Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(E,3R,5S)-7-(4-(3-(4-fluorophenyl)pentan-3-yl)-2-isopropylphenyl)-3,5-dihydroxyhept-6-enoic acid | competitive inhibitor, shows slight inhibitory activity | Rattus norvegicus | |
fluvastatin | - |
Rattus norvegicus | |
mevastatin | - |
Rattus norvegicus | |
additional information | (E,3R,5S)-7-(4-(3-(4-fluorophenyl)pentan-3-yl)phenyl)-3,5-dihydroxyhept-6-enoic acid shows no apparent HMGR inhibitory activity even at 100 mM | Rattus norvegicus | |
sodium (E,3R,5S)-7-(2-(2-fluorophenyl)-4-(3-phenylpentan-3-yl)phenyl)-3,5-dihydroxy-hept-6-enoate | has almost no effect on the activity | Rattus norvegicus | |
sodium (E,3R,5S)-7-(2-(3-fluorophenyl)-4-(3-phenylpentan-3-yl)phenyl)-3,5-dihydroxy-hept-6-enoate | - |
Rattus norvegicus | |
sodium (E,3R,5S)-7-(2-(4-fluorophenyl)-4-(3-phenylpentan-3-yl)phenyl)-3,5-dihydroxy-hept-6-enoate | shows the most potent inhibitory activity among compounds comparable with that of clinically useful mevastatin | Rattus norvegicus | |
sodium (E,3R,5S)-7-(2-phenyl-4-(3-phenylpentan-3-yl)phenyl)-3,5-dihydroxyhept-6-enoate | has almost no effect on the activity | Rattus norvegicus | |
sodium (E,3R,5S)-7-(4-(3-(2-fluorophenyl)pentan-3-yl)-2-isopropylphenyl)-3,5-dihydroxyhept-6-enoate | - |
Rattus norvegicus | |
sodium (E,3R,5S)-7-(4-(3-(3-fluorophenyl)pentan-3-yl)-2-isopropylphenyl)-3,5-dihydroxyhept-6-enoate | - |
Rattus norvegicus | |
sodium (E,3R,5S)-7-(4-(3-phenylpentan-3-yl)-2-isopropylphenyl)-3,5-dihydroxyhept-6-enoate | - |
Rattus norvegicus |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Rattus norvegicus | - |
- |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
DL-3-hydroxy-3-methylglutaryl-CoA + NADPH | - |
Rattus norvegicus | mevalonate + CoA + NADP+ | - |
? |
Synonyms | Comment | Organism |
---|---|---|
3-hydroxy-3-methylglutaryl coenzyme A reductase | - |
Rattus norvegicus |
HMG-CoA reductase | - |
Rattus norvegicus |
HMGR | - |
Rattus norvegicus |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.003 | - |
DL-[3-14C]3-hydroxy-3-methylglutaryl-CoA (0.37 MBq) and 10 mg protein of microsomal fraction incubated at 37°C for 30 min | Rattus norvegicus | fluvastatin | |
0.04 | - |
DL-[3-14C]3-hydroxy-3-methylglutaryl-CoA (0.37 MBq) and 10 mg protein of microsomal fraction incubated at 37°C for 30 min | Rattus norvegicus | mevastatin | |
0.15 | - |
DL-[3-14C]3-hydroxy-3-methylglutaryl-CoA (0.37 MBq) and 10 mg protein of microsomal fraction incubated at 37°C for 30 min | Rattus norvegicus | sodium (E,3R,5S)-7-(2-(4-fluorophenyl)-4-(3-phenylpentan-3-yl)phenyl)-3,5-dihydroxy-hept-6-enoate | |
0.82 | - |
DL-[3-14C]3-hydroxy-3-methylglutaryl-CoA (0.37 MBq) and 10 mg protein of microsomal fraction incubated at 37°C for 30 min | Rattus norvegicus | sodium (E,3R,5S)-7-(2-(2-fluorophenyl)-4-(3-phenylpentan-3-yl)phenyl)-3,5-dihydroxy-hept-6-enoate | |
0.85 | - |
DL-[3-14C]3-hydroxy-3-methylglutaryl-CoA (0.37 MBq) and 10 mg protein of microsomal fraction incubated at 37°C for 30 min | Rattus norvegicus | sodium (E,3R,5S)-7-(2-phenyl-4-(3-phenylpentan-3-yl)phenyl)-3,5-dihydroxyhept-6-enoate | |
1.2 | - |
DL-[3-14C]3-hydroxy-3-methylglutaryl-CoA (0.37 MBq) and 10 mg protein of microsomal fraction incubated at 37°C for 30 min | Rattus norvegicus | sodium (E,3R,5S)-7-(2-(3-fluorophenyl)-4-(3-phenylpentan-3-yl)phenyl)-3,5-dihydroxy-hept-6-enoate | |
1.8 | - |
DL-[3-14C]3-hydroxy-3-methylglutaryl-CoA (0.37 MBq) and 10 mg protein of microsomal fraction incubated at 37°C for 30 min | Rattus norvegicus | sodium (E,3R,5S)-7-(4-(3-phenylpentan-3-yl)-2-isopropylphenyl)-3,5-dihydroxyhept-6-enoate | |
2.2 | - |
DL-[3-14C]3-hydroxy-3-methylglutaryl-CoA (0.37 MBq) and 10 mg protein of microsomal fraction incubated at 37°C for 30 min | Rattus norvegicus | (E,3R,5S)-7-(4-(3-(4-fluorophenyl)pentan-3-yl)-2-isopropylphenyl)-3,5-dihydroxyhept-6-enoic acid | |
7.4 | - |
DL-[3-14C]3-hydroxy-3-methylglutaryl-CoA (0.37 MBq) and 10 mg protein of microsomal fraction incubated at 37°C for 30 min | Rattus norvegicus | sodium (E,3R,5S)-7-(4-(3-(2-fluorophenyl)pentan-3-yl)-2-isopropylphenyl)-3,5-dihydroxyhept-6-enoate | |
26 | - |
DL-[3-14C]3-hydroxy-3-methylglutaryl-CoA (3.7 MBq) and 10 mg protein of microsomal fraction incubated at 37°C for 30 min | Rattus norvegicus | (E,3R,5S)-7-(4-(3-(4-fluorophenyl)pentan-3-yl)-2-isopropylphenyl)-3,5-dihydroxyhept-6-enoic acid | |
92 | - |
DL-[3-14C]3-hydroxy-3-methylglutaryl-CoA (3.7 MBq) and 10 mg protein of microsomal fraction incubated at 37°C for 30 min | Rattus norvegicus | sodium (E,3R,5S)-7-(4-(3-(3-fluorophenyl)pentan-3-yl)-2-isopropylphenyl)-3,5-dihydroxyhept-6-enoate |