HMG-CoA-Reductase-HMGCR-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/HMG-CoA Reductase (HMGCR).html HMG-CoA HYPERLINK https:/www.MedChemE/Targets/HMG-CoA Reductase (HMGCR).html HYPERLINK https:/www.MedChemE/Targets/HMG-CoA Reductase (HMGCR).html Reductase HYPERLINK https:/www.MedChemE/Targets/HMG-CoA Reductase (HMGCR).html HYPER

2、LINK https:/www.MedChemE/Targets/HMG-CoA Reductase (HMGCR).html (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-Co

3、A reductase, theClass 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 isoprenoidbiosynthesis. In humans, the HMG-CoA reductase reaction

4、 is rate-limiting for the biosynthesis of cholesterol and thereforeconstitutes a prime target of drugs that reduce serum cholesterol levels.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/HMG-CoA Reductase (HMGCR).html HMG-CoA HYPERLINK https:/www.MedChemE/Targets/HMG-CoA Reductase (HMGCR).html

5、 HYPERLINK https:/www.MedChemE/Targets/HMG-CoA Reductase (HMGCR).html Reductase HYPERLINK https:/www.MedChemE/Targets/HMG-CoA Reductase (HMGCR).html HYPERLINK https:/www.MedChemE/Targets/HMG-CoA Reductase (HMGCR).html (HMGCR) HYPERLINK https:/www.MedChemE/Targets/HMG-CoA Reductase (HMGCR).html HYPER

6、LINK https:/www.MedChemE/Targets/HMG-CoA Reductase (HMGCR).html Inhibitors HYPERLINK https:/www.MedChemE/3r-5r-rosuvastatin.html (3R,5R)-RosuvastatinCat. No.: HY-17504C HYPERLINK https:/www.MedChemE/3r-5s-fluvastatin.html (3R,5S)-Fluvastatin(3R,5S)-XU 62-320 free acid) Cat. No.: HY-14664B(3R,5R)-Ros

7、uvastatin is the (3R,5R)-enantiomer ofRosuvastatin. Rosuvastatin is a competitiveHMG-CoA reductase inhibitor with an IC of 1150nM. Rosuvastatin potently blocks humanether-a-go-go related gene (hERG) current with anIC of 195 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg(3R,5S

8、)-Fluvastatin is the3R,5S-isomer Fluvastatin. Fluvastatin (XU62-320 free acid) is a first fully synthetic,competitive HMG-CoA reductase inhibitor withan IC of 8 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/3s-5r-fluvastatin-d6-sodium.html (3S,5

9、R)-Fluvastatin HYPERLINK https:/www.MedChemE/3s-5r-fluvastatin-d6-sodium.html HYPERLINK https:/www.MedChemE/3s-5r-fluvastatin-d6-sodium.html D6 HYPERLINK https:/www.MedChemE/3s-5r-fluvastatin-d6-sodium.html HYPERLINK https:/www.MedChemE/3s-5r-fluvastatin-d6-sodium.html sodium(3S,5R)-XU 62-320 D6) Ca

10、t. No.: HY-14664CS HYPERLINK https:/www.MedChemE/3s-5r-fluvastatin-sodium.html (3S,5R)-Fluvastatin HYPERLINK https:/www.MedChemE/3s-5r-fluvastatin-sodium.html HYPERLINK https:/www.MedChemE/3s-5r-fluvastatin-sodium.html sodium(3S,5R)-XU 62-320) Cat. No.: HY-14664C(3S,5R)-Fluvastatin D6 sodium is thed

11、euterium labeled (3S,5R)-Fluvastatin sodium.Fluvastatin is a first fully synthetic,competitive HMG-CoAreductase inhibitor with an IC of 8 nM.50(3S,5R)-Fluvastatin sodium (3S,5R)-XU 62-320) isthe (3S,5R)-enantiomer of Fluvastatin.Fluvastatin is a first fully synthetic,competitive HMG-CoAreductase inh

12、ibitor with an IC of 8 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg HYPERLINK https:/www.MedChemE/3s-5r-fluvastatin-d7-sodium.html (3S,5R)-Fluvastatin-d7 HYPERLINK https:/www.MedChemE/3s-5r-fluvastatin-d7-sodium.htm

13、l HYPERLINK https:/www.MedChemE/3s-5r-fluvastatin-d7-sodium.html sodium(3S,5R)-XU 62-320-d7 sodium) Cat. No.: HY-14664CS1 HYPERLINK https:/www.MedChemE/3s-5r-rosuvastatin.html (3S,5R)-RosuvastatinCat. No.: HY-17504D(3S,5R)-Fluvastatin-d7 sodium (3S,5R)-XU62-320-d7 sodium) is the deuterium labeled(3S

14、,5R)-Fluvastatin sodium. (3S,5R)-Fluvastatinsodium (3S,5R)-XU 62-320) is the(3S,5R)-enantiomer of Fluvastatin.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg(3S,5R)-Rosuvastatin is the (3S,5R)-enantiomer ofRosuvastatin. Rosuvastatin is a competitiveHMG-CoA reductase inhibitor with

15、an IC of 1150nM. Rosuvastatin potently blocks humanether-a-go-go related gene (hERG) current with anIC of 195 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/rac-5-keto-fluvastatin.html (Rac)-5-Keto HYPERLINK https:/www.MedChemE/rac-5-keto-fluvast

16、atin.html HYPERLINK https:/www.MedChemE/rac-5-keto-fluvastatin.html Fluvastatin HYPERLINK https:/www.MedChemE/rac-5-keto-fluvastatin.html HYPERLINK https:/www.MedChemE/rel-atorvastatin.html (rel)-Atorvastatin(3-Hydroxy-5-Keto Fluvastatin) Cat. No.: HY-135358Cat. No.: HY-B0589A(Rac)-5-Keto Fluvastati

17、n (3-Hydroxy-5-KetoFluvastatin) is an impurity of Fluvastatin (XU62320). Fluvastatin is a HMG-CoA reductaseinhibitor with an IC of 8 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg(rel)-Atorvastatin, a relative configuration ofAtorvastatin. Atorvastatin is an orally activeHMG-CoA re

18、ductase inhibitor, has the ability toeffectively decrease blood lipids. Atorvastatininhibits human SV-SMC proliferation and invasionwith IC s of 0.39 M and 2.39 M, respectively.50Purity: 98%Clinical Data: LaunchedSize: 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/2-ethyl-simvastatin.html 2-Eth

19、yl HYPERLINK https:/www.MedChemE/2-ethyl-simvastatin.html HYPERLINK https:/www.MedChemE/2-ethyl-simvastatin.html Simvastatin HYPERLINK https:/www.MedChemE/2-ethyl-simvastatin.html HYPERLINK https:/www.MedChemE/3-hydroxy-pravastatin-sodium.html 3-Hydroxy HYPERLINK https:/www.MedChemE/3-hydroxy-pravas

20、tatin-sodium.html HYPERLINK https:/www.MedChemE/3-hydroxy-pravastatin-sodium.html pravastatin HYPERLINK https:/www.MedChemE/3-hydroxy-pravastatin-sodium.html HYPERLINK https:/www.MedChemE/3-hydroxy-pravastatin-sodium.html sodiumCat. No.: HY-135402 Cat. No.: HY-1363472-Ethyl Simvastatin (compound 6)

21、is a Mevinolinanalog, with HMG-CoA reductase inhibition.3-Hydroxy pravastatin sodium is the majormetabolite of Pravastatin. Pravastatin is acompetitive HMG-CoA reductase inhibitor.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize:

22、1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/atorvastatin.html AtorvastatinCat. No.: HY-B0589 HYPERLINK https:/www.MedChemE/atorvastatin-hemicalcium-salt.html Atorvastatin HYPERLINK https:/www.MedChemE/atorvastatin-hemicalcium-salt.html HYPERLINK

23、 https:/www.MedChemE/atorvastatin-hemicalcium-salt.html hemicalcium HYPERLINK https:/www.MedChemE/atorvastatin-hemicalcium-salt.html HYPERLINK https:/www.MedChemE/atorvastatin-hemicalcium-salt.html salt(CI-981; Atorvastatin hemicalcium) Cat. No.: HY-17379Atorvastatin is an orally active HMG-CoAreduc

24、tase inhibitor, has the ability toeffectively decrease blood lipids. Atorvastatininhibits human SV-SMC proliferation and invasionwith IC s of 0.39 M and 2.39 M, respectively.50Atorvastatin hemicalcium salt (CI-981) is anorally active 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitor

25、, hasthe ability to effectively decrease blood lipids.Purity: 99.05%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mgPurity: 99.94%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg HYPERLINK https:/www.MedChemE/atorvastatin-lactone.html Atorvastatin HYPERLINK

26、https:/www.MedChemE/atorvastatin-lactone.html HYPERLINK https:/www.MedChemE/atorvastatin-lactone.html lactone HYPERLINK https:/www.MedChemE/atorvastatin-lactone.html HYPERLINK https:/www.MedChemE/atorvastatin-lactone-d5.html Atorvastatin HYPERLINK https:/www.MedChemE/atorvastatin-lactone-d5.html HYP

27、ERLINK https:/www.MedChemE/atorvastatin-lactone-d5.html lactone HYPERLINK https:/www.MedChemE/atorvastatin-lactone-d5.html HYPERLINK https:/www.MedChemE/atorvastatin-lactone-d5.html D5Cat. No.: HY-101873 Cat. No.: HY-101873SAtorvastatin lactone is a prodrug form ofatorvastatin. Atorvastatin is an or

28、ally active3-hydroxy-3-methylglutaryl coenzyme A(HMG-CoA) reductase inhibitor.Atorvastatin lactone D5 is a deuterated form ofAtorvastatin lactone (HY-101873). Atorvastatinlactone is a prodrug form of atorvastatin.Atorvastatin is an orally active3-hydroxy-3-methylglutaryl coenzyme A(HMG-CoA) reductas

29、e inhibitor.Purity: 96.95%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/atorvastatin-d5-hemicalcium.html Atorvastatin-d5 HYPERLINK https:/www.MedChemE/atorvastatin-d5-hemicalcium.html HYPE

30、RLINK https:/www.MedChemE/atorvastatin-d5-hemicalcium.html hemicalcium HYPERLINK https:/www.MedChemE/atorvastatin-d5-hemicalcium.html HYPERLINK https:/www.MedChemE/atorvastatin-d5-sodium-salt.html Atorvastatin-d5 HYPERLINK https:/www.MedChemE/atorvastatin-d5-sodium-salt.html HYPERLINK https:/www.Med

31、ChemE/atorvastatin-d5-sodium-salt.html sodiumCat. No.: HY-B0589S Cat. No.: HY-B0589S1Atorvastatin-d5 hemicalcium is the deuteriumlabeled Atorvastatin. Atorvastatin hemicalcium isan orally active HMG-CoA reductase inhibitor,has the ability to effectively decrease bloodlipids.Purity: 98%Clinical Data:

32、 No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mg HYPERLINK https:/www.MedChemE/cerivastatin.html Cerivastatin HYPERLINK https:/www.MedChemE/cerivastatin.html HYPERLINK https:/www.MedChemE/cerivastatin-sodium.html Cerivastatin HYPERLINK https:

33、/www.MedChemE/cerivastatin-sodium.html HYPERLINK https:/www.MedChemE/cerivastatin-sodium.html sodiumCat. No.: HY-129458 Cat. No.: HY-109523Cerivastatin is a synthetic lipid-lowering agentand a highly potent, well-tolerated and orallyactive HMG-CoA reductase inhibitor, with a Kiof 1.3 nM/L. Cerivasta

34、tin reduces low-densitylipoprotein cholesterol levels.Cerivastatin sodium is a synthetic lipid-loweringagent and a highly potent, well-tolerated andorally active HMG-CoA reductase inhibitor,with a Ki of 1.3 nM/L. Cerivastatin sodium reduceslow-density lipoprotein cholesterol levels.Purity: 98%Clinic

35、al Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.89%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/Clinofibrate.html Clinofibrate HYPERLINK https:/www.MedChemE/Clinofibrate.html HYPERLINK https:/www.MedChemE/epi-lovastatin-d3.html Epi HYPE

36、RLINK https:/www.MedChemE/epi-lovastatin-d3.html HYPERLINK https:/www.MedChemE/epi-lovastatin-d3.html Lovastatin-d3(S-8527) Cat. No.: HY-13528Cat. No.: HY-N0504SClinofibrate (S-8527) is a hypelipidemic agent anda HMG-CoA reductase inhibitor.Epi Lovastatin-d3 is the deuterium labeledLovastatin. Lovas

37、tatin is a cell-permeableHMG-CoA reductase inhibitor used to lowercholesterol.Purity: 99.70%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/Fluvastatin.html Fluva

38、statin(XU 62-320 free acid) Cat. No.: HY-14664 HYPERLINK https:/www.MedChemE/Fluvastatin-D6-sodium.html Fluvastatin HYPERLINK https:/www.MedChemE/Fluvastatin-D6-sodium.html HYPERLINK https:/www.MedChemE/Fluvastatin-D6-sodium.html D6 HYPERLINK https:/www.MedChemE/Fluvastatin-D6-sodium.html HYPERLINK

39、https:/www.MedChemE/Fluvastatin-D6-sodium.html sodium(XU 62-320 (D6) Cat. No.: HY-14664ASFluvastatin (XU 62-320 free acid) is a first fullysynthetic, competitive HMG-CoA reductaseinhibitor with an IC of 8 nM. Fluvastatin50protects vascular smooth muscle cells againstoxidative stress through the Nrf2

40、-dependentantioxidant pathway.Fluvastatin D6 sodium (XU 62-320 D6) is deuteriumlabeled Fluvastatin sodium. Fluvastatin sodium (XU62320) is a first fully synthetic, competitiveHMG-CoA reductase inhibitor with an IC of 850nM.Purity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mgPurity: 98%Clinical Data: N

41、o Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Fluvastatin-sodium.html Fluvastatin HYPERLINK https:/www.MedChemE/Fluvastatin-sodium.html HYPERLINK https:/www.MedChemE/Fluvastatin-sodium.html sodium(XU 62-320) Cat. No.: HY-14664A HYPERLINK https:/www.MedChemE/hesperetin-7-o-gluc

42、oside.html Hesperetin HYPERLINK https:/www.MedChemE/hesperetin-7-o-glucoside.html HYPERLINK https:/www.MedChemE/hesperetin-7-o-glucoside.html 7-O-glucosideCat. No.: HY-125130Fluvastatin sodium (XU 62320) is a first fullysynthetic, competitive HMG-CoA reductaseinhibitor with an IC of 8 nM. Fluvastati

43、n sodium50protects vascular smooth muscle cells againstoxidative stress through the Nrf2-dependentantioxidant pathway.Hesperetin 7-O-glucoside is produced by theenzymatic conversion of Hesperidin. Hesperetin7-O-glucoside is a potent human HMG-CoAreductase inhibitor and also effectively inhibitsthe g

44、rowth of Helicobacter pylori. Antihypertensiveeffect.Purity: 99.90%Clinical Data: LaunchedSize: 10 mM 1 mL, 50 mg, 100 mgPurity: 98.08%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/HMG499.html HMG499Cat. No.: HY-114316 HYPERLINK https:/www.MedChemE/Lovastatin.h

45、tml Lovastatin(Mevinolin) Cat. No.: HY-N0504HMG499 is a potent and selective HMG-CoAreductase inhibitor with an IC of 0.41 M.50HMG499 can prevent statins-induced accumulation ofHMGCR, reduce serum cholesterol levels anddecrease atherosclerosis.Lovastatin is a cell-permeable HMG-CoAreductase inhibito

46、r used to lower cholesterol.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mgPurity: 99.93%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/lovastatin-hydroxy-acid-sodium.html Lovastatin HYPERLINK https:/www.MedChemE/lovastatin-hydroxy-acid

47、-sodium.html HYPERLINK https:/www.MedChemE/lovastatin-hydroxy-acid-sodium.html hydroxy HYPERLINK https:/www.MedChemE/lovastatin-hydroxy-acid-sodium.html HYPERLINK https:/www.MedChemE/lovastatin-hydroxy-acid-sodium.html acid HYPERLINK https:/www.MedChemE/lovastatin-hydroxy-acid-sodium.html HYPERLINK

48、https:/www.MedChemE/lovastatin-hydroxy-acid-sodium.html sodium HYPERLINK https:/www.MedChemE/lovastatin-hydroxy-acid-sodium.html HYPERLINK https:/www.MedChemE/lovastatin-d3.html Lovastatin-d3(Mevinolinic acid sodium) Cat. No.: HY-123672 (Mevinolin-d3) Cat. No.: HY-N0504S2Lovastatin hydroxy acid sodi

49、um (Mevinolinic acidsodium) is a highly potent inhibitor of HMG-CoAreductase with a K of 0.6 nM.iLovastatin-d3 is deuterium labeled Lovastatin.Lovastatin is a cell-permeable HMG-CoA reductaseinhibitor used to lower cholesterol.Purity: 98.62%Clinical Data: No Development ReportedSize: 5 mgPurity: 98%

50、Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/lovastatin-d3-hydroxy-acid-sodium.html Lovastatin-d3 HYPERLINK https:/www.MedChemE/lovastatin-d3-hydroxy-acid-sodium.html HYPERLINK https:/www.MedChemE/lovastatin-d3-hydroxy-acid-sodium.html hydroxy HYPERLINK https:

51、/www.MedChemE/lovastatin-d3-hydroxy-acid-sodium.html HYPERLINK https:/www.MedChemE/lovastatin-d3-hydroxy-acid-sodium.html acid HYPERLINK https:/www.MedChemE/lovastatin-d3-hydroxy-acid-sodium.html HYPERLINK https:/www.MedChemE/lovastatin-d3-hydroxy-acid-sodium.html sodium HYPERLINK https:/www.MedChem

52、E/lovastatin-d3-hydroxy-acid-sodium.html HYPERLINK https:/www.MedChemE/lovastatin-d9.html Lovastatin-d9Cat. No.: HY-123672S Cat. No.: HY-N0504S1Lovastatin-d3 hydroxy acid (Mevinolinic acid-d3)sodium is the deuterium labeled Lovastatin hydroxyacid sodium. Lovastatin hydroxy acid sodium(Mevinolinic ac

53、id sodium) is a highly potentinhibitor of HMG-CoA reductase with a K of 0.6inM.Lovastatin-d9 is the deuterium labeled Lovastatin.Lovastatin is a cell-permeable HMG-CoAreductase inhibitor used to lower cholesterol.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mgPurity: 98%Clinical D

54、ata: No Development ReportedSize: 1 mg, 5 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/Meglutol.html Meglutol(Dicrotalic acid; 3-Hydroxy-3-methylglutaric acid) Cat. No.: HY-B1189 HYPERLINK https:/www.MedChemE/mevastatin.html Mevastatin(Compactin; ML236B)

55、 Cat. No.: HY-17408Meglutol is an antilipemic agent which lowerscholesterol, triglycerides, serumbeta-lipoproteins and phospholipids, and inhibitsthe activity of hydroxymethylglutarryl CoAreductases, which is the rate limiting enzyme inthe biosynthesis of cholesterol.Mevastatin (Compactin) is a firs

56、t HMG-CoAreductase inhibitor that belongs to the statinsclass. Mevastatin is a lipid-lowering agent, andinduces apoptosis, arrests cancer cells in G /G0 1phase.Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mgPurity: 99.20%Clinical Data: No Development ReportedSize: 10 mM 1

57、mL, 50 mg, 100 mg, 500 mg HYPERLINK https:/www.MedChemE/Monacolin_J.html Monacolin HYPERLINK https:/www.MedChemE/Monacolin_J.html HYPERLINK https:/www.MedChemE/Monacolin_J.html J(Antibiotic MB 530A; Lovastatin diol lactone) Cat. No.: HY-104051 HYPERLINK https:/www.MedChemE/pitavastatin.html Pitavast

58、atin(NK-104) Cat. No.: HY-B0144AMonacolin J is an inhibitor of cholesterolbiosynthesis, and inhibits the activity ofHMG-CoA reductase.Pitavastatin (NK-104) is a potenthydroxymethylglutaryl-CoA (HMG-CoA) reductaseinhibitor. Pitavastatin inhibits cholesterolsynthesis from acetic acid with an IC of 5.8

59、 nM50in HepG2 cells.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/pitavastatin-calcium.html Pitavastatin HYPERLINK https:/www.MedChemE/pitavastatin-calcium.html HYPERLINK https:/www.MedChemE/pitavasta

60、tin-calcium.html Calcium(NK-104 hemicalcium; Pitavastatin hemicalcium) Cat. No.: HY-B0144 HYPERLINK https:/www.MedChemE/Pitavastatin-D4.html Pitavastatin HYPERLINK https:/www.MedChemE/Pitavastatin-D4.html HYPERLINK https:/www.MedChemE/Pitavastatin-D4.html D4(NK-104 D4) Cat. No.: HY-B0144ASPitavastat