HMG-CoA reductase activity by locating in the hydrophobic binding cleft of HMG CoA reductase.
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Mevalonolactone
0 ImagesMevalonolactone is an intermediate metabolite in the eukaryotic mevalonate pathway, serving as the stable δ-lactone form of mevalonate with oral activity. Mevalonolactone exhibits binding affinity for ZNF384 (Ka = 12.6 μM) and inhibitory activity against aconitase (aconitase). Mevalonolactone promotes the nuclear localization of ZNF384 and enhances its binding to the GGPPS promoter. Mevalonolactone induces insulin resistance, disrupts glucose and lipid metabolism, enhances the isoprenylation of K-Ras, and inhibits the activation of the insulin signaling pathway. Mevalonolactone inhibits polypeptide synthesis of HMG-CoA reductase in isolated rat hepatocytes, promotes its degradation, and reduces its enzymatic activity. Mevalonolactone impairs mitochondrial function in rat brains. Mevalonolactone promotes the development of metabolically unhealthy obesity. Mevalonolactone can be used in research related to metabolically abnormal obesity, mevalonic aciduria, HMGCR-related limb-girdle myopathy, and statin-induced myopathy.
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Atorvastatin lactone
0 ImagesCat. No.: HY-101873CAS No.: 125995-03-1Atorvastatin lactone is a metabolite of Atorvastatin acid, an HMG-CoA reductase inhibitor. Atorvastatin lactone exhibits myotoxicity.
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2-Butenoyl coenzyme A lithium
0 Images2-Butenoyl coenzyme A lithium is an inactivator and a substrate of Plasmodium falciparum enoyl-β-hydroxyacyl-acyl carrier protein (ACP) reductase and other enoyl-CoA reductases, and it is also the lithium salt of trans-2-methyl-2-butenoyl coenzyme A. 2-Butenoyl coenzyme A lithium acts on short-chain and medium-chain coenzyme A dehydrogenases as well as glutaryl-CoA dehydrogenase, and shows no activity against wild-type isovaleryl-CoA dehydrogenase. 2-Butenoyl coenzyme A lithium functions as a metabolite in the L-isoleucine catabolic pathway, and can serve as a substrate in the activity assay of 3-ketothiolase. 2-Butenoyl coenzyme A lithium is applicable to research related to 3-ketothiolase deficiency.
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Rosuvastatin-d3 sodium
0 ImagesRosuvastatin-d3 sodium is the deuterated-labeled Rosuvastatin Sodium (HY-17504B). Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM. Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
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Clinofibrate
0 ImagesSynonyms: S-8527Clinofibrate (S-8527) is a hypelipidemic agent and a HMG-CoA reductase inhibitor.
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Atorvastatin-d5 hemicalcium
0 ImagesAtorvastatin-d5 (hemicalcium) is the deuterium labeled Atorvastatin. Atorvastatin hemicalcium is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids. Atorvastatin hemicalcium inhibits human SV-SMC proliferation and invasion with IC50s of 0.39 μM and 2.39 μM, respectively.
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7α,27-Dihydroxycholesterol
0 Images7α,27-Dihydroxycholesterol is an oxysterol, a human metabolite, and a ligand for EBI2 (GPR183), which is involved in lipid synthesis. 7α,27-Dihydroxycholesterol mediates the chemotaxis of cells expressing EBI2. 7α,27-Dihydroxycholesterol can be converted into 7α,27-dihydroxy-4-cholesten-3-one (HY-W414457), thereby inhibiting HMG-CoA reductase (HMGCR), the rate-limiting enzyme in cholesterol synthesis.
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Simvastatin (Standard)
0 ImagesSynonyms: MK 733 (Standard)Simvastatin (Standard) is the analytical standard of Simvastatin. This product is intended for research and analytical applications. Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.
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Simvastatin acid
0 ImagesSynonyms: TenivastatinSimvastatin acid (Tenivastatin), a hydrolysate of Simvastatin (HY-17502), is a HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene.
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HMG499
0 ImagesCat. No.: HY-114316CAS No.: 2416941-68-7HMG499 is a potent and selective HMG-CoA reductase inhibitor with an IC50 of 0.41 μM. HMG499 can prevent statins-induced accumulation of HMGCR, reduce serum cholesterol levels and decrease atherosclerosis.
