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Subcellular fractions, derived from the endoplasmic reticulum of liver, contain a rich variety of metabolic enzymes for assessing the in vitro metabolism of drug candidates (Table 1) and are suitable for a variety of experiments:
50 donor human liver microsome pool
Designed to maximize functionality for all your study types- suitable for inhibition, clearance, or metabolic identification.
11 specialty human liver microsome pools
Prepared with 5 to 20 donors each and pooled for your convenience according to age, gender, body mass index, high 3A activity, and high 2D6 activity.
Customized microsome pools
Our scientists will create a customized pool specifically for your unique research needs using our large, fully characterized single-donor database.
We provide liver subcellular fractions from a variety of tox species, including human, nonhuman primates (Cynomolgus Monkey and Rhesus Monkey), dog (Beagle), rat (Sprague-Dawley), mouse (CD-1), and trout (Oncorhynchus mykiss). Custom species are available upon request.
Each product contains an average representative pool of donors. Human microsome pools are fully characterized (Km and Vmax) according to GLP standards for major cytochrome P450 activities and select Phase II enzymes using FDA recommended substrates (Tables 2-3).
Metabolic Enzymes | Liver Microsomes | Liver S9 Fractions | Liver Cytosol |
---|---|---|---|
Aldehyde Oxidase | X | X | |
Cytochromes P450 (CYP) | X | X | |
Flavin Monooxygenases (FMO) | X | X | |
Glutathione Transferase (GST) | X | ||
Monamine Oxidase (MAO) | X | ||
Sulfurotrnasferase (SULT) | X | X | |
Uridine Glucuronide Transferase (UGT) | X | X |
Enzyme Monitored | Marker Substrate | Incubation (min) | Protein Concentration (mg/ml) | Metabolite |
---|---|---|---|---|
CYP1A1/2 | Phenacetin | 30 | 0.1 | Acetaminophen |
CYP2A6 | Coumarin | 5 | 0.025 | 7-Hydroxycoumarin |
CYP2B6 | Bupropion | 20 | 0.25 | Hydroxybupropion |
CYP2C8 | Paclitaxel | 10 | 0.075 | 6α-Hydroxypaclitaxel |
CYP2C9 | Tolbutamide | 20 | 0.1 | Hydroxytolubutamide |
CYP2C19 | (S) Mephenytoin | 30 | 0.1 | 4'-Hydroxymephenytoin |
CYP2D6 | Dextromethorphan | 15 | 0.2 | Dextrorphan |
CYP2E1 | Chlorzoxazone | 20 | 0.1 | 6-Hydroxychlorzoxazone |
CYP3A4/5 | Midazolam | 4 | 0.025 | 1'-Hydroxymidazolam |
CYP3A4/5 | Testosterone | 7 | 0.05 | 6β-Hydroxytestosterone |
CYP4A11 | Lauric Acid | 15 | 0.2 | 12-Hydroxydecanoic Acid |
FMO | Methyl p-Tolylsulfide | 15 | 0.05 | Methyl p-Tolylsulfide |
UGT | 7-Hydroxycoumarin | 30 | 0.2 | 7-Hydroxycoumarin Glucuronide |
Isoform | Metabolite | Km(μM) | Vmax (nmol/min/mg) |
---|---|---|---|
CYP1A2 | Acetaminophen | 78 | 0.73 |
CYP2A6 | 7-Hydroxycoumarin | 1.1 | 0.53 |
CYP2B6 | Hydroxybupropion | 64 | 0.29 |
CYP2C8 | 6α-Hydroxypaclitaxel | 5.5 | 0.15 |
CYP2C9 | Hydroxytolbutamide | 220 | 0.19 |
CYP2C19 | 4'-Hydroxymephenytoin | 34 | 0.031 |
CYP2D6 | Dextrophan | 3.2 | 0.13 |
CYP2E1 | 6-Hydroxychlorzoxazone | 70 | 1.4 |
CYP3A4 | 6β-Hydroxytestosterone | 19 | 4.0 |
CYP3A4 | 1'-Hydroxymidazolam | 1.6 | 1.1 |
For Research Use Only. Not for use in diagnostic procedures.