Your metabolic tools for drug discovery & development GIBCO® microsomes & other liver subcellular fractions
- Large pooled lots for reproducible, long-term studies
- Fractions carefully isolated by experts in hepatic biology
- Microsomes functionally tested for select CYP450 and Phase II enzyme activities
Human microsome pools and subcellular fractions
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:
- Cytochrome P450 inhibition studies
- Metabolic stability
- Cytochrome P450 phenotyping
- Metabolite characterization
50 donor human liver microsome pool
Designed to maximize functionality for all your study types- suitable for inhibition, clearance, or metabolic identification.
- Equal representation of all 50 donors
- Activities representing the typical patient population
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.
Life Technologies provides 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).
Table 1 - Relevant applications for liver subcellular fractions
| 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 |
Table 2 - Cytochrome P450 and Phase II enzymes tested in GIBCO® human microsome pools
| 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 |
Table 3 - Kinetic parameters for the GIBCO® 50 donor human liver microsome pool
| 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 |
Ordering Is Simple!
To call in orders please use the following information:
Asia-Pacific Sales:
Tel: 866.952.3559
Fax: 866.902.3559
Email: hepaticproducts@invitrogen.com
Invitrogen Japan Sales:
Tel: +81 3 5566 6160
Fax: +81 3 5566 6505
or order by email at jpinfo@invitrogen.com
| Product | Concentration | Quantity | Cat. No. | Price |
|---|---|---|---|---|
| Human microsomes, 50 donors | 20 mg/ml | 0.5 ml | HMMC-PL050 | $105 |
| Dog (beagle) microsomes | 20 mg/ml | 0.5 ml | DGMC-PL | $60 |
| Monkey (cynomolgus) microsomes | 20 mg/ml | 0.5 ml | MKMC-PL | $120 |
| Mouse (Balb/c) microsomes | 20 mg/ml | 0.5 ml | MSMC-PL | $45 |
| Rat (Sprague-Dawley) microsomes | 20 mg/ml | 0.5 ml | RTMC-PL | $35 |
| Human S9 fractions, pooled | 20 mg/ml | 1.0 ml | HMS9-PL | $85 |
| Dog (beagle) S9 fractions | 20 mg/ml | 1.0 ml | DGS9-PL | $65 |
| Monkey (cynomolgus) S9 fractions | 20 mg/ml | 1.0 ml | MKS9-PL | $80 |
| Mouse (CD-1) S9 fractions | 20 mg/ml | 1.0 ml | MSS9-PL | $45 |
| Rat (Sprague-Dawley) S9 fractions | 20 mg/ml | 1.0 ml | RTS9-PL | $35 |
| Fish (rainbow trout) S9 fractions | 20 mg/ml | 1.0 ml | TRS9-PL | $60 |
| Human cytosol, pooled | 20 mg/ml | 1.0 ml | HMCY-PL | $45 |
| Dog (beagle) cytosol | 20 mg/ml | 1.0 ml | DGCY-PL | $40 |
| Monkey (cynomolgus) cytosol | 20 mg/ml | 1.0 ml | MKCY-PL | $60 |
| Mouse (CD-1) cytosol | 20 mg/ml | 1.0 ml | MSCY-PL | $40 |
| Rat (Sprague-Dawley) cytosol | 20 mg/ml | 1.0 ml | RTCY-PL | $30 |
For Research Use Only. Not for use in diagnostic procedures.